Olsalazine 250mg/5ml oral suspension
Prescription only
Requires a prescription from a doctor or prescriber
Oral suspension
250mg/5ml
Oral
Chronic bowel disorders
Active ingredients:
Olsalazine
No active safety alerts
Official documents, adverse reaction reporting, and safety monitoring
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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.
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Suspected adverse reactions reported for Olsalazine
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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.
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EMA
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Suspected adverse reactions reported for Olsalazine
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EudraVigilance data is published by the European Medicines Agency (EMA). A suspected adverse reaction is not necessarily caused by the medicine.
1 branded products available
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WHO defined daily dose (DDD)
1 gram
Not a recommended dose. The DDD is the assumed average maintenance dose per day for a drug used for its main indication in adults. It is a statistical measure used for research and comparison purposes only.
Source: WHO Collaborating Centre for Drug Statistics Methodology, distributed via NHS dm+d BNF mapping files. Contains public sector information licensed under the Open Government Licence v3.0.
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Tablet
1.6g
Same therapeutic group
Mesalazine 1g gastro-resistant tablets
Tablet
1g
Same therapeutic group
Mesalazine 300mg/5ml oral suspension
Oral suspension
300mg/5ml
Same therapeutic group
Mesalazine 4g modified-release granules sachets sugar free
Granules
4g
Same therapeutic group
Mesalazine 3g gastro-resistant modified-release granules sachets sugar free
Granules
3g
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
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Clinical guidelines and formulary information
British National Formulary
Olsalazine
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(1)
Source: National Institute for Health and Care Excellence (NICE). Contains public sector information licensed under the Open Government Licence v3.0.
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Supply & product information
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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
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These codes are used by healthcare IT systems and prescribers to identify this medicine.
NHS UK identifiers
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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
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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
234 found
Half-life
0.9 hours
Mechanism
Upon administration, the azo bond connecting two molecules of mesalamine (also k…
Food interactions
1 warning
Human targets
3 targets
Data: DrugBank · CC BY-NC 4.0
Pharmacokinetics at a glance
Absorption
5%
After oral administration, olsalazine has limited systemic bioavailability, with less than 5% of the oral dose being absorbed.
[A257063]…
[A257063]…
Half-life
0.9 hours
Olsalazine has a very short serum half-life, approximately 0.9…
Protein binding
99%
Olsalazine and its metabolite olsalazine-S, are more than 99% bound to plasma proteins.…
Volume of distribution
5L
The steady-state volume of distribution determined in healthy volunteers is approximately 5L.
[A257063]
[A257063]
Metabolism
0.1%
Olsalazine is cleaved by colonic bacteria to release its active ingredient, mesalamine.…
Elimination
90 to 97%
Olsalazine and its metabolites are excreted in the urine.
[A257063]
Total recovery of oral 14C-labeled olsalazine in animals and humans ranges from 90 to 97%.…
[A257063]
Total recovery of oral 14C-labeled olsalazine in animals and humans ranges from 90 to 97%.…
Pharmacokinetic data: DrugBank · CC BY-NC 4.0
Status:
Approved
Small molecule
About this compound
Olsalazine is an aminosalicylate and a prodrug of [mesalamine] (5-aminosalicylic acid, 5-ASA).[A257063] It was first developed for delivering mesalamine to the colon without the use of [sulfapyridine].[A257078] Olsalazine comprises two mesalamine molecules joined by an azo bridge, which is cleaved in the colon.[A257078] Olsalazine is an anti-inflammatory agent that works by inhibiting cyclooxygenase and lipoxygenase, subsequently reducing the production of pro-inflammatory factors like prostaglandin and leukotriene.[A257063] Olsalazine is used in the treatment of ulcerative colitis.[L45023][L45151]
Properties:
solid
Avg. mass: 302.24 Da
DrugBank indication
In the US, olsalazine is indicated for the maintenance of remission of ulcerative colitis in adult patients who are intolerant to [sulfasalazine].
[L45023]
In Canada, it is used in the treatment of acute ulcerative colitis of mild to moderate severity, with or without the concomitant use of steroids. It is also indicated for the long-term maintenance of patients with ulcerative colitis in remission.
[L45151]
[L45023]
In Canada, it is used in the treatment of acute ulcerative colitis of mild to moderate severity, with or without the concomitant use of steroids. It is also indicated for the long-term maintenance of patients with ulcerative colitis in remission.
[L45151]
Also known as(73)
Olsalazine
1.14.99.1
COX-1
COX1
Cyclooxygenase-1
PGH synthase 1
PGHS-1
PHS 1
Dosage forms(5)
Capsule (Oral)
Capsule (Oral) — 250 mg/1
Capsule (Oral) — 250 mg
Capsule, gelatin coated (Oral) — 250 mg/1
Tablet (Oral) — 500 MG
Molecular properties(19)
Drug interactions(975)
Known interactions with other medications. Always consult a healthcare professional.
Ammonium chloride
Unknown severity
The serum concentration of Olsalazine can be increased when it is combined with Ammonium chloride.
Ginkgo biloba
Unknown severity
The risk or severity of bleeding can be increased when Ginkgo biloba is combined with Olsalazine.
Pralatrexate
Unknown severity
The serum concentration of Pralatrexate can be increased when it is combined with Olsalazine.
Desmopressin
Moderate
Olsalazine may decrease the excretion rate of Desmopressin which could result in a higher serum level.
Olsalazine may decrease the excretion rate of Digoxin which could result in a higher serum level.
Metildigoxin
Unknown severity
The serum concentration of Metildigoxin can be decreased when it is combined with Olsalazine.
Acetyldigoxin
Unknown severity
The serum concentration of Acetyldigoxin can be decreased when it is combined with Olsalazine.
Haloperidol
Moderate
Olsalazine may decrease the excretion rate of Haloperidol which could result in a higher serum level.
Hydralazine
Moderate
Olsalazine may decrease the excretion rate of Hydralazine which could result in a higher serum level.
The risk or severity of nephrotoxicity can be increased when Lithium citrate is combined with Olsalazine.
The risk or severity of nephrotoxicity can be increased when Lithium carbonate is combined with Olsalazine.
Methotrexate
Major
The risk or severity of nephrotoxicity can be increased when Methotrexate is combined with Olsalazine.
Pemetrexed
Moderate
Olsalazine may decrease the excretion rate of Pemetrexed which could result in a higher serum level.
Probenecid
Moderate
The therapeutic efficacy of Probenecid can be decreased when used in combination with Olsalazine.
Treprostinil
Unknown severity
The risk or severity of bleeding can be increased when Treprostinil is combined with Olsalazine.
Vancomycin
Major
The risk or severity of nephrotoxicity can be increased when Vancomycin is combined with Olsalazine.
The risk or severity of nephrotoxicity can be increased when Olsalazine is combined with Foscarnet.
The risk or severity of nephrotoxicity can be increased when Mannitol is combined with Olsalazine.
The risk or severity of nephrotoxicity can be increased when Tenofovir disoproxil is combined with Olsalazine.
The risk or severity of nephrotoxicity can be increased when Tenofovir alafenamide is combined with Olsalazine.
The risk or severity of nephrotoxicity can be increased when Tenofovir is combined with Olsalazine.
The risk or severity of nephrotoxicity and hypocalcemia can be increased when Olsalazine is combined with Alendronic acid.
The risk or severity of bleeding can be increased when Olsalazine is combined with Lepirudin.
Bivalirudin
Unknown severity
The risk or severity of bleeding can be increased when Olsalazine is combined with Bivalirudin.
The risk or severity of bleeding can be increased when Olsalazine is combined with Alteplase.
The risk or severity of bleeding can be increased when Olsalazine is combined with Urokinase.
The risk or severity of bleeding can be increased when Olsalazine is combined with Reteplase.
Anistreplase
Unknown severity
The risk or severity of bleeding can be increased when Olsalazine is combined with Anistreplase.
Tenecteplase
Unknown severity
The risk or severity of bleeding can be increased when Olsalazine is combined with Tenecteplase.
The risk or severity of bleeding can be increased when Olsalazine is combined with Abciximab.
Drotrecogin alfa
Unknown severity
The risk or severity of bleeding can be increased when Olsalazine is combined with Drotrecogin alfa.
Streptokinase
Unknown severity
The risk or severity of bleeding can be increased when Olsalazine is combined with Streptokinase.
Dicoumarol
Moderate
Olsalazine may increase the anticoagulant activities of Dicoumarol.
Argatroban
Unknown severity
The risk or severity of bleeding can be increased when Olsalazine is combined with Argatroban.
The risk or severity of bleeding can be increased when Ardeparin is combined with Olsalazine.
