Cabotegravir 600mg/3ml prolonged-release suspension for injection vials
Prescription only
Requires a prescription from a doctor or prescriber
Antiviral drugs
Active ingredients:
Cabotegravir
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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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
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Suspected adverse reactions reported for Cabotegravir
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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.
2 branded products available
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2 products
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Apretude 600mg/3ml prolonged-release suspension for injection vials
Vocabria 600mg/3ml prolonged-release suspension for injection vials
Therapeutically similar medicines
Show details
Cabotegravir 30mg tablets
Tablet
30mg
Same therapeutic group
Dolutegravir 5mg dispersible tablets sugar free
Tablet
5mg
Same therapeutic group
Raltegravir 600mg tablets
Tablet
600mg
Same therapeutic group
Dolutegravir 10mg tablets
Tablet
10mg
Same therapeutic group
Dolutegravir 25mg tablets
Tablet
25mg
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
Cabotegravir
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(2)
Cabotegravir with rilpivirine for treating HIV-1 (TA757)
TA757
Technology appraisal
Updated Jan 2022Cabotegravir for preventing HIV-1 in adults and young people (TA1106)
TA1106
Technology appraisal
Updated Nov 2025Source: 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
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
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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
None known
Half-life
41 hours
Mechanism
Cabotegravir binds to the active site of HIV integrase, preventing strand transf…
Food interactions
2 warnings
Human targets
None mapped
Data: DrugBank · CC BY-NC 4.0
Pharmacokinetics at a glance
Absorption
3 hours
Oral cabotegravir has a Tmax of 3 hours, reaches a Cmax of 8.0…
Half-life
41 hours
The mean half life of oral cabotegravir is 41 hours.
[L31188]
The mean half life of intramuscular extended-release cabotegravir is 5.6-11.5…
[L31188]
The mean half life of intramuscular extended-release cabotegravir is 5.6-11.5…
Protein binding
99.8%
Cabotegravir is >99.8% bound to proteins in plasma, usually alubmin.
[A227643][L31188]
[A227643][L31188]
Volume of distribution
Data regarding the volume of distribution of cabotegravir is not readily available.
[A227663][L31193][L31203]
[A227663][L31193][L31203]
Metabolism
67%
Cabotegravir is O-glucuronidated to the M1 and M2 metabolites, with 67% of glucuronidation performed by UGT1A1, and 33% by UGT1A9.
[A227653][A227658]
[A227653][A227658]
Elimination
58.5%
An oral radiolabelled dose of cabotegravir is 58.5% recovered in the feces and 26.8% recovered in the urine.
[A227653][A227658][L31188]
[A227653][A227658][L31188]
Clearance
0.34 mL/min/kg
Data regarding the clearance of cabotegravir is not readily available.
[A227663][L31193][L31203]…
[A227663][L31193][L31203]…
Pharmacokinetic data: DrugBank · CC BY-NC 4.0
Status:
Approved
Investigational
Small molecule
About this compound
Cabotegravir, or GSK1265744, is an HIV-1 integrase inhibitor that is prescribed with the non-nucleoside reverse transcriptase inhibitor, [rilpivirine].[A227668][L31188][L31193] Early research into cabotegravir showed it had lower oral bioavailability than [dolutegravir],[A227668] which resulted in the development of long acting monthly intramuscular injection formulation for cabotegravir.[A227668][L31193]
Cabotegravir was granted FDA approval on 21 January 2021 in combination with rilpivirine to treat HIV-1 infection in virologically suppressed individuals.[L31198] While previously administered once monthly only, this combination product was granted FDA approval for dosing every two months on February 01, 2022 [L40084] and without the need for an oral lead-in period prior.[L31193]
Cabotegravir was granted FDA approval on 21 January 2021 in combination with rilpivirine to treat HIV-1 infection in virologically suppressed individuals.[L31198] While previously administered once monthly only, this combination product was granted FDA approval for dosing every two months on February 01, 2022 [L40084] and without the need for an oral lead-in period prior.[L31193]
Properties:
liquid
Avg. mass: 405.36 Da
DrugBank indication
Oral cabotegravir is indicated in combination with [rilpivirine] for the short-term treatment of HIV-1 in virologically suppressed adults with no history of treatment failure to assess tolerability of cabotegravir or who have missed an injected dose of cabotegravir.
[L31188]
Intramuscular extended-release cabotegravir in combination with rilpivirine is indicated as a complete regimen for the treatment of HIV-1 infection in adults and adolescents 12 years of age and older weighing at least 35 kg to replace the current antiretroviral regimen in those who are virologically suppressed (HIV-1 RNA <50 copies/mL) on a stable antiretroviral regimen with no history of treatment failure and with no known or suspected resistance to either cabotegravir or rilpivirine.
[L31193]
An extended-release injectable suspension formulation of cabotegravir is also indicated for the prevention of sexually-acquired HIV-1 infection (i.e. for pre-exposure prophylaxis, PrEP) in at-risk adults and adolescents weighing at least 35kg.
[L39548]
[L31188]
Intