Ibuprofen 5% foam
Drugs for the relief of soft-tissue inflammation and topical pain relief
Active ingredients:
Ibuprofen
No active safety alerts
Official documents, adverse reaction reporting, and safety monitoring
Report a side effect
Submit a Yellow Card report to the MHRA
Official medicine documents
Source: MHRA Products DatabaseOGL 3.0
Updated 3 months ago(16 Jan 2026)Safety monitoring data
Yellow Card reports
MHRA
The MHRA Yellow Card scheme collects reports of suspected side effects from healthcare professionals and patients. View the Drug Analysis Profile (iDAP) for real-world adverse reaction data.
View Drug Analysis Profile
Suspected adverse reactions reported for Ibuprofen
Browse all iDAP reports
Interactive Drug Analysis Profiles for all medicines
Report a side effect
Submit a Yellow Card report to the MHRA
Data from the MHRA Yellow Card scheme. A reported reaction does not necessarily mean the medicine caused it. Contains public sector information licensed under the Open Government Licence v3.0.
EudraVigilance
EMA
The European Medicines Agency (EMA) collects suspected adverse reaction reports from across the EU/EEA through the EudraVigilance system. Search for safety data on this medicine.
View EudraVigilance report
Suspected adverse reactions reported for Ibuprofen
About EudraVigilance
Learn about EU pharmacovigilance and safety monitoring
EudraVigilance data is published by the European Medicines Agency (EMA). A suspected adverse reaction is not necessarily caused by the medicine.
2 branded products available
Show details
Part of the Brufen brand family (generic: Ibuprofen)
2 products
MHRA licensed products
View all licensed products for Ibuprofen on the MHRA register
Therapeutically similar medicines
Show details
Diclofenac sodium 1% gel
Gel
1%
Same therapeutic group
Ibuprofen 200mg medicated plasters
Other
200mg
Same therapeutic group
Ketoprofen 10% gel
Gel
10%
Same therapeutic group
Diclofenac 140mg medicated plasters
Other
140mg
Same therapeutic group
Diclofenac diethylammonium 2.32% gel
Gel
2.32%
Same therapeutic group
Similarity based on WHO Anatomical Therapeutic Chemical (ATC) classification and NHS BNF section grouping. Source data: NHS dm+d via TRUD (OGL v3.0), WHO ATC/DDD Index.
NHS prescribing volume and spending trends
Show details
Loading prescribing data...
Clinical guidelines and formulary information
British National Formulary
Ibuprofen
BNF
Drug monograph — bnf.nice.org.ukSource: British National Formulary, NICE. Joint Formulary Committee. Contains public sector information licensed under the Open Government Licence v3.0.
NICE clinical guidance(14)
Otitis media (acute): antimicrobial prescribing (NG91)
NG91
Guidance
Updated Mar 2022Urinary tract infection (lower): antimicrobial prescribing (NG109)
NG109
Guidance
Updated Oct 2018Sore throat (acute): antimicrobial prescribing (NG84)
NG84
Guidance
Updated Jan 2018Prostatitis (acute): antimicrobial prescribing (NG110)
NG110
Guidance
Updated Oct 2018Sinusitis (acute): antimicrobial prescribing (NG79)
NG79
Guidance
Updated Oct 2017Bronchiolitis in children (QS122)
QS122
Quality standard
Updated Jun 2016Perioperative care in adults (NG180)
NG180
NICE guideline
Updated Aug 2020End of life care for infants, children and young people with life-limiting conditions: planning and management (NG61)
NG61
NICE guideline
Updated Jul 2019Fever in under 5s: assessment and initial management (NG143)
NG143
NICE guideline
Updated Nov 2021Fractures (non-complex): assessment and management (NG38)
NG38
NICE guideline
Updated Feb 2016Cough (acute): antimicrobial prescribing (NG120)
NG120
Guidance
Updated Feb 2019Targeted muscle reinnervation for managing limb amputation pain (HTG750)
HTG750
Guidance
Updated Jun 2025Gastro-oesophageal reflux disease and dyspepsia in adults: investigation and management (CG184)
CG184
Clinical guideline
Updated Oct 2019Drug allergy: diagnosis and management (CG183)
CG183
Clinical guideline
Updated Sept 2014Source: National Institute for Health and Care Excellence (NICE). Contains public sector information licensed under the Open Government Licence v3.0.
Check stock at pharmacies and supply information
Show details
Pharmacy stock checkers
Search for this medicine at major UK pharmacy chains. These links open the retailer's own website — results depend on their current online catalogue.
Supply & product information
Official product databases and supply status monitoring
Pharmacy links redirect to the retailer's own search and do not represent real-time stock levels. emc (electronic medicines compendium) is operated by Datapharm Ltd. Shortage information sourced from NHS Specialist Pharmacy Service (SPS), sps.nhs.uk.
Codes for healthcare professionals and prescribing systems
Show details
These codes are used by healthcare IT systems and prescribers to identify this medicine.
NHS UK identifiers
Browse tools
SNOMED CT and dm+d codes from NHS TRUD (Technology Reference data Update Distribution), licensed under the Open Government Licence v3.0. BNF codes from NHS Business Services Authority (NHSBSA). ATC codes from the WHO Collaborating Centre for Drug Statistics Methodology (whocc.no).
Active and completed clinical studies from ClinicalTrials.gov
Show details
Searching UK clinical trials...
Source: ClinicalTrials.gov, a database of the U.S. National Library of Medicine (NLM), National Institutes of Health (NIH). Data accessed via ClinicalTrials.gov API v2. Trial information is provided for research purposes and does not constitute medical advice.
Pharmacology and chemical data from DrugBank
Key facts
Drug status
Approved
Major interactions
67 found
Half-life
1.2-2 hours
Mechanism
The exact mechanism of action of ibuprofen is unknown.
Food interactions
2 warnings
Human targets
13 targets
Data: DrugBank · CC BY-NC 4.0
Pharmacokinetics at a glance
Absorption
1 to 2 hours
It is very well absorbed orally and the peak serum concentration can be attained in 1 to 2 hours after extravascular administration.…
Half-life
1.2-2 hours
The serum half-life of ibuprofen is 1.2-2 hours.
[A39092]
In patients with a compromised liver function, the half-life can be prolonged to 3.1-3.4…
[A39092]
In patients with a compromised liver function, the half-life can be prolonged to 3.1-3.4…
Protein binding
99%
Ibuprofen dosage is more than 99% bound to plasma proteins and site II of purified albumin, binding appears to be saturable and becomes non-linear at concentrations exceeding 20 mcg/ml.
[A39092]…
[A39092]…
Volume of distribution
0.1 L/kg
The apparent volume of distribution of ibuprofen is of 0.1 L/kg.
[A39195]
[A39195]
Metabolism
53-65%
Ibuprofen is rapidly metabolized and biotransformed in the liver to the formation of major metabolites which are the hydroxylated and carboxylated derivatives.
[A39092]…
[A39092]…
Elimination
90%
Ibuprofen is rapidly metabolized and eliminated in the urine thus, this via accounts for more than 90% of the administered dose.…
Clearance
3-13 L/h
The clearance rate ranges between 3-13 L/h depending on the route of administration, enantiomer type and dosage.
[A39190]
[A39190]
Pharmacokinetic data: DrugBank · CC BY-NC 4.0
Status:
Approved
Investigational
Small molecule
About this compound
Ibuprofen is a non-steroidal anti-inflammatory drug (NSAID) derived from propionic acid and it is considered the first of the propionics.[A39074] The formula of ibuprofen is 2-(4-isobutylphenyl) propionic acid and its initial development was in 1960 while researching for a safer alternative for aspirin.[A39075] Ibuprofen was finally patented in 1961 and this drug was first launched against rheumatoid arthritis in the UK in 1969 and USA in 1974. It was the first available over-the-counter NSAID.[A39076]
On the available products, ibuprofen is administered as a racemic mixture. Once administered, the R-enantiomer undergoes extensive interconversion to the S-enantiomer in vivo by the activity of the alpha-methylacyl-CoA racemase. In particular, it is generally proposed that the S-enantiomer is capable of eliciting stronger pharmacological activity than the R-enantiomer.[A39194]
On the available products, ibuprofen is administered as a racemic mixture. Once administered, the R-enantiomer undergoes extensive interconversion to the S-enantiomer in vivo by the activity of the alpha-methylacyl-CoA racemase. In particular, it is generally proposed that the S-enantiomer is capable of eliciting stronger pharmacological activity than the R-enantiomer.[A39194]
Properties:
View FDA drug labelsolid
Avg. mass: 206.28 Da
DrugBank indication
Ibuprofen is the most commonly used and prescribed NSAID. It is a very common over-the-counter medication widely used as an analgesic, anti-inflammatory and antipyretic.
[A39096]
The use of ibuprofen and its enantiomer DB09213 in a racemic mix is common for the management of mild to moderate pain related to dysmenorrhea, headache, migraine, postoperative dental pain, spondylitis, osteoarthritis, rheumatoid arthritis, and soft tissue disorder.
[A39097]
Due to its activity against prostaglandin and thromboxane synthesis, ibuprofen has been attributed to alteration of platelet function and prolongation of gestation and labour.
[A39092]
As ibuprofen is a widely used medication, the main therapeutic indications are:
* Patent Ductus Arteriosus - it is a neonatal condition wherein the ductus arteriosus (blood vessel that connects the main pulmonary artery to the proximal descending aorta) fails to close after birth causing severe risk of heart failure. The prostaglandin inhibition of ibuprofen has been studied for the treatment of this condition as it is known that prostaglandin E2 is responsible for keeping the ductus arteriosus open.
[A39100]
* Rheumatoid- and osteo-arthritis - ibuprofen is very commonly used in the symptomatic treatment of inflammatory, musculoskeletal and rheumatic disorders.
[A39176]
* Cystic fibrosis - the use of high dosages of ibuprofen has been proven to decrease inflammation and decreasing polymorphonuclear cell influx in the lungs.
[A39177]
* Orthostatic hypotension - ibuprofen can induce sodium retention and antagonize the effect of diuretics which has been reported to be beneficial for patients with severe orthostatic hypotension.
[A1651]
* Dental pain - ibuprofen is used to manage acute and chronic orofacial pain.
[A10901]
* Pain - ibuprofen is widely used to reduce minor aches and pains as well as to reduce fever and manage dysmenorrhea.
It is very commonly used for the relief of acute indications such as fever and tension headaches.
[A39092]
It is also used to manage mild to moderate pain and moderate to severe pain as an adjunct to opioid analgesics.
[L40208]
* Investigational uses - efforts have been put into developing ibuprofen for the prophylaxis of Alzheimer's disease, Parkinson disease, and breast cancer.
[A39092]
[A39096]
The use of ibuprofen and its enantiomer DB09213 in a racemic mix is common for the management of mild to moderate pain related to dysmenorrhea, headache, migraine, postoperative dental pain, spondylitis, osteoarthritis, rheumatoid arthritis, and soft tissue disorder.
[A39097]
Due to its activity against prostaglandin and thromboxane synthesis, ibuprofen has been attributed to alteration of platelet function and prolongation of gestation and labour.
[A39092]
As ibuprofen is a widely used medication, the main therapeutic indications are:
* Patent Ductus Arteriosus - it is a neonatal condition wherein the ductus arteriosus (blood vessel that connects the main pulmonary artery to the proximal descending aorta) fails to close after birth causing severe risk of heart failure. The prostaglandin inhibition of ibuprofen has been studied for the treatment of this condition as it is known that prostaglandin E2 is responsible for keeping the ductus arteriosus open.
[A39100]
* Rheumatoid- and osteo-arthritis - ibuprofen is very commonly used in the symptomatic treatment of inflammatory, musculoskeletal and rheumatic disorders.
[A39176]
* Cystic fibrosis - the use of high dosages of ibuprofen has been proven to decrease inflammation and decreasing polymorphonuclear cell influx in the lungs.
[A39177]
* Orthostatic hypotension - ibuprofen can induce sodium retention and antagonize the effect of diuretics which has been reported to be beneficial for patients with severe orthostatic hypotension.
[A1651]
* Dental pain - ibuprofen is used to manage acute and chronic orofacial pain.
[A10901]
* Pain - ibuprofen is widely used to reduce minor aches and pains as well as to reduce fever and manage dysmenorrhea.
It is very commonly used for the relief of acute indications such as fever and tension headaches.
[A39092]
It is also used to manage mild to moderate pain and moderate to severe pain as an adjunct to opioid analgesics.
[L40208]
* Investigational uses - efforts have been put into developing ibuprofen for the prophylaxis of Alzheimer's disease, Parkinson disease, and breast cancer.
[A39092]
Also known as(236)
(±)-2-(p-isobutylphenyl)propionic acid
(±)-ibuprofen
(±)-p-isobutylhydratropic acid
(±)-α-methyl-4-(2-methylpropyl)benzeneacetic acid
(4-isobutylphenyl)-α-methylacetic acid
(RS)-ibuprofen
2-(4-isobutylphenyl)propanoic acid
4-isobutylhydratropic acid
Dosage forms(318)
Kit (Ophthalmic; Oral; Respiratory (inhalation); Topical)
Cream; kit; liquid; ointment; swab; tablet (Oral; Topical)
Kit (Ophthalmic; Oral; Topical)
Tablet (Not applicable)
Injection, powder, for solution (Intramuscular)
Capsule (Oral) — 400.000 mg
Gel (Cutaneous) — 5.00 g
Suspension (Oral) — 2000.000 mg
Molecular properties(18)
Drug interactions(1682)
Known interactions with other medications. Always consult a healthcare professional.
Amlodipine
Moderate
The metabolism of Ibuprofen can be decreased when combined with Amlodipine.
The risk or severity of hypertension can be increased when Midodrine is combined with Ibuprofen.
Isoetharine
Unknown severity
The risk or severity of hypertension can be increased when Isoetharine is combined with Ibuprofen.
Zolmitriptan
Unknown severity
The risk or severity of hypertension can be increased when Zolmitriptan is combined with Ibuprofen.
Norepinephrine
Unknown severity
The risk or severity of hypertension can be increased when Norepinephrine is combined with Ibuprofen.
Droperidol
Unknown severity
The risk or severity of hypertension can be increased when Droperidol is combined with Ibuprofen.
The risk or severity of hypertension can be increased when Doxapram is combined with Ibuprofen.
The risk or severity of hypertension can be increased when Atropine is combined with Ibuprofen.
The risk or severity of hypertension can be increased when Linezolid is combined with Ibuprofen.
Metaraminol
Unknown severity
The risk or severity of hypertension can be increased when Metaraminol is combined with Ibuprofen.
Furazolidone
Unknown severity
The risk or severity of hypertension can be increased when Furazolidone is combined with Ibuprofen.
Nicergoline
Unknown severity
The risk or severity of hypertension can be increased when Nicergoline is combined with Ibuprofen.
Methoxamine
Unknown severity
The risk or severity of hypertension can be increased when Methoxamine is combined with Ibuprofen.
Isoflurane
Unknown severity
The risk or severity of hypertension can be increased when Isoflurane is combined with Ibuprofen.
Propiomazine
Unknown severity
The risk or severity of hypertension can be increased when Propiomazine is combined with Ibuprofen.
The risk or severity of hypertension can be increased when Minaprine is combined with Ibuprofen.
Orciprenaline
Unknown severity
The risk or severity of hypertension can be increased when Orciprenaline is combined with Ibuprofen.
Phenmetrazine
Unknown severity
The risk or severity of hypertension can be increased when Phenmetrazine is combined with Ibuprofen.
The risk or severity of hypertension can be increased when Ritodrine is combined with Ibuprofen.
Bitolterol
Unknown severity
The risk or severity of hypertension can be increased when Bitolterol is combined with Ibuprofen.
Oxymetazoline
Unknown severity
The risk or severity of hypertension can be increased when Oxymetazoline is combined with Ibuprofen.
Naratriptan
Unknown severity
The risk or severity of hypertension can be increased when Naratriptan is combined with Ibuprofen.
Frovatriptan
Unknown severity
The risk or severity of hypertension can be increased when Frovatriptan is combined with Ibuprofen.
Isoprenaline
Unknown severity
The risk or severity of hypertension can be increased when Ibuprofen is combined with Isoprenaline.
Arbutamine
Unknown severity
The risk or severity of hypertension can be increased when Ibuprofen is combined with Arbutamine.
Dutasteride
Unknown severity
The risk or severity of hypertension can be increased when Ibuprofen is combined with Dutasteride.
Desflurane
Unknown severity
The risk or severity of hypertension can be increased when Ibuprofen is combined with Desflurane.
Isocarboxazid
Unknown severity
The risk or severity of hypertension can be increased when Ibuprofen is combined with Isocarboxazid.
The risk or severity of hypertension can be increased when Ibuprofen is combined with Fenoterol.
Pirbuterol
Unknown severity
The risk or severity of hypertension can be increased when Ibuprofen is combined with Pirbuterol.
Ephedra sinica root
Unknown severity
The risk or severity of hypertension can be increased when Ibuprofen is combined with Ephedra sinica root.
The risk or severity of hypertension can be increased when Ibuprofen is combined with Ephedrine.
Procaterol
Unknown severity
The risk or severity of hypertension can be increased when Ibuprofen is combined with Procaterol.
Clenbuterol
Unknown severity
The risk or severity of hypertension can be increased when Ibuprofen is combined with Clenbuterol.
Bambuterol
Unknown severity
The risk or severity of hypertension can be increased when Ibuprofen is combined with Bambuterol.
4-Methoxyamphetamine
Unknown severity
The risk or severity of hypertension can be increased when Ibuprofen is combined with 4-Methoxyamphetamine.
Phendimetrazine
Unknown severity
The risk or severity of hypertension can be increased when Ibuprofen is combined with Phendimetrazine.
Epicaptopril
Unknown severity
The risk or severity of hypertension can be increased when Ibuprofen is combined with Epicaptopril.
Clorgiline
Unknown severity
The risk or severity of hypertension can be increased when Ibuprofen is combined with Clorgiline.
1-benzylimidazole
Unknown severity
The risk or severity of hypertension can be increased when Ibuprofen is combined with 1-benzylimidazole.
The risk or severity of hypertension can be increased when Ibuprofen is combined with Nialamide.
The risk or severity of hypertension can be increased when Ibuprofen is combined with Amibegron.
The risk or severity of hypertension can be increased when Ibuprofen is combined with Naluzotan.
The risk or severity of hypertension can be increased when Ibuprofen is combined with Pizotifen.
Solabegron
Unknown severity
The risk or severity of hypertension can be increased when Ibuprofen is combined with Solabegron.
Esmirtazapine
Unknown severity
The risk or severity of hypertension can be increased when Ibuprofen is combined with Esmirtazapine.
Nitrous oxide
Unknown severity
The risk or severity of hypertension can be increased when Ibuprofen is combined with Nitrous oxide.
Xylometazoline
Unknown severity
The risk or severity of hypertension can be increased when Ibuprofen is combined with Xylometazoline.
Dexmethylphenidate
Unknown severity
The risk or severity of hypertension can be increased when Ibuprofen is combined with Dexmethylphenidate.
Isometheptene
Unknown severity
The risk or severity of hypertension can be increased when Ibuprofen is combined with Isometheptene.
Showing 50 of 1682 interactions
Food & lifestyle interactions
Avoid Alcohol
Avoid alcohol.
Take With Food
Take with food. Food reduces irritation.
Toxicity & overdose
The symptoms of overdose are presented in individuals that consumed more than 99 mg/kg. Most common symptoms of overdose are abdominal pain, nausea, vomiting, lethargy, vertigo, drowsiness (somnolence), dizziness and insomnia. Other symptoms of overdose include headache, loss of consciousness, tinnitus, CNS depression, convulsions and seizures.
May rarely cause metabolic acidosis, abnormal hepatic function, hyperkalemia, renal failure, dyspnea, respiratory depression, coma, acute renal failure, and apnea (primarily in very young pediatric patients).
[A39200]
The reported LD50 of ibuprofen is of 636 mg/kg in rat, 740 mg/kg in mouse and 495 mg/kg in guinea pig.MSDS
May rarely cause metabolic acidosis, abnormal hepatic function, hyperkalemia, renal failure, dyspnea, respiratory depression, coma, acute renal failure, and apnea (primarily in very young pediatric patients).
[A39200]
The reported LD50 of ibuprofen is of 636 mg/kg in rat, 740 mg/kg in mouse and 495 mg/kg in guinea pig.MSDS
How it works
Mechanism of action
The exact mechanism of action of ibuprofen is unknown. However, ibuprofen is considered an NSAID and thus it is a non-selective inhibitor of cyclooxygenase, which is an enzyme involved in prostaglandin (mediators of pain and fever) and thromboxane (stimulators of blood clotting) synthesis via the arachidonic acid pathway.[L4614]
Ibuprofen is a non-selective COX inhibitor and hence, it inhibits the activity of both COX-1 and COX-2. The inhibition of COX-2 activity decreases the synthesis of prostaglandins involved in mediating inflammation, pain, fever, and swelling while the inhibition of COX-1 is thought to cause some of the side effects of ibuprofen including GI ulceration.[A39195]
Ibuprofen is a non-selective COX inhibitor and hence, it inhibits the activity of both COX-1 and COX-2. The inhibition of COX-2 activity decreases the synthesis of prostaglandins involved in mediating inflammation, pain, fever, and swelling while the inhibition of COX-1 is thought to cause some of the side effects of ibuprofen including GI ulceration.[A39195]
Pharmacodynamics
Ibuprofen has multiple actions in different inflammatory pathways involved in acute and chronic inflammation. The main effects reported in ibuprofen are related to the control of pain, fever and acute inflammation by the inhibition of the synthesis of prostanoids by COX-1 and COX-2. Pain relief is attributed to peripheral affected regions and central nervous system effects in the pain transmission mediated by the dorsal horn and higher spinothalamic tract. Some reports have tried to link the pain regulation with a possible enhancement on the synthesis of endogenous cannabinoids and action on the NMDA receptors. The effect on pain has been shown to be related to the cortically evoked potentials.[A39190]
The antipyretic effect is reported to be linked to the effect on the prostanoid synthesis due to the fact that the prostanoids are the main signaling mediator of pyresis in the hypothalamic-preoptic region.[A39190]
The use of ibuprofen in dental procedures is attributed to the local inhibition of prostanoid production as well as to anti-oedemic activity and an increase of plasma beta-endorphins. Some reports have suggested a rapid local reduction of the expression of COX-2 in dental pulp derived by the administration of ibuprofen.[A39190]
The administration of ibuprofen in patients with rheumatic diseases has shown to control joint symptoms.[A39092]
Ibuprofen is largely used in OTC products such as an agent for the management of dysmenorrhea which has been proven to reduce the amount of menstrual prostanoids and to produce a reduction in the uterine hypercontractility.[A39181] As well, it has been reported to reduce significantly the fever and the pain caused by migraines.[A39182][A39183] This effect is thought to be related to the effect on platelet activation and thromboxane A2 production which produces local vascular effects in the affected regions. This effect is viable as ibuprofen can enter in the central nervous system.[A39190]
In the investigational uses of ibuprofen, it has been reported to reduce neurodegeneration when given in low doses over a long time.[A39184] On the other hand, its use in Parkinson disease is related to the importance of inflammation and oxidative stress in the pathology of this condition.[A39185] The use of ibuprofen for breast cancer is related to a study that shows a decrease of 50% in the rate of breast cancer.[A39186]
The antipyretic effect is reported to be linked to the effect on the prostanoid synthesis due to the fact that the prostanoids are the main signaling mediator of pyresis in the hypothalamic-preoptic region.[A39190]
The use of ibuprofen in dental procedures is attributed to the local inhibition of prostanoid production as well as to anti-oedemic activity and an increase of plasma beta-endorphins. Some reports have suggested a rapid local reduction of the expression of COX-2 in dental pulp derived by the administration of ibuprofen.[A39190]
The administration of ibuprofen in patients with rheumatic diseases has shown to control joint symptoms.[A39092]
Ibuprofen is largely used in OTC products such as an agent for the management of dysmenorrhea which has been proven to reduce the amount of menstrual prostanoids and to produce a reduction in the uterine hypercontractility.[A39181] As well, it has been reported to reduce significantly the fever and the pain caused by migraines.[A39182][A39183] This effect is thought to be related to the effect on platelet activation and thromboxane A2 production which produces local vascular effects in the affected regions. This effect is viable as ibuprofen can enter in the central nervous system.[A39190]
In the investigational uses of ibuprofen, it has been reported to reduce neurodegeneration when given in low doses over a long time.[A39184] On the other hand, its use in Parkinson disease is related to the importance of inflammation and oxidative stress in the pathology of this condition.[A39185] The use of ibuprofen for breast cancer is related to a study that shows a decrease of 50% in the rate of breast cancer.[A39186]
Pharmacokinetics
How the body processes this drug — absorption, distribution, metabolism, and elimination
Absorption
It is very well absorbed orally and the peak serum concentration can be attained in 1 to 2 hours after extravascular administration. When ibuprofen is administered immediately after a meal there is a slight reduction in the absorption rate but there is no change in the extent of the absorption.
[A39092]
When orally administered, the absorption of ibuprofen in adults is very rapidly done in the upper GI tract.
[A39190]
The average Cmax, Tmax and AUC ranges around 20 mcg/ml, 2 h and 70 mcg.h/ml. These parameters can vary depending on the enantiomer form, route, and dose of administration.
[A39190]
[A39092]
When orally administered, the absorption of ibuprofen in adults is very rapidly done in the upper GI tract.
[A39190]
The average Cmax, Tmax and AUC ranges around 20 mcg/ml, 2 h and 70 mcg.h/ml. These parameters can vary depending on the enantiomer form, route, and dose of administration.
[A39190]
Half-life
The serum half-life of ibuprofen is 1.2-2 hours.
[A39092]
In patients with a compromised liver function, the half-life can be prolonged to 3.1-3.4 hours.
[A39190]
[A39092]
In patients with a compromised liver function, the half-life can be prolonged to 3.1-3.4 hours.
[A39190]
Protein binding
Ibuprofen dosage is more than 99% bound to plasma proteins and site II of purified albumin, binding appears to be saturable and becomes non-linear at concentrations exceeding 20 mcg/ml.
[A39092]
[A39092]
Volume of distribution
The apparent volume of distribution of ibuprofen is of 0.1 L/kg.
[A39195]
[A39195]
Metabolism
Ibuprofen is rapidly metabolized and biotransformed in the liver to the formation of major metabolites which are the hydroxylated and carboxylated derivatives.
[A39092]
As soon as it is absorbed, the R-enantiomer undergoes extensive enantiomeric conversion (53-65%) to the more active S-enantiomer in vivo by the activity of alpha-methylacyl-CoA racemase.
[A39194]
Ibuprofen metabolism can be divided in phase I which is represented by the hydroxylation of the isobutyl chains for the formation of 2 or 3-hydroxy derivatives followed by oxidation to 2-carboxy-ibuprofen and p-carboxy-2-propionate. These oxidative reactions are performed by the activity of the cytochrome P450 isoforms CYP 2C9, CYP 2C19 and CYP 2C8. Therefore, these enzymes participate in the oxidation of the alkyl side chain to hydroxyl and carboxyl derivatives.
From this enzymes, the major catalyst in the formation of oxidative metabolites is the isoform CYP 2C9.
[A39190]
The metabolic phase I is followed by a phase II in which the oxidative metabolites may be conjugated to glucuronide prior to excretion. This activity forms phenolic and acyl glucuronides.
[A39190]
[A39092]
As soon as it is absorbed, the R-enantiomer undergoes extensive enantiomeric conversion (53-65%) to the more active S-enantiomer in vivo by the activity of alpha-methylacyl-CoA racemase.
[A39194]
Ibuprofen metabolism can be divided in phase I which is represented by the hydroxylation of the isobutyl chains for the formation of 2 or 3-hydroxy derivatives followed by oxidation to 2-carboxy-ibuprofen and p-carboxy-2-propionate. These oxidative reactions are performed by the activity of the cytochrome P450 isoforms CYP 2C9, CYP 2C19 and CYP 2C8. Therefore, these enzymes participate in the oxidation of the alkyl side chain to hydroxyl and carboxyl derivatives.
From this enzymes, the major catalyst in the formation of oxidative metabolites is the isoform CYP 2C9.
[A39190]
The metabolic phase I is followed by a phase II in which the oxidative metabolites may be conjugated to glucuronide prior to excretion. This activity forms phenolic and acyl glucuronides.
[A39190]
Route of elimination
Ibuprofen is rapidly metabolized and eliminated in the urine thus, this via accounts for more than 90% of the administered dose. It is completely eliminated in 24 hours after the last dose and almost all the administered dose goes through metabolism, representing about 99% of the eliminated dose.
[A39092]
The biliary excretion of unchanged drug and active phase II metabolites represents 1% of the administered dose.
[A39190]
In summary, ibuprofen is excreted as metabolites or their conjugates. The elimination of ibuprofen is not impaired by old age or the presence of renal impairment.
[A39092]
[A39092]
The biliary excretion of unchanged drug and active phase II metabolites represents 1% of the administered dose.
[A39190]
In summary, ibuprofen is excreted as metabolites or their conjugates. The elimination of ibuprofen is not impaired by old age or the presence of renal impairment.
[A39092]
Clearance
The clearance rate ranges between 3-13 L/h depending on the route of administration, enantiomer type and dosage.
[A39190]
[A39190]
Drug targets(13)
Proteins and enzymes this drug interacts with in the body
Prostaglandin G/H synthase 2
PTGS2
inhibitor
Specific functionenzyme binding
Cellular location
Microsome membrane
General function & pharmacology
Dual cyclooxygenase and peroxidase in the biosynthesis pathway of prostanoids, a class of C20 oxylipins mainly derived from arachidonate ((5Z,8Z,11Z,14Z)-eicosatetraenoate, AA, C20:4(n-6)), with a particular role in the inflammatory response .
PMID:11939906 PMID:16373578 PMID:19540099 PMID:22942274 PMID:26859324 PMID:27226593 PMID:7592599 PMID:7947975 PMID:9261177
The cyclooxygenase activity oxygenates AA to the hydroperoxy endoperoxide prostaglandin G2 (PGG2), and the peroxidase activity reduces PGG2 to the hydroxy endoperoxide prostaglandin H2 (PGH2), the precursor of all 2-series prostaglandins and thromboxanes .
PMID:16373578 PMID:22942274 PMID:26859324 PMID:27226593 PMID:7592599 PMID:7947975 PMID:9261177
This complex transformation is initiated by abstraction of hydrogen at carbon 13 (with S-stereochemistry), followed by insertion of molecular O2 to form the endoperoxide bridge between carbon 9 and 11 that defines prostaglandins. The insertion of a second molecule of O2 (bis-oxygenase activity) yields a hydroperoxy group in PGG2 that is then reduced to PGH2 by two electrons .
PMID:16373578 PMID:22942274 PMID:26859324 PMID:27226593 PMID:7592599 PMID:7947975 PMID:9261177
Similarly catalyzes successive cyclooxygenation and peroxidation of dihomo-gamma-linoleate (DGLA, C20:3(n-6)) and eicosapentaenoate (EPA, C20:5(n-3)) to corresponding PGH1 and PGH3, the precursors of 1- and 3-series prostaglandins .
PMID:11939906 PMID:19540099
In an alternative pathway of prostanoid biosynthesis, converts 2-arachidonoyl lysophopholipids to prostanoid lysophopholipids, which are then hydrolyzed by intracellular phospholipases to release free prostanoids .
PMID:27642067
Metabolizes 2-arachidonoyl glycerol yielding the glyceryl ester of PGH2, a process that can contribute to pain response .
PMID:22942274
Generates lipid mediators from n-3 and n-6 polyunsaturated fatty acids (PUFAs) via a lipoxygenase-type mechanism. Oxygenates PUFAs to hydroperoxy compounds and then reduces them to corresponding alcohols .
PMID:11034610 PMID:11192938 PMID:9048568 PMID:9261177
Plays a role in the generation of resolution phase interaction products (resolvins) during both sterile and infectious inflammation .
PMID:12391014
Metabolizes docosahexaenoate (DHA, C22:6(n-3)) to 17R-HDHA, a precursor of the D-series resolvins (RvDs) .
PMID:12391014
As a component of the biosynthetic pathway of E-series resolvins (RvEs), converts eicosapentaenoate (EPA, C20:5(n-3)) primarily to 18S-HEPE that is further metabolized by ALOX5 and LTA4H to generate 18S-RvE1 and 18S-RvE2 .
PMID:21206090
In vascular endothelial cells, converts docosapentaenoate (DPA, C22:5(n-3)) to 13R-HDPA, a precursor for 13-series resolvins (RvTs) shown to activate macrophage phagocytosis during bacterial infection .
PMID:26236990
In activated leukocytes, contributes to oxygenation of hydroxyeicosatetraenoates (HETE) to diHETES (5,15-diHETE and 5,11-diHETE) .
PMID:22068350 PMID:26282205
Can also use linoleate (LA, (9Z,12Z)-octadecadienoate, C18:2(n-6)) as substrate and produce hydroxyoctadecadienoates (HODEs) in a regio- and stereospecific manner, being (9R)-HODE ((9R)-hydroxy-(10E,12Z)-octadecadienoate) and (13S)-HODE ((13S)-hydroxy-(9Z,11E)-octadecadienoate) its major products (By similarity).
During neuroinflammation, plays a role in neuronal secretion of specialized preresolving mediators (SPMs) 15R-lipoxin A4 that regulates phagocytic microglia (By similarity)
PMID:11939906 PMID:16373578 PMID:19540099 PMID:22942274 PMID:26859324 PMID:27226593 PMID:7592599 PMID:7947975 PMID:9261177
The cyclooxygenase activity oxygenates AA to the hydroperoxy endoperoxide prostaglandin G2 (PGG2), and the peroxidase activity reduces PGG2 to the hydroxy endoperoxide prostaglandin H2 (PGH2), the precursor of all 2-series prostaglandins and thromboxanes .