Phenindione
Moderate
Olsalazine may increase the anticoagulant activities of Phenindione.
Fondaparinux
Unknown severity
The risk or severity of bleeding can be increased when Olsalazine is combined with Fondaparinux.
The risk or severity of bleeding can be increased when Warfarin is combined with Olsalazine.
Pentosan polysulfate
Unknown severity
The risk or severity of bleeding can be increased when Pentosan polysulfate is combined with Olsalazine.
Phenprocoumon
Moderate
Olsalazine may increase the anticoagulant activities of Phenprocoumon.
Dipyridamole
Unknown severity
The risk or severity of bleeding can be increased when Olsalazine is combined with Dipyridamole.
The risk or severity of bleeding can be increased when Heparin is combined with Olsalazine.
Enoxaparin
Unknown severity
The risk or severity of bleeding can be increased when Enoxaparin is combined with Olsalazine.
Epoprostenol
Unknown severity
The risk or severity of bleeding can be increased when Olsalazine is combined with Epoprostenol.
Acenocoumarol
Unknown severity
The risk or severity of bleeding can be increased when Acenocoumarol is combined with Olsalazine.
4-hydroxycoumarin
Moderate
Olsalazine may increase the anticoagulant activities of 4-hydroxycoumarin.
Olsalazine may increase the anticoagulant activities of Coumarin.
Ximelagatran
Unknown severity
The risk or severity of bleeding can be increased when Olsalazine is combined with Ximelagatran.
Desmoteplase
Unknown severity
The risk or severity of bleeding can be increased when Olsalazine is combined with Desmoteplase.
Defibrotide
Unknown severity
The risk or severity of bleeding can be increased when Olsalazine is combined with Defibrotide.
Showing 50 of 975 interactions
Food & lifestyle interactions
Take With Food
Take with food. Food does not affect drug absorption or exposure, but may mitigate the risk for drug-related adverse effects.
Toxicity & overdose
There is no information available regarding acute toxicity (LD50) of olsalazine. Symptoms of salicylate toxicity include nausea, vomiting and abdominal pain, tachypnea, hyperpnea, tinnitus, and neurologic symptoms (headache, dizziness, confusion, seizures). Severe intoxication may lead to electrolyte and blood pH imbalance and potentially to organ damage.
There is no antidote for olsalazine overdose; however, conventional therapy for salicylate toxicity, such as gastrointestinal tract decontamination, may be beneficial in acute overdosage. Overdose should be managed with proper medical care and appropriate supportive care, including the possible use of emesis, cathartics, and activated charcoal to prevent further absorption. Fluid and electrolyte imbalance may be managed with appropriate intravenous therapy and maintenance of adequate renal function.
[L45023]
There is no antidote for olsalazine overdose; however, conventional therapy for salicylate toxicity, such as gastrointestinal tract decontamination, may be beneficial in acute overdosage. Overdose should be managed with proper medical care and appropriate supportive care, including the possible use of emesis, cathartics, and activated charcoal to prevent further absorption. Fluid and electrolyte imbalance may be managed with appropriate intravenous therapy and maintenance of adequate renal function.
[L45023]
How it works
Mechanism of action
Upon administration, the azo bond connecting two molecules of mesalamine (also known as 5-aminosalicylic acid or 5-ASA) is cleaved by azoreductase-containing bacteria in the colon. The two molecules of mesalamine are released to mediate therapeutic effects.[A257063] The exact mechanism of action of olsalazine and its active moiety mesalamine in ulcerative colitis has not been elucidated; however, it is understood that mesalamine mediates an anti-inflammatory action on epithelial cells of the colon.[L45023] The COX-derived (i.e., prostanoids such as prostaglandin E2) and lipoxygenase-derived products (i.e., leukotrienes [LTs] and hydroxyeicosatetraenoic acids [HETEs]) of arachidonic acid metabolism have been implicated in the pathogenesis and maintenance of inflammatory disorders, including ulcerative colitis and inflammatory bowel disease.[A257063][L45023] Mesalamine may attenuate inflammation by blocking the COX enzyme and inhibiting prostaglandin production in the colon.[A257221][A4391][L45023] Olsalazine was also shown to inhibit xanthine oxidase, an enzyme that generates oxygen-derived free radicals.[A257078]
Olsalazine may attenuate intestinal inflammation by limiting macrophage migration to inflamed intestinal mucosa: it was shown to inhibit in vitro migration of intestinal macrophages in response to leukotriene B4. Olsalazine may also act as a free radical scavenger, and mesalazine may suppress fatty acid peroxidation.[A257063]
Olsalazine may attenuate intestinal inflammation by limiting macrophage migration to inflamed intestinal mucosa: it was shown to inhibit in vitro migration of intestinal macrophages in response to leukotriene B4. Olsalazine may also act as a free radical scavenger, and mesalazine may suppress fatty acid peroxidation.[A257063]
Pharmacodynamics
Olsalazine is an anti-inflammatory agent that blocks the production of cyclooxygenase (COX)-derived products of arachidonic acid metabolism.[L45023] It works to alleviate inflammation in ulcerative colitis.[A257063]
Olsalazine was shown to decrease water and sodium absorption. While olsalazine is not expected to affect the motility and transit time of small intestines, it decreased small bowel transit time at high doses ranging from 60 to 120 mg/kg. In about 40% of the patients with ulcerative colitis, administration of olsalazine 1g daily was associated with a decrease in whole gut transit time.[A257063]
Olsalazine was shown to decrease water and sodium absorption. While olsalazine is not expected to affect the motility and transit time of small intestines, it decreased small bowel transit time at high doses ranging from 60 to 120 mg/kg. In about 40% of the patients with ulcerative colitis, administration of olsalazine 1g daily was associated with a decrease in whole gut transit time.[A257063]
Pharmacokinetics
How the body processes this drug — absorption, distribution, metabolism, and elimination
Absorption
After oral administration, olsalazine has limited systemic bioavailability, with less than 5% of the oral dose being absorbed.
[A257063]
Based on oral and intravenous dosing studies, approximately 2.4% of a single 1 g oral dose is absorbed. Maximum serum concentrations of olsalazine appear after approximately one hour and, even after a 1 g single dose, are low (e.g., 1.6 to 6.2 µmol/L).
[L45023]
Patients on daily doses of 1 g olsalazine for two to four years show a stable plasma concentration of olsalazine-S (3.3 to 12.4 µmol/L). Olsalazine-S accumulates to a steady state within two to three weeks.
Serum concentrations of mesalamine are detected after four to eight hours. The peak levels of mesalamine after an oral dose of 1 g olsalazine are low (i.e., 0 to 4.3 µmol/L).
[L45023]
[A257063]
Based on oral and intravenous dosing studies, approximately 2.4% of a single 1 g oral dose is absorbed. Maximum serum concentrations of olsalazine appear after approximately one hour and, even after a 1 g single dose, are low (e.g., 1.6 to 6.2 µmol/L).
[L45023]
Patients on daily doses of 1 g olsalazine for two to four years show a stable plasma concentration of olsalazine-S (3.3 to 12.4 µmol/L). Olsalazine-S accumulates to a steady state within two to three weeks.
Serum concentrations of mesalamine are detected after four to eight hours. The peak levels of mesalamine after an oral dose of 1 g olsalazine are low (i.e., 0 to 4.3 µmol/L).
[L45023]
Half-life
Olsalazine has a very short serum half-life, approximately 0.9 hours. Olsalazine-S has a half-life of seven days due to slow dissociation from the protein binding site.
[A257063][L45023]
[A257063][L45023]
Protein binding
Olsalazine and its metabolite olsalazine-S, are more than 99% bound to plasma proteins. Less than 1% of both olsalazine and olsalazine-S appears undissociated in plasma. It does not interfere with the protein binding of warfarin.
[L45023]
Mesalamine (5-aminosalicylic acid, 5-ASA) and its metabolite, N-acetyl-5-ASA, are 74 and 81%, respectively, bound to plasma proteins.
[L45023]
[L45023]
Mesalamine (5-aminosalicylic acid, 5-ASA) and its metabolite, N-acetyl-5-ASA, are 74 and 81%, respectively, bound to plasma proteins.
[L45023]
Volume of distribution
The steady-state volume of distribution determined in healthy volunteers is approximately 5L.
[A257063]
[A257063]
Metabolism
Olsalazine is cleaved by colonic bacteria to release its active ingredient, mesalamine. Mesalamine can undergo acetylation to form N-acetyl-5-aminosalicylic acid (N-acetyl-5-ASA, Ac-5-ASA) by the colonic epithelium; however, the extent of acetylation depends on transit time.
[A257063]
Approximately 0.1% of an oral dose of olsalazine is metabolized in the liver to olsalazine-O-sulfate (olsalazine-S).