PMID:16373578 PMID:22942274 PMID:26859324 PMID:27226593 PMID:7592599 PMID:7947975 PMID:9261177
This complex transformation is initiated by abstraction of hydrogen at carbon 13 (with S-stereochemistry), followed by insertion of molecular O2 to form the endoperoxide bridge between carbon 9 and 11 that defines prostaglandins. The insertion of a second molecule of O2 (bis-oxygenase activity) yields a hydroperoxy group in PGG2 that is then reduced to PGH2 by two electrons .
PMID:16373578 PMID:22942274 PMID:26859324 PMID:27226593 PMID:7592599 PMID:7947975 PMID:9261177
Similarly catalyzes successive cyclooxygenation and peroxidation of dihomo-gamma-linoleate (DGLA, C20:3(n-6)) and eicosapentaenoate (EPA, C20:5(n-3)) to corresponding PGH1 and PGH3, the precursors of 1- and 3-series prostaglandins .
PMID:11939906 PMID:19540099
In an alternative pathway of prostanoid biosynthesis, converts 2-arachidonoyl lysophopholipids to prostanoid lysophopholipids, which are then hydrolyzed by intracellular phospholipases to release free prostanoids .
PMID:27642067
Metabolizes 2-arachidonoyl glycerol yielding the glyceryl ester of PGH2, a process that can contribute to pain response .
PMID:22942274
Generates lipid mediators from n-3 and n-6 polyunsaturated fatty acids (PUFAs) via a lipoxygenase-type mechanism. Oxygenates PUFAs to hydroperoxy compounds and then reduces them to corresponding alcohols .
PMID:11034610 PMID:11192938 PMID:9048568 PMID:9261177
Plays a role in the generation of resolution phase interaction products (resolvins) during both sterile and infectious inflammation .
PMID:12391014
Metabolizes docosahexaenoate (DHA, C22:6(n-3)) to 17R-HDHA, a precursor of the D-series resolvins (RvDs) .
PMID:12391014
As a component of the biosynthetic pathway of E-series resolvins (RvEs), converts eicosapentaenoate (EPA, C20:5(n-3)) primarily to 18S-HEPE that is further metabolized by ALOX5 and LTA4H to generate 18S-RvE1 and 18S-RvE2 .
PMID:21206090
In vascular endothelial cells, converts docosapentaenoate (DPA, C22:5(n-3)) to 13R-HDPA, a precursor for 13-series resolvins (RvTs) shown to activate macrophage phagocytosis during bacterial infection .
PMID:26236990
In activated leukocytes, contributes to oxygenation of hydroxyeicosatetraenoates (HETE) to diHETES (5,15-diHETE and 5,11-diHETE) .
PMID:22068350 PMID:26282205
Can also use linoleate (LA, (9Z,12Z)-octadecadienoate, C18:2(n-6)) as substrate and produce hydroxyoctadecadienoates (HODEs) in a regio- and stereospecific manner, being (9R)-HODE ((9R)-hydroxy-(10E,12Z)-octadecadienoate) and (13S)-HODE ((13S)-hydroxy-(9Z,11E)-octadecadienoate) its major products (By similarity).
During neuroinflammation, plays a role in neuronal secretion of specialized preresolving mediators (SPMs) 15R-lipoxin A4 that regulates phagocytic microglia (By similarity)
Prostaglandin G/H synthase 1
PTGS1
inhibitor
Specific functionheme binding
Cellular location
Microsome membrane
General function & pharmacology
Dual cyclooxygenase and peroxidase that plays an important role in the biosynthesis pathway of prostanoids, a class of C20 oxylipins mainly derived from arachidonate ((5Z,8Z,11Z,14Z)-eicosatetraenoate, AA, C20:4(n-6)), with a particular role in the inflammatory response. The cyclooxygenase activity oxygenates AA to the hydroperoxy endoperoxide prostaglandin G2 (PGG2), and the peroxidase activity reduces PGG2 to the hydroxy endoperoxide prostaglandin H2 (PGH2), the precursor of all 2-series prostaglandins and thromboxanes. This complex transformation is initiated by abstraction of hydrogen at carbon 13 (with S-stereochemistry), followed by insertion of molecular O2 to form the endoperoxide bridge between carbon 9 and 11 that defines prostaglandins.
The insertion of a second molecule of O2 (bis-oxygenase activity) yields a hydroperoxy group in PGG2 that is then reduced to PGH2 by two electrons .
PMID:7947975
Involved in the constitutive production of prostanoids in particular in the stomach and platelets. In gastric epithelial cells, it is a key step in the generation of prostaglandins, such as prostaglandin E2 (PGE2), which plays an important role in cytoprotection. In platelets, it is involved in the generation of thromboxane A2 (TXA2), which promotes platelet activation and aggregation, vasoconstriction and proliferation of vascular smooth muscle cells (Probable).
Can also use linoleate (LA, (9Z,12Z)-octadecadienoate, C18:2(n-6)) as substrate and produce hydroxyoctadecadienoates (HODEs) in a regio- and stereospecific manner, being (9R)-HODE ((9R)-hydroxy-(10E,12Z)-octadecadienoate) and (13S)-HODE ((13S)-hydroxy-(9Z,11E)-octadecadienoate) its major products (By similarity)
The insertion of a second molecule of O2 (bis-oxygenase activity) yields a hydroperoxy group in PGG2 that is then reduced to PGH2 by two electrons .
PMID:7947975
Involved in the constitutive production of prostanoids in particular in the stomach and platelets. In gastric epithelial cells, it is a key step in the generation of prostaglandins, such as prostaglandin E2 (PGE2), which plays an important role in cytoprotection. In platelets, it is involved in the generation of thromboxane A2 (TXA2), which promotes platelet activation and aggregation, vasoconstriction and proliferation of vascular smooth muscle cells (Probable).
Can also use linoleate (LA, (9Z,12Z)-octadecadienoate, C18:2(n-6)) as substrate and produce hydroxyoctadecadienoates (HODEs) in a regio- and stereospecific manner, being (9R)-HODE ((9R)-hydroxy-(10E,12Z)-octadecadienoate) and (13S)-HODE ((13S)-hydroxy-(9Z,11E)-octadecadienoate) its major products (By similarity)
Interleukin-8
CXCL8
inhibitor
Specific functionchemokine activity
Cellular location
Secreted
General function & pharmacology
Chemotactic factor that mediates inflammatory response by attracting neutrophils, basophils, and T-cells to clear pathogens and protect the host from infection .
PMID:18692776 PMID:7636208
Also plays an important role in neutrophil activation .
PMID:2145175 PMID:9623510
Released in response to an inflammatory stimulus, exerts its effect by binding to the G-protein-coupled receptors CXCR1 and CXCR2, primarily found in neutrophils, monocytes and endothelial cells .
PMID:1840701 PMID:1891716
G-protein heterotrimer (alpha, beta, gamma subunits) constitutively binds to CXCR1/CXCR2 receptor and activation by IL8 leads to beta and gamma subunits release from Galpha (GNAI2 in neutrophils) and activation of several downstream signaling pathways including PI3K and MAPK pathways PMID:11971003 PMID:8662698
PMID:18692776 PMID:7636208
Also plays an important role in neutrophil activation .
PMID:2145175 PMID:9623510
Released in response to an inflammatory stimulus, exerts its effect by binding to the G-protein-coupled receptors CXCR1 and CXCR2, primarily found in neutrophils, monocytes and endothelial cells .
PMID:1840701 PMID:1891716
G-protein heterotrimer (alpha, beta, gamma subunits) constitutively binds to CXCR1/CXCR2 receptor and activation by IL8 leads to beta and gamma subunits release from Galpha (GNAI2 in neutrophils) and activation of several downstream signaling pathways including PI3K and MAPK pathways PMID:11971003 PMID:8662698
C-X-C chemokine receptor type 2
CXCR2
inhibitor
Specific functionC-C chemokine binding
Cellular location
Cell membrane
General function & pharmacology
Receptor for interleukin-8 which is a powerful neutrophil chemotactic factor .
PMID:1891716
Binding of IL-8 to the receptor causes activation of neutrophils. This response is mediated via a G-protein that activates a phosphatidylinositol-calcium second messenger system .
PMID:8662698
Binds to IL-8 with high affinity. Also binds with high affinity to CXCL3, GRO/MGSA and NAP-2
PMID:1891716
Binding of IL-8 to the receptor causes activation of neutrophils. This response is mediated via a G-protein that activates a phosphatidylinositol-calcium second messenger system .
PMID:8662698
Binds to IL-8 with high affinity. Also binds with high affinity to CXCL3, GRO/MGSA and NAP-2
C-X-C chemokine receptor type 1
CXCR1
inhibitor
Specific functionC-C chemokine binding
Cellular location
Cell membrane
General function & pharmacology
Receptor to interleukin-8, which is a powerful neutrophils chemotactic factor .
PMID:1840701
Binding of IL-8 to the receptor causes activation of neutrophils. This response is mediated via a G-protein that activates a phosphatidylinositol-calcium second messenger system PMID:8662698
PMID:1840701
Binding of IL-8 to the receptor causes activation of neutrophils. This response is mediated via a G-protein that activates a phosphatidylinositol-calcium second messenger system PMID:8662698
Metabolizing enzymes(9)
Enzymes involved in drug metabolism — important for understanding drug interactions
Enzyme activity key
substrate
inhibitor
inducer
CYP2C9Cytochrome P450 2C9
substrate
CYP2C8Cytochrome P450 2C8
substrate
CYP2C19Cytochrome P450 2C19
substrate
UGT1A3UDP-glucuronosyltransferase 1A3
substrate
UGT1A9UDP-glucuronosyltransferase 1A9
substrate
UGT2B4UDP-glucuronosyltransferase 2B4
substrate
UGT2B7UDP-glucuronosyltransferase 2B7
substrate
AMACRAlpha-methylacyl-CoA racemase
substrate
CYP3A4Cytochrome P450 3A4
substrate
Transporters(8)
Proteins that transport this drug across cell membranes
Solute carrier organic anion transporter family member 2B1
SLCO2B1
substrate
Specific functionbile acid transmembrane transporter activity
Cellular location
Cell membrane
General function & pharmacology
Mediates the Na(+)-independent transport of steroid sulfate conjugates and other specific organic anions .
PMID:10873595 PMID:11159893 PMID:11932330 PMID:12724351 PMID:14610227 PMID:16908597 PMID:18501590 PMID:20507927 PMID:22201122 PMID:23531488 PMID:25132355 PMID:26383540 PMID:27576593 PMID:28408210 PMID:29871943 PMID:34628357
Responsible for the transport of estrone 3-sulfate (E1S) through the basal membrane of syncytiotrophoblast, highlighting a potential role in the placental absorption of fetal-derived sulfated steroids including the steroid hormone precursor dehydroepiandrosterone sulfate (DHEA-S) .
PMID:11932330 PMID:12409283
Also facilitates the uptake of sulfated steroids at the basal/sinusoidal membrane of hepatocytes, therefore accounting for the major part of organic anions clearance of liver .
PMID:11159893
Mediates the intestinal uptake of sulfated steroids .