[L45023]
[A257063]
Approximately 0.1% of an oral dose of olsalazine is metabolized in the liver to olsalazine-O-sulfate (olsalazine-S).
[L45023]
Route of elimination
Olsalazine and its metabolites are excreted in the urine.
[A257063]
Total recovery of oral 14C-labeled olsalazine in animals and humans ranges from 90 to 97%. Approximately 20% of the total mesalamine is recovered in the urine. Of the total mesalamine found in the urine, more than 90% is N-acetyl-5-ASA.
Only small amounts of mesalamine are detected in the urine. The remaining mesalamine is partially acetylated and excreted in the feces. From fecal dialysis, the concentration of mesalamine in the colon following olsalazine has been calculated to be 18 to 49 mmol/L.
[L45023]
The urinary recovery of olsalazine is below 1%.
[L45023]
Less than 5% of an oral dose (0.25 to 2g) was recovered unchanged in the feces; however, more than 50% of the oral dose was excreted in feces as unchanged olsalazine when the whole gut transit time was decreased by approximately 50%.
[A257063]
[A257063]
Total recovery of oral 14C-labeled olsalazine in animals and humans ranges from 90 to 97%. Approximately 20% of the total mesalamine is recovered in the urine. Of the total mesalamine found in the urine, more than 90% is N-acetyl-5-ASA.
Only small amounts of mesalamine are detected in the urine. The remaining mesalamine is partially acetylated and excreted in the feces. From fecal dialysis, the concentration of mesalamine in the colon following olsalazine has been calculated to be 18 to 49 mmol/L.
[L45023]
The urinary recovery of olsalazine is below 1%.
[L45023]
Less than 5% of an oral dose (0.25 to 2g) was recovered unchanged in the feces; however, more than 50% of the oral dose was excreted in feces as unchanged olsalazine when the whole gut transit time was decreased by approximately 50%.
[A257063]
Drug targets(3)
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)
Thiopurine S-methyltransferase
TPMT
inhibitor
Specific functionS-adenosyl-L-methionine binding
Cellular location
Cytoplasm
General function & pharmacology
Catalyzes the S-methylation of thiopurine drugs such as 6-mercaptopurine (also called mercaptopurine, 6-MP or its brand name Purinethol) and 6-thioguanine (also called tioguanine or 6-TG) using S-adenosyl-L-methionine as the methyl donor .
PMID:18484748 PMID:657528
TPMT activity modulates the cytotoxic effects of thiopurine prodrugs. A natural substrate for this enzyme has yet to be identified
PMID:18484748 PMID:657528
TPMT activity modulates the cytotoxic effects of thiopurine prodrugs. A natural substrate for this enzyme has yet to be identified
Xanthine dehydrogenase/oxidase
XDH
inhibitor
Specific function2 iron, 2 sulfur cluster binding
Cellular location
Cytoplasm
General function & pharmacology
Key enzyme in purine degradation. Catalyzes the oxidation of hypoxanthine to xanthine. Catalyzes the oxidation of xanthine to uric acid.
Contributes to the generation of reactive oxygen species. Has also low oxidase activity towards aldehydes (in vitro)
Contributes to the generation of reactive oxygen species. Has also low oxidase activity towards aldehydes (in vitro)
Transporters(5)
Proteins that transport this drug across cell membranes
Solute carrier family 2, facilitated glucose transporter member 9
SLC2A9
downregulator
Specific functioncarbohydrate
Cellular location
Cell membrane
General function & pharmacology
High-capacity urate transporter, which may play a role in the urate reabsorption by proximal tubules .
PMID:18327257 PMID:18701466 PMID:22647630 PMID:28083649 PMID:36749388
May have a residual high-affinity, low-capacity glucose and fructose transporter activity .
PMID:18327257 PMID:18701466 PMID:18842065
Transports urate at rates 45- to 60-fold faster than glucose .
PMID:18842065
Does not transport galactose .
PMID:28083649
May mediate small uptake of adenine but not of other nucleobases PMID:22647630
PMID:18327257 PMID:18701466 PMID:22647630 PMID:28083649 PMID:36749388
May have a residual high-affinity, low-capacity glucose and fructose transporter activity .
PMID:18327257 PMID:18701466 PMID:18842065
Transports urate at rates 45- to 60-fold faster than glucose .
PMID:18842065
Does not transport galactose .