PMID:12724351 PMID:28408210
Mediates the uptake of the neurosteroids DHEA-S and pregnenolone sulfate (PregS) into the endothelial cells of the blood-brain barrier as the first step to enter the brain .
PMID:16908597 PMID:25132355
Also plays a role in the reuptake of neuropeptides such as substance P/TAC1 and vasoactive intestinal peptide/VIP released from retinal neurons .
PMID:25132355
May act as a heme transporter that promotes cellular iron availability via heme oxygenase/HMOX2 and independently of TFRC .
PMID:35714613
Also transports heme by-product coproporphyrin III (CPIII), and may be involved in their hepatic disposition .
PMID:26383540
Mediates the uptake of other substrates such as prostaglandins D2 (PGD2), E1 (PGE1) and E2 (PGE2), taurocholate, L-thyroxine, leukotriene C4 and thromboxane B2 (PubMed:10873595, PubMed:14610227, PubMed:19129463, PubMed:29871943, Ref.25). May contribute to regulate the transport of organic compounds in testis across the blood-testis-barrier (Probable). Shows a pH-sensitive substrate specificity which may be ascribed to the protonation state of the binding site and leads to a stimulation of substrate transport in an acidic microenvironment .
PMID:14610227 PMID:19129463 PMID:22201122
The exact transport mechanism has not been yet deciphered but most likely involves an anion exchange, coupling the cellular uptake of organic substrate with the efflux of an anionic compound .
PMID:19129463 PMID:20507927 PMID:26277985
Hydrogencarbonate/HCO3(-) acts as a probable counteranion that exchanges for organic anions .
PMID:19129463
Cytoplasmic glutamate may also act as counteranion in the placenta .
PMID:26277985
An inwardly directed proton gradient has also been proposed as the driving force of E1S uptake with a (H(+):E1S) stoichiometry of (1:1) PMID:20507927
PMID:10873595 PMID:11159893 PMID:11932330 PMID:12724351 PMID:14610227 PMID:16908597 PMID:18501590 PMID:20507927 PMID:22201122 PMID:23531488 PMID:25132355 PMID:26383540 PMID:27576593 PMID:28408210 PMID:29871943 PMID:34628357
Responsible for the transport of estrone 3-sulfate (E1S) through the basal membrane of syncytiotrophoblast, highlighting a potential role in the placental absorption of fetal-derived sulfated steroids including the steroid hormone precursor dehydroepiandrosterone sulfate (DHEA-S) .
PMID:11932330 PMID:12409283
Also facilitates the uptake of sulfated steroids at the basal/sinusoidal membrane of hepatocytes, therefore accounting for the major part of organic anions clearance of liver .
PMID:11159893
Mediates the intestinal uptake of sulfated steroids .
PMID:12724351 PMID:28408210
Mediates the uptake of the neurosteroids DHEA-S and pregnenolone sulfate (PregS) into the endothelial cells of the blood-brain barrier as the first step to enter the brain .
PMID:16908597 PMID:25132355
Also plays a role in the reuptake of neuropeptides such as substance P/TAC1 and vasoactive intestinal peptide/VIP released from retinal neurons .
PMID:25132355
May act as a heme transporter that promotes cellular iron availability via heme oxygenase/HMOX2 and independently of TFRC .
PMID:35714613
Also transports heme by-product coproporphyrin III (CPIII), and may be involved in their hepatic disposition .
PMID:26383540
Mediates the uptake of other substrates such as prostaglandins D2 (PGD2), E1 (PGE1) and E2 (PGE2), taurocholate, L-thyroxine, leukotriene C4 and thromboxane B2 (PubMed:10873595, PubMed:14610227, PubMed:19129463, PubMed:29871943, Ref.25). May contribute to regulate the transport of organic compounds in testis across the blood-testis-barrier (Probable). Shows a pH-sensitive substrate specificity which may be ascribed to the protonation state of the binding site and leads to a stimulation of substrate transport in an acidic microenvironment .
PMID:14610227 PMID:19129463 PMID:22201122
The exact transport mechanism has not been yet deciphered but most likely involves an anion exchange, coupling the cellular uptake of organic substrate with the efflux of an anionic compound .
PMID:19129463 PMID:20507927 PMID:26277985
Hydrogencarbonate/HCO3(-) acts as a probable counteranion that exchanges for organic anions .
PMID:19129463
Cytoplasmic glutamate may also act as counteranion in the placenta .
PMID:26277985
An inwardly directed proton gradient has also been proposed as the driving force of E1S uptake with a (H(+):E1S) stoichiometry of (1:1) PMID:20507927
ATP-dependent translocase ABCB1
ABCB1
substrate
Specific functionABC-type xenobiotic transporter activity
Cellular location
Cell membrane
General function & pharmacology
Translocates drugs and phospholipids across the membrane .
PMID:2897240 PMID:35970996 PMID:8898203 PMID:9038218 PMID:35507548
Catalyzes the flop of phospholipids from the cytoplasmic to the exoplasmic leaflet of the apical membrane. Participates mainly to the flop of phosphatidylcholine, phosphatidylethanolamine, beta-D-glucosylceramides and sphingomyelins .
PMID:8898203
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells PMID:2897240 PMID:35970996 PMID:9038218
PMID:2897240 PMID:35970996 PMID:8898203 PMID:9038218 PMID:35507548
Catalyzes the flop of phospholipids from the cytoplasmic to the exoplasmic leaflet of the apical membrane. Participates mainly to the flop of phosphatidylcholine, phosphatidylethanolamine, beta-D-glucosylceramides and sphingomyelins .
PMID:8898203
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells PMID:2897240 PMID:35970996 PMID:9038218
ATP-binding cassette sub-family C member 4
ABCC4
inhibitor
Specific function15-hydroxyprostaglandin dehydrogenase (NAD+) activity
Cellular location
Basolateral cell membrane
General function & pharmacology
ATP-dependent transporter of the ATP-binding cassette (ABC) family that actively extrudes physiological compounds and xenobiotics from cells. Transports a range of endogenous molecules that have a key role in cellular communication and signaling, including cyclic nucleotides such as cyclic AMP (cAMP) and cyclic GMP (cGMP), bile acids, steroid conjugates, urate, and prostaglandins .
PMID:11856762 PMID:12523936 PMID:12835412 PMID:12883481 PMID:15364914 PMID:15454390 PMID:16282361 PMID:17959747 PMID:18300232 PMID:26721430
Mediates the ATP-dependent efflux of glutathione conjugates such as leukotriene C4 (LTC4) and leukotriene B4 (LTB4) too. The presence of GSH is necessary for the ATP-dependent transport of LTB4, whereas GSH is not required for the transport of LTC4 .
PMID:17959747
Mediates the cotransport of bile acids with reduced glutathione (GSH) .
PMID:12523936 PMID:12883481 PMID:16282361
Transports a wide range of drugs and their metabolites, including anticancer, antiviral and antibiotics molecules .
PMID:11856762 PMID:12105214 PMID:15454390 PMID:17344354 PMID:18300232
Confers resistance to anticancer agents such as methotrexate PMID:11106685
PMID:11856762 PMID:12523936 PMID:12835412 PMID:12883481 PMID:15364914 PMID:15454390 PMID:16282361 PMID:17959747 PMID:18300232 PMID:26721430
Mediates the ATP-dependent efflux of glutathione conjugates such as leukotriene C4 (LTC4) and leukotriene B4 (LTB4) too. The presence of GSH is necessary for the ATP-dependent transport of LTB4, whereas GSH is not required for the transport of LTC4 .
PMID:17959747
Mediates the cotransport of bile acids with reduced glutathione (GSH) .
PMID:12523936 PMID:12883481 PMID:16282361
Transports a wide range of drugs and their metabolites, including anticancer, antiviral and antibiotics molecules .
PMID:11856762 PMID:12105214 PMID:15454390 PMID:17344354 PMID:18300232
Confers resistance to anticancer agents such as methotrexate PMID:11106685
Multidrug resistance-associated protein 1
ABCC1
inhibitor
Specific functionABC-type glutathione S-conjugate transporter activity
Cellular location
Cell membrane
General function & pharmacology
Mediates export of organic anions and drugs from the cytoplasm .
PMID:10064732 PMID:11114332 PMID:16230346 PMID:7961706 PMID:9281595
Mediates ATP-dependent transport of glutathione and glutathione conjugates, leukotriene C4, estradiol-17-beta-o-glucuronide, methotrexate, antiviral drugs and other xenobiotics .
PMID:10064732 PMID:11114332 PMID:16230346 PMID:7961706 PMID:9281595
Confers resistance to anticancer drugs by decreasing accumulation of drug in cells, and by mediating ATP- and GSH-dependent drug export .
PMID:9281595
Hydrolyzes ATP with low efficiency .
PMID:16230346
Catalyzes the export of sphingosine 1-phosphate from mast cells independently of their degranulation .
PMID:17050692
Participates in inflammatory response by allowing export of leukotriene C4 from leukotriene C4-synthesizing cells (By similarity). Mediates ATP-dependent, GSH-independent cyclic GMP-AMP (cGAMP) export .
PMID:36070769
Thus, by limiting intracellular cGAMP concentrations negatively regulates the cGAS-STING pathway .
PMID:36070769
Exports S-geranylgeranyl-glutathione (GGG) in lymphoid cells and stromal compartments of lymphoid organs. ABCC1 (via extracellular transport) with GGT5 (via GGG catabolism) establish GGG gradients within lymphoid tissues to position P2RY8-positive lymphocytes at germinal centers in lymphoid follicles and restrict their chemotactic transmigration from blood vessels to the bone marrow parenchyma (By similarity).
Mediates basolateral export of GSH-conjugated R- and S-prostaglandin A2 diastereomers in polarized epithelial cells PMID:9426231
PMID:10064732 PMID:11114332 PMID:16230346 PMID:7961706 PMID:9281595
Mediates ATP-dependent transport of glutathione and glutathione conjugates, leukotriene C4, estradiol-17-beta-o-glucuronide, methotrexate, antiviral drugs and other xenobiotics .
PMID:10064732 PMID:11114332 PMID:16230346 PMID:7961706 PMID:9281595
Confers resistance to anticancer drugs by decreasing accumulation of drug in cells, and by mediating ATP- and GSH-dependent drug export .
PMID:9281595
Hydrolyzes ATP with low efficiency .
PMID:16230346
Catalyzes the export of sphingosine 1-phosphate from mast cells independently of their degranulation .
PMID:17050692
Participates in inflammatory response by allowing export of leukotriene C4 from leukotriene C4-synthesizing cells (By similarity). Mediates ATP-dependent, GSH-independent cyclic GMP-AMP (cGAMP) export .
PMID:36070769
Thus, by limiting intracellular cGAMP concentrations negatively regulates the cGAS-STING pathway .
PMID:36070769
Exports S-geranylgeranyl-glutathione (GGG) in lymphoid cells and stromal compartments of lymphoid organs. ABCC1 (via extracellular transport) with GGT5 (via GGG catabolism) establish GGG gradients within lymphoid tissues to position P2RY8-positive lymphocytes at germinal centers in lymphoid follicles and restrict their chemotactic transmigration from blood vessels to the bone marrow parenchyma (By similarity).
Mediates basolateral export of GSH-conjugated R- and S-prostaglandin A2 diastereomers in polarized epithelial cells PMID:9426231
Solute carrier organic anion transporter family member 1A2
SLCO1A2
inhibitor
Specific functionbile acid transmembrane transporter activity
Cellular location
Cell membrane
General function & pharmacology
Na(+)-independent transporter that mediates the cellular uptake of a broad range of organic anions such as the endogenous bile salts cholate and deoxycholate, either in their unconjugated or conjugated forms (taurocholate and glycocholate), at the plasmam membrane .
PMID:19129463 PMID:7557095
Responsible for intestinal absorption of bile acids (By similarity). Transports dehydroepiandrosterone 3-sulfate (DHEAS), a major circulating steroid secreted by the adrenal cortex, as well as estrone 3-sulfate and 17beta-estradiol 17-O-(beta-D-glucuronate) .
PMID:11159893 PMID:12568656 PMID:19129463 PMID:23918469 PMID:25560245 PMID:9539145
Mediates apical uptake of all-trans-retinol (atROL) across human retinal pigment epithelium, which is essential to maintaining the integrity of the visual cycle and thus vision .
PMID:25560245
Involved in the uptake of clinically used drugs .
PMID:17301733 PMID:20686826 PMID:27777271
Capable of thyroid hormone transport (both T3 or 3,3',5'-triiodo-L-thyronine, and T4 or L-tyroxine) .
PMID:19129463 PMID:20358049
Also transports prostaglandin E2 .
PMID:19129463
Plays roles in blood-brain and -cerebrospinal fluid barrier transport of organic anions and signal mediators, and in hormone uptake by neural cells (By similarity). May also play a role in the reuptake of neuropeptides such as substance P/TAC1 and vasoactive intestinal peptide/VIP released from retinal neurons .
PMID:25132355
May play an important role in plasma and tissue distribution of the structurally diverse chemotherapeutic drugs methotrexate and paclitaxel .
PMID:23243220
Shows a pH-sensitive substrate specificity which may be ascribed to the protonation state of the binding site and leads to a stimulation of substrate transport in an acidic microenvironment .
PMID:19129463
Hydrogencarbonate/HCO3(-) acts as the probable counteranion that exchanges for organic anions .
PMID:19129463
May contribute to regulate the transport of organic compounds in testis across the blood-testis-barrier (Probable)
PMID:19129463 PMID:7557095
Responsible for intestinal absorption of bile acids (By similarity). Transports dehydroepiandrosterone 3-sulfate (DHEAS), a major circulating steroid secreted by the adrenal cortex, as well as estrone 3-sulfate and 17beta-estradiol 17-O-(beta-D-glucuronate) .
PMID:11159893 PMID:12568656 PMID:19129463 PMID:23918469 PMID:25560245 PMID:9539145
Mediates apical uptake of all-trans-retinol (atROL) across human retinal pigment epithelium, which is essential to maintaining the integrity of the visual cycle and thus vision .
PMID:25560245
Involved in the uptake of clinically used drugs .
PMID:17301733 PMID:20686826 PMID:27777271
Capable of thyroid hormone transport (both T3 or 3,3',5'-triiodo-L-thyronine, and T4 or L-tyroxine) .
PMID:19129463 PMID:20358049
Also transports prostaglandin E2 .
PMID:19129463
Plays roles in blood-brain and -cerebrospinal fluid barrier transport of organic anions and signal mediators, and in hormone uptake by neural cells (By similarity). May also play a role in the reuptake of neuropeptides such as substance P/TAC1 and vasoactive intestinal peptide/VIP released from retinal neurons .
PMID:25132355
May play an important role in plasma and tissue distribution of the structurally diverse chemotherapeutic drugs methotrexate and paclitaxel .
PMID:23243220
Shows a pH-sensitive substrate specificity which may be ascribed to the protonation state of the binding site and leads to a stimulation of substrate transport in an acidic microenvironment .
PMID:19129463
Hydrogencarbonate/HCO3(-) acts as the probable counteranion that exchanges for organic anions .
PMID:19129463
May contribute to regulate the transport of organic compounds in testis across the blood-testis-barrier (Probable)
Solute carrier family 22 member 6
SLC22A6
inhibitor
Specific functionalpha-ketoglutarate transmembrane transporter activity
Cellular location
Basolateral cell membrane
General function & pharmacology
Secondary active transporter that functions as a Na(+)-independent organic anion (OA)/dicarboxylate antiporter where the uptake of one molecule of OA into the cell is coupled with an efflux of one molecule of intracellular dicarboxylate such as 2-oxoglutarate or glutarate .
PMID:11669456 PMID:11907186 PMID:14675047 PMID:22108572 PMID:23832370 PMID:28534121 PMID:9950961
Mediates the uptake of OA across the basolateral side of proximal tubule epithelial cells, thereby contributing to the renal elimination of endogenous OA from the systemic circulation into the urine .
PMID:9887087
Functions as a biopterin transporters involved in the uptake and the secretion of coenzymes tetrahydrobiopterin (BH4), dihydrobiopterin (BH2) and sepiapterin to urine, thereby determining baseline levels of blood biopterins .
PMID:28534121
Transports prostaglandin E2 (PGE2) and prostaglandin F2-alpha (PGF2-alpha) and may contribute to their renal excretion .
PMID:11907186
Also mediates the uptake of cyclic nucleotides such as cAMP and cGMP .
PMID:26377792
Involved in the transport of neuroactive tryptophan metabolites kynurenate (KYNA) and xanthurenate (XA) and may contribute to their secretion from the brain .
PMID:22108572 PMID:23832370
May transport glutamate .
PMID:26377792
Also involved in the disposition of uremic toxins and potentially toxic xenobiotics by the renal organic anion secretory pathway, helping reduce their undesired toxicological effects on the body .
PMID:11669456 PMID:14675047
Uremic toxins include the indoxyl sulfate (IS), hippurate/N-benzoylglycine (HA), indole acetate (IA), 3-carboxy-4- methyl-5-propyl-2-furanpropionate (CMPF) and urate .
PMID:14675047 PMID:26377792
Xenobiotics include the mycotoxin ochratoxin (OTA) .
PMID:11669456
May also contribute to the transport of organic compounds in testes across the blood-testis-barrier PMID:35307651
PMID:11669456 PMID:11907186 PMID:14675047 PMID:22108572 PMID:23832370 PMID:28534121 PMID:9950961
Mediates the uptake of OA across the basolateral side of proximal tubule epithelial cells, thereby contributing to the renal elimination of endogenous OA from the systemic circulation into the urine .
PMID:9887087
Functions as a biopterin transporters involved in the uptake and the secretion of coenzymes tetrahydrobiopterin (BH4), dihydrobiopterin (BH2) and sepiapterin to urine, thereby determining baseline levels of blood biopterins .
PMID:28534121
Transports prostaglandin E2 (PGE2) and prostaglandin F2-alpha (PGF2-alpha) and may contribute to their renal excretion .
PMID:11907186
Also mediates the uptake of cyclic nucleotides such as cAMP and cGMP .
PMID:26377792
Involved in the transport of neuroactive tryptophan metabolites kynurenate (KYNA) and xanthurenate (XA) and may contribute to their secretion from the brain .
PMID:22108572 PMID:23832370
May transport glutamate .
PMID:26377792
Also involved in the disposition of uremic toxins and potentially toxic xenobiotics by the renal organic anion secretory pathway, helping reduce their undesired toxicological effects on the body .
PMID:11669456 PMID:14675047
Uremic toxins include the indoxyl sulfate (IS), hippurate/N-benzoylglycine (HA), indole acetate (IA), 3-carboxy-4- methyl-5-propyl-2-furanpropionate (CMPF) and urate .
PMID:14675047 PMID:26377792
Xenobiotics include the mycotoxin ochratoxin (OTA) .
PMID:11669456
May also contribute to the transport of organic compounds in testes across the blood-testis-barrier PMID:35307651
Organic anion transporter 3
SLC22A8
inhibitor
Specific functionorganic anion transmembrane transporter activity
Cellular location
Basolateral cell membrane
General function & pharmacology
Functions as an organic anion/dicarboxylate exchanger that couples organic anion uptake indirectly to the sodium gradient .
PMID:14586168 PMID:15644426 PMID:15846473 PMID:16455804 PMID:31553721
Transports organic anions such as estrone 3-sulfate (E1S) and urate in exchange for dicarboxylates such as glutarate or ketoglutarate (2-oxoglutarate) .
PMID:14586168 PMID:15846473 PMID:15864504 PMID:22108572 PMID:23832370
Plays an important role in the excretion of endogenous and exogenous organic anions, especially from the kidney and the brain .
PMID:11306713 PMID:14586168 PMID:15846473
E1S transport is pH- and chloride-dependent and may also involve E1S/cGMP exchange .
PMID:26377792
Responsible for the transport of prostaglandin E2 (PGE2) and prostaglandin F2(alpha) (PGF2(alpha)) in the basolateral side of the renal tubule .
PMID:11907186
Involved in the transport of neuroactive tryptophan metabolites kynurenate and xanthurenate .
PMID:22108572 PMID:23832370
Functions as a biopterin transporters involved in the uptake and the secretion of coenzymes tetrahydrobiopterin (BH4), dihydrobiopterin (BH2) and sepiapterin to urine, thereby determining baseline levels of blood biopterins .
PMID:28534121
May be involved in the basolateral transport of steviol, a metabolite of the popular sugar substitute stevioside .
PMID:15644426
May participate in the detoxification/ renal excretion of drugs and xenobiotics, such as the histamine H(2)-receptor antagonists fexofenadine and cimetidine, the antibiotic benzylpenicillin (PCG), the anionic herbicide 2,4-dichloro-phenoxyacetate (2,4-D), the diagnostic agent p-aminohippurate (PAH), the antiviral acyclovir (ACV), and the mycotoxin ochratoxin (OTA), by transporting these exogenous organic anions across the cell membrane in exchange for dicarboxylates such as 2-oxoglutarate .
PMID:11669456 PMID:15846473 PMID:16455804
Contributes to the renal uptake of potent uremic toxins (indoxyl sulfate (IS), indole acetate (IA), hippurate/N-benzoylglycine (HA) and 3-carboxy-4-methyl-5-propyl-2-furanpropionate (CMPF)), pravastatin, PCG, E1S and dehydroepiandrosterone sulfate (DHEAS), and is partly involved in the renal uptake of temocaprilat (an angiotensin-converting enzyme (ACE) inhibitor) .
PMID:14675047
May contribute to the release of cortisol in the adrenals .
PMID:15864504
Involved in one of the detoxification systems on the choroid plexus (CP), removes substrates such as E1S or taurocholate (TC), PCG, 2,4-D and PAH, from the cerebrospinal fluid (CSF) to the blood for eventual excretion in urine and bile (By similarity). Also contributes to the uptake of several other organic compounds such as the prostanoids prostaglandin E(2) and prostaglandin F(2-alpha), L-carnitine, and the therapeutic drugs allopurinol, 6-mercaptopurine (6-MP) and 5-fluorouracil (5-FU) (By similarity). Mediates the transport of PAH, PCG, and the statins pravastatin and pitavastatin, from the cerebrum into the blood circulation across the blood-brain barrier (BBB).
In summary, plays a role in the efflux of drugs and xenobiotics, helping reduce their undesired toxicological effects on the body (By similarity)
PMID:14586168 PMID:15644426 PMID:15846473 PMID:16455804 PMID:31553721
Transports organic anions such as estrone 3-sulfate (E1S) and urate in exchange for dicarboxylates such as glutarate or ketoglutarate (2-oxoglutarate) .