PMID:28083649
May mediate small uptake of adenine but not of other nucleobases PMID:22647630
Solute carrier family 22 member 6
SLC22A6
upregulator
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
upregulator
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)
Sodium-dependent phosphate transporter 1
SLC20A1
upregulator
Specific functionhigh-affinity phosphate
Cellular location
Cell membrane
General function & pharmacology
Sodium-phosphate symporter which preferentially transports the monovalent form of phosphate with a stoichiometry of two sodium ions per phosphate ion .
PMID:11009570 PMID:16790504 PMID:17494632 PMID:19726692 PMID:7929240 PMID:8041748
May play a role in extracellular matrix and cartilage calcification as well as in vascular calcification .
PMID:11009570
Essential for cell proliferation but this function is independent of its phosphate transporter activity PMID:19726692
PMID:11009570 PMID:16790504 PMID:17494632 PMID:19726692 PMID:7929240 PMID:8041748
May play a role in extracellular matrix and cartilage calcification as well as in vascular calcification .
PMID:11009570
Essential for cell proliferation but this function is independent of its phosphate transporter activity PMID:19726692
Sodium/potassium-transporting ATPase subunit gamma
FXYD2
inhibitor
Specific functionATPase activator activity
Cellular location
Membrane
General function & pharmacology
May be involved in forming the receptor site for cardiac glycoside binding or may modulate the transport function of the sodium ATPase
Scientific references(4)
Wadworth A.N., Fitton A.
Olsalazine.
A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential in inflammatory bowel disease
Drugs. 1991 Apr41(4):647-64. doi: 10.2165/00003495-199141040-00009
Campbell D.E., Berglindh T.
Pharmacology of olsalazine.
Scand Journal Gastroenterol Suppl
1988148:7-12. doi: 10.3109/00365528809101539
Horn H., Preclik G., Stange E.F., Ditschuneit H.
Modulation of arachidonic acid metabolism by olsalazine and other aminosalicylates in leukocytes.
Scand Journal Gastroenterol
1991 Aug26(8):867-79. doi: 10.3109/00365529109037024
Allgayer H.
Review article: mechanisms of action of mesalazine in preventing colorectal carcinoma in inflammatory bowel disease.
Alimentary Pharmacology & Therapeutics
200318(s2):10-14. doi: 10.1046/j.1365-2036.18.s2.1.x
ATC classification(1 code)
ATC A07EC03
Affected organisms(1)
Humans and other mammals
Salt forms(1)
Olsalazine sodium(DBSALT000191)
Experimental properties(1)
Protein Data Bank entries(1)
Commercial products(6)
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)
Olsalazine
Additional database identifiers
Drugs Product Database (DPD)
1226
ChemSpider
10642377
PDB
JBC
ZINC
ZINC000003812865
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: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:12014
GenAtlas
TPMT
GeneCards
TPMT
GenBank Gene Database
S62904
GenBank Protein Database
386420
UniProt Accession
TPMT_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:12805
GenAtlas
XDH
GeneCards
XDH
GenBank Gene Database
D11456
GenBank Protein Database
10336525
Guide to Pharmacology
2646
UniProt Accession
XDH_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:13446
GeneCards
SLC2A9
UniProt Accession
GTR9_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:10946
GeneCards
SLC20A1
UniProt Accession
S20A1_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:799
GenAtlas
ATP1A1
GeneCards
ATP1A1
GenBank Gene Database
D00099
GenBank Protein Database
219942
UniProt Accession
AT1A1_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:800
GeneCards
ATP1A2
UniProt Accession
AT1A2_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:801
GeneCards
ATP1A3
UniProt Accession
AT1A3_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:14073
GeneCards
ATP1A4
UniProt Accession
AT1A4_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:804
GeneCards
ATP1B1
UniProt Accession
AT1B1_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:805
GeneCards
ATP1B2
UniProt Accession
AT1B2_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:806
GeneCards
ATP1B3
UniProt Accession
AT1B3_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:4026
GenAtlas
FXYD2
GeneCards
FXYD2
GenBank Gene Database
U50743
GenBank Protein Database
1575004
UniProt Accession
ATNG_HUMAN
International reference pricing
1 formulations
Reference pricing from DrugBank. Prices are indicative and may not reflect current UK costs.
Dipentum 250 mg capsule
$1.80/capsule
Source: DrugBank. Used under CC BY-NC 4.0 academic licence for non-commercial purposes.
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)