PMID:14586168 PMID:15846473 PMID:15864504 PMID:22108572 PMID:23832370
Plays an important role in the excretion of endogenous and exogenous organic anions, especially from the kidney and the brain .
PMID:11306713 PMID:14586168 PMID:15846473
E1S transport is pH- and chloride-dependent and may also involve E1S/cGMP exchange .
PMID:26377792
Responsible for the transport of prostaglandin E2 (PGE2) and prostaglandin F2(alpha) (PGF2(alpha)) in the basolateral side of the renal tubule .
PMID:11907186
Involved in the transport of neuroactive tryptophan metabolites kynurenate and xanthurenate .
PMID:22108572 PMID:23832370
Functions as a biopterin transporters involved in the uptake and the secretion of coenzymes tetrahydrobiopterin (BH4), dihydrobiopterin (BH2) and sepiapterin to urine, thereby determining baseline levels of blood biopterins .
PMID:28534121
May be involved in the basolateral transport of steviol, a metabolite of the popular sugar substitute stevioside .
PMID:15644426
May participate in the detoxification/ renal excretion of drugs and xenobiotics, such as the histamine H(2)-receptor antagonists fexofenadine and cimetidine, the antibiotic benzylpenicillin (PCG), the anionic herbicide 2,4-dichloro-phenoxyacetate (2,4-D), the diagnostic agent p-aminohippurate (PAH), the antiviral acyclovir (ACV), and the mycotoxin ochratoxin (OTA), by transporting these exogenous organic anions across the cell membrane in exchange for dicarboxylates such as 2-oxoglutarate .
PMID:11669456 PMID:15846473 PMID:16455804
Contributes to the renal uptake of potent uremic toxins (indoxyl sulfate (IS), indole acetate (IA), hippurate/N-benzoylglycine (HA) and 3-carboxy-4-methyl-5-propyl-2-furanpropionate (CMPF)), pravastatin, PCG, E1S and dehydroepiandrosterone sulfate (DHEAS), and is partly involved in the renal uptake of temocaprilat (an angiotensin-converting enzyme (ACE) inhibitor) .
PMID:14675047
May contribute to the release of cortisol in the adrenals .
PMID:15864504
Involved in one of the detoxification systems on the choroid plexus (CP), removes substrates such as E1S or taurocholate (TC), PCG, 2,4-D and PAH, from the cerebrospinal fluid (CSF) to the blood for eventual excretion in urine and bile (By similarity). Also contributes to the uptake of several other organic compounds such as the prostanoids prostaglandin E(2) and prostaglandin F(2-alpha), L-carnitine, and the therapeutic drugs allopurinol, 6-mercaptopurine (6-MP) and 5-fluorouracil (5-FU) (By similarity). Mediates the transport of PAH, PCG, and the statins pravastatin and pitavastatin, from the cerebrum into the blood circulation across the blood-brain barrier (BBB).
In summary, plays a role in the efflux of drugs and xenobiotics, helping reduce their undesired toxicological effects on the body (By similarity)
Solute carrier family 22 member 11
SLC22A11
inhibitor
Specific functionorganic anion transmembrane transporter activity
Cellular location
Cell membrane
General function & pharmacology
Antiporter that mediates the transport of conjugated steroids and other specific organic anions at the basal membrane of syncytiotrophoblast and at the apical membrane of proximal tubule epithelial cells, in exchange for anionic compounds .
PMID:10660625 PMID:11907186 PMID:15037815 PMID:15102942 PMID:15291761 PMID:15576633 PMID:17229912 PMID:18501590 PMID:26277985 PMID:28027879
May be responsible for placental absorption of fetal-derived steroid sulfates such as estrone sulfate (E1S) and the steroid hormone precursor dehydroepiandrosterone sulfate (DHEA-S), as well as clearing waste products and xenobiotics from the fetus .
PMID:12409283
Maybe also be involved in placental urate homeostasis .
PMID:17229912
Facilitates the renal reabsorption of organic anions such as urate and derived steroid sulfates .
PMID:15037815 PMID:17229912
Organic anion glutarate acts as conteranion for E1S renal uptake .
PMID:15037815 PMID:17229912
Possible transport mode may also include DHEA-S/E1S exchange .
PMID:28027879
Also interacts with inorganic anions such as chloride and hydroxyl ions, therefore possible transport modes may include E1S/Cl(-), E1S/OH(-), urate/Cl(-) and urate/OH(-) .
PMID:17229912
Also mediates the transport of prostaglandin E2 (PGE2) and prostaglandin F2-alpha (PGF2-alpha) and may be involved in their renal excretion .
PMID:11907186
Also able to uptake anionic drugs, diuretics, bile salts and ochratoxin A .
PMID:10660625 PMID:26277985
Mediates the unidirectional efflux of glutamate and aspartate .
PMID:28027879
Glutamate efflux down its transmembrane gradient may drive SLC22A11/OAT4-mediated placental uptake of E1S PMID:26277985
PMID:10660625 PMID:11907186 PMID:15037815 PMID:15102942 PMID:15291761 PMID:15576633 PMID:17229912 PMID:18501590 PMID:26277985 PMID:28027879
May be responsible for placental absorption of fetal-derived steroid sulfates such as estrone sulfate (E1S) and the steroid hormone precursor dehydroepiandrosterone sulfate (DHEA-S), as well as clearing waste products and xenobiotics from the fetus .
PMID:12409283
Maybe also be involved in placental urate homeostasis .
PMID:17229912
Facilitates the renal reabsorption of organic anions such as urate and derived steroid sulfates .
PMID:15037815 PMID:17229912
Organic anion glutarate acts as conteranion for E1S renal uptake .
PMID:15037815 PMID:17229912
Possible transport mode may also include DHEA-S/E1S exchange .
PMID:28027879
Also interacts with inorganic anions such as chloride and hydroxyl ions, therefore possible transport modes may include E1S/Cl(-), E1S/OH(-), urate/Cl(-) and urate/OH(-) .
PMID:17229912
Also mediates the transport of prostaglandin E2 (PGE2) and prostaglandin F2-alpha (PGF2-alpha) and may be involved in their renal excretion .
PMID:11907186
Also able to uptake anionic drugs, diuretics, bile salts and ochratoxin A .
PMID:10660625 PMID:26277985
Mediates the unidirectional efflux of glutamate and aspartate .
PMID:28027879
Glutamate efflux down its transmembrane gradient may drive SLC22A11/OAT4-mediated placental uptake of E1S PMID:26277985
Carriers(1)
Proteins that carry this drug through the body
Albumin
ALB
binder
Specific functionantioxidant activity
Cellular location
Secreted
General function & pharmacology
Binds water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs (Probable). Its main function is the regulation of the colloidal osmotic pressure of blood (Probable). Major zinc transporter in plasma, typically binds about 80% of all plasma zinc .
PMID:19021548
Major calcium and magnesium transporter in plasma, binds approximately 45% of circulating calcium and magnesium in plasma (By similarity).
Potentially has more than two calcium-binding sites and might additionally bind calcium in a non-specific manner (By similarity). The shared binding site between zinc and calcium at residue Asp-273 suggests a crosstalk between zinc and calcium transport in the blood (By similarity). The rank order of affinity is zinc > calcium > magnesium (By similarity).
Binds to the bacterial siderophore enterobactin and inhibits enterobactin-mediated iron uptake of E.coli from ferric transferrin, and may thereby limit the utilization of iron and growth of enteric bacteria such as E.coli .
PMID:6234017
Does not prevent iron uptake by the bacterial siderophore aerobactin PMID:6234017
PMID:19021548
Major calcium and magnesium transporter in plasma, binds approximately 45% of circulating calcium and magnesium in plasma (By similarity).
Potentially has more than two calcium-binding sites and might additionally bind calcium in a non-specific manner (By similarity). The shared binding site between zinc and calcium at residue Asp-273 suggests a crosstalk between zinc and calcium transport in the blood (By similarity). The rank order of affinity is zinc > calcium > magnesium (By similarity).
Binds to the bacterial siderophore enterobactin and inhibits enterobactin-mediated iron uptake of E.coli from ferric transferrin, and may thereby limit the utilization of iron and growth of enteric bacteria such as E.coli .
PMID:6234017
Does not prevent iron uptake by the bacterial siderophore aerobactin PMID:6234017
Biological pathways(2)
Scientific references(26)
Zawada ET Jr
Renal consequences of nonsteroidal antiinflammatory drugs.
Postgraduate Medicine
198271(5):223-230. doi: 10.1080/00325481.1982.11716077
Townsend K.P., Pratico D.
Novel therapeutic opportunities for Alzheimer's disease: focus on nonsteroidal anti‐inflammatory drugs.
The FASEB Journal
200519(12):1592-1601. doi: 10.1096/fj.04-3620rev
Chen H., Jacobs E., Schwarzschild M.A., McCullough M.L., Calle E.E., Thun M.J., Ascherio A.
Nonsteroidal antiinflammatory drug use and the risk for Parkinson's disease.
Annals of Neurology
200558(6):963-967. doi: 10.1002/ana.20682
Geisslinger G., Dietzel K., Bezler H., Nuernberg B., Brune K.
Pharmacological differences between R(−)-and S(+)-ibuprofen.
Agents and Actions
198927(3-4):455-457. doi: 10.1007/bf01972851
Bergner T., Przybilla B.
Photosensitization caused by ibuprofen.
Journal of the American Academy of Dermatology
199226(1):114-116. doi: 10.1016/0190-9622(92)70018-b
Dill J., Patel A.R., Yang X.L., Bachoo R., Powell C.M., Li S.
A molecular mechanism for ibuprofen-mediated RhoA inhibition in neurons.
Journal Neurosci
2010 Jan 2030(3):963-72. doi: 10.1523/JNEUROSCI.5045-09.2010
Adams S.S.
The Propionic Acids: A Personal Perspective.
The Journal of Clinical Pharmacology
199232(4):317-323. doi: 10.1002/j.1552-4604.1992.tb03842.x
Rainsford K.D.
Safety and Efficacy of Non‐prescription, Over‐the‐Counter (OTC) Ibuprofen. Ibuprofen. 2015;:313-345. doi: 10.
1002/9781118743614
ch7
Halford G.M., Lordkipanidze M., Watson S.P.
50th anniversary of the discovery of ibuprofen: an interview with Dr Stewart Adams.
Platelets
201223(6):415-22. doi: 10.3109/09537104.2011.632032. Epub 2011 Nov 18
Bushra R., Aslam N.
An overview of clinical pharmacology of Ibuprofen.
Oman Medicine Journal
2010 Jul25(3):155-1661. doi: 10.5001/omj.2010.49
Adams S.S., McCullough K.F., Nicholson J.S.
Anti-inflammatory, analgesic, antipyretic and related properties of meloxicam, a new non-steroidal anti-inflammatory agent with favourable gastrointestinal tolerance.
Inflammation Research
199544(10):423-433. doi: 10.1007/bf01757699
Potthast H., Dressman J.B., Junginger H.E., Midha K.K., Oeser H., Shah V.P., Vogelpoel H., Barends D.M.
Biowaiver monographs for immediate release solid oral dosage forms: ibuprofen.
Journal of Pharmaceutical Sciences
2005 Oct94(10):2121-31. doi: 10.1002/jps.20444
Sharma P.K., Garg S.K., Narang A.
Pharmacokinetics of Oral Ibuprofen in Premature Infants.
The Journal of Clinical Pharmacology
200343(9):968-973. doi: 10.1177/0091270003254635
Tan S.C., Patel B.K., Jackson S.H., Swift C.G., Hutt A.J.
Enantiospecific analysis of ibuprofen by high performance liquid chromatography: Determination of free and total drug enantiomer concentrations in serum and urine.
Chromatographia
199746(1-2):23-32. doi: 10.1007/bf02490926
Konstan M.W., Krenicky J.E., Finney M.R., Kirchner H.L., Hilliard K.A., Hilliard J.B., Davis P.B., Hoppel C.L.
Effect of ibuprofen on neutrophil migration in vivo in cystic fibrosis and healthy subjects.
Journal of Pharmacology and Experimental Therapeutics
2003 Sep306(3):1086-91. doi: 10.1124/jpet.103.052449. Epub 2003 Jun 13
Moore P.A., Hersh E.V.
Celecoxib and rofecoxib.
The Journal of the American Dental Association
2001132(4):451-456. doi: 10.14219/jada.archive.2001.0207
Dawood M.Y.
Primary dysmenorrhea: advances in pathogenesis and management.
Obstetrics Gynecology
2006 Aug108(2):428-41. doi: 10.1097/01.AOG.0000230214.26638.0c
Krishna S., Pukrittayakamee S., Supanaranond W., ter Kuile F., Ruprah M., Sura T., White N.J.
Fever in uncomplicated Plasmodium falciparum malaria: randomized double-‘blind’ comparison of ibuprofen and paracetamol treatment.
Transactions of the Royal Society of Tropical Medicine and Hygiene
199589(5):507-509. doi: 10.1016/0035-9203(95)90087-x
Evers S., Rahmann A., Kraemer C., Kurlemann G., Debus O., Husstedt I.W., Frese A.
Treatment of childhood migraine attacks with oral zolmitriptan and ibuprofen.
Neurology
2006 Aug 867(3):497-9. doi: 10.1212/01.wnl.0000231138.18629.d5. Epub 2006 Jun 14
Casper D., Yaparpalvi U., Rempel N., Werner P.
Ibuprofen protects dopaminergic neurons against glutamate toxicity in vitro.
Neuroscience Letters
2000289(3):201-204. doi: 10.1016/s0304-3940(00)01294-5
ATC classification(9 codes)
ATC C01EB16
ATC R02AX02
ATC N02AJ19
ATC M01AE51
ATC G02CC01
ATC M01AE01
ATC M02AA13
ATC N02AJ08
ATC N02AJ23
Affected organisms(1)
Humans and other mammals
International brands(89)
Salt forms(5)
Ibuprofen aluminum(DBSALT002285)
Ibuprofen arginine(DBSALT003107)
Ibuprofen lysine(DBSALT001397)
Ibuprofen potassium(DBSALT002284)
Ibuprofen sodium(DBSALT001483)
Experimental properties(7)
Commercial products(3143)
Chemical identifiers
CAS, UNII, InChI Key and database cross-references
Show
Chemical identifiers
CAS, UNII, InChI Key and database cross-references
Linked compound data from DrugBank Open Data (CC BY-NC 4.0)
Ibuprofen
Additional database identifiers
Drugs Product Database (DPD)
2609
ChemSpider
3544
BindingDB
50009859
Guide to Pharmacology
2713
HUGO Gene Nomenclature Committee (HGNC)
HGNC:9605
GenAtlas
PTGS2
GeneCards
PTGS2
GenBank Gene Database
L15326
GenBank Protein Database
291988
Guide to Pharmacology
1376
UniProt Accession
PGH2_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:9604
GenAtlas
PTGS1
GeneCards
PTGS1
GenBank Gene Database
M31822
GenBank Protein Database
387018
Guide to Pharmacology
1375
UniProt Accession
PGH1_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:6025
GenAtlas
IL8
GeneCards
CXCL8
GenBank Gene Database
Y00787
GenBank Protein Database
34519
UniProt Accession
IL8_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:6027
GeneCards
CXCR2
Guide to Pharmacology
69
UniProt Accession
CXCR2_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:6026
GeneCards
CXCR1
GenBank Gene Database
L19591
GenBank Protein Database
559050
Guide to Pharmacology
68
UniProt Accession
CXCR1_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:990
GenAtlas
BCL2
GeneCards
BCL2
GenBank Gene Database
M13994
GenBank Protein Database
179367
Guide to Pharmacology
2844
UniProt Accession
BCL2_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:11784
GenAtlas
THBD
GeneCards
THBD
GenBank Gene Database
X05495
GenBank Protein Database
736251
UniProt Accession
TRBM_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:3556
GeneCards
FABP2
GenBank Gene Database
BC069466
GenBank Protein Database
46854681
UniProt Accession
FABPI_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:9236
GenAtlas
PPARG
GeneCards
PPARG
GenBank Gene Database
U79012
GenBank Protein Database
1711117
Guide to Pharmacology
595
UniProt Accession
PPARG_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:1884
GenAtlas
CFTR
GeneCards
CFTR
GenBank Gene Database
M28668
GenBank Protein Database
180332
Guide to Pharmacology
707
UniProt Accession
CFTR_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:9232
GenAtlas
PPARA
GeneCards
PPARA
GenBank Gene Database
L02932
GenBank Protein Database
307341
Guide to Pharmacology
593
UniProt Accession
PPARA_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:4439
GenAtlas
GP1BA
GeneCards
GP1BA
GenBank Gene Database
J02940
GenBank Protein Database
306793
UniProt Accession
GP1BA_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:10497
GeneCards
S100A7
GenBank Gene Database
M86757
GenBank Protein Database
190668
UniProt Accession
S10A7_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:2623
GenAtlas
CYP2C9
GeneCards
CYP2C9
GenBank Gene Database
AY341248
Guide to Pharmacology
1326
UniProt Accession
CP2C9_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:2622
GenAtlas
CYP2C8
GeneCards
CYP2C8
GenBank Gene Database
M17397
Guide to Pharmacology
1325
UniProt Accession
CP2C8_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:2621
GeneCards
CYP2C19
GenBank Gene Database
M61854
GenBank Protein Database
181344
Guide to Pharmacology
1328
UniProt Accession
CP2CJ_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:12535
GeneCards
UGT1A3
GenBank Gene Database
M84127
GenBank Protein Database
340135
UniProt Accession
UD13_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:12541
GeneCards
UGT1A9
GenBank Gene Database
S55985
GenBank Protein Database
7690346
UniProt Accession
UD19_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:12553
GeneCards
UGT2B4
GenBank Gene Database
Y00317
GenBank Protein Database
37589
UniProt Accession
UD2B4_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:12554
GeneCards
UGT2B7
GenBank Gene Database
J05428
GenBank Protein Database
340080
UniProt Accession
UD2B7_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:451
UniProt Accession
D6RB81_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:2637
GenAtlas
CYP3A4
GeneCards
CYP3A4
GenBank Gene Database
M18907
Guide to Pharmacology
1337
UniProt Accession
CP3A4_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:399
GenAtlas
ALB
GeneCards
ALB
GenBank Gene Database
V00494
GenBank Protein Database
28590
UniProt Accession
ALBU_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:10962
GenAtlas
SLCO2B1
GeneCards
SLCO2B1
GenBank Gene Database
AB026256
GenBank Protein Database
5006263
Guide to Pharmacology
1224
UniProt Accession
SO2B1_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:40
GenAtlas
ABCB1
GeneCards
ABCB1
GenBank Gene Database
M14758
GenBank Protein Database
307180
Guide to Pharmacology
768
UniProt Accession
MDR1_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:55
GenAtlas
ABCC4
GeneCards
ABCC4
GenBank Gene Database
AF071202
GenBank Protein Database
3335173
Guide to Pharmacology
782
UniProt Accession
MRP4_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:51
GenAtlas
ABCC1
GeneCards
ABCC1
GenBank Gene Database
L05628
GenBank Protein Database
1835659
Guide to Pharmacology
779
UniProt Accession
MRP1_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:10956
GeneCards
SLCO1A2
GenBank Gene Database
U21943
GenBank Protein Database
885978
Guide to Pharmacology
1219
UniProt Accession
SO1A2_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:10970
GenAtlas
hROAT1
GeneCards
SLC22A6
GenBank Gene Database
AF057039
GenBank Protein Database
3831566
Guide to Pharmacology
1025
UniProt Accession
S22A6_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:10972
GeneCards
SLC22A8
GenBank Gene Database
AF097491
GenBank Protein Database
4378059
Guide to Pharmacology
1027
UniProt Accession
S22A8_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:18120
GenAtlas
SLC22A11
GeneCards
SLC22A11
GenBank Gene Database
AB026116
GenBank Protein Database
7707622
Guide to Pharmacology
1030
UniProt Accession
S22AB_HUMAN
International reference pricing
71 formulations
Reference pricing from DrugBank. Prices are indicative and may not reflect current UK costs.
From $0.02/caplet
To $304.50/ml
CVS Pharmacy ibuprofen 200 mg caplet
$0.02/caplet
Pv ibuprofen 200 mg tablet
$0.02/tablet
Ibuprofen 200 mg tablet
$0.03/tablet
Children's motrin cold
$0.04/ml
Pv ibuprofen 200 mg caplet
$0.04/caplet
Source: DrugBank. Used under CC BY-NC 4.0 academic licence for non-commercial purposes.
Patent information
27 active patents, 13 expired
11918693
United States
Approved 5 Mar 2024 · Expires 9 Jul 2041
15y 3m
11197830
United States
Approved 14 Dec 2021 · Expires 27 Feb 2039
12y 11m
11534407
United States
Approved 27 Dec 2022 · Expires 27 Feb 2039
12y 11m
11213498
United States
Approved 4 Jan 2022 · Expires 14 Jan 2036
9y 9m
11389416
United States
Approved 19 Jul 2022 · Expires 17 Jul 2035
9y 3m
The earliest active patent expires July 2026. Generic versions may become available after this date.
Source: DrugBank · CC BY-NC 4.0. Patent data sourced from national patent offices. Expiry dates may not reflect extensions, regulatory exclusivity periods, or legal challenges.
DrugBank citations
If you use DrugBank data in your research, please cite the following publications:
Knox C., Wilson M., Klinger C.M., et al
DrugBank 6.
0: the DrugBank Knowledgebase for 2024
Nucleic Acids Res. 2024 Jan 552(D1):D1265-D1275
Wishart D.S., Feunang Y.D., Guo A.C., et al
DrugBank 5.
0: a major update to the DrugBank database for 2018
Nucleic Acids Res. 2017 Nov 846(D1):D1074-D1082
Show earlier publications
Law V., Knox C., Djoumbou Y., et al
DrugBank 4.
0: shedding new light on drug metabolism
Nucleic Acids Res. 2014 Jan 142(1):D1091-7
Knox C., Law V., Jewison T., et al
DrugBank 3.
0: a comprehensive resource for 'omics' research on drugs
Nucleic Acids Res. 2011 Jan39(Database issue):D1035-41
Wishart D.S., Knox C., Guo A.C., et al
DrugBank: a knowledgebase for drugs, drug actions and drug targets.
Nucleic Acids Research
2008 Jan36(Database issue):D901-6
Wishart D.S., Knox C., Guo A.C., et al
DrugBank: a comprehensive resource for in silico drug discovery and exploration.
Nucleic Acids Research
2006 Jan 134(Database issue):D668-72
Source: go.drugbank.comCC BY-NC 4.0
Updated 26 days ago(8 Mar 2026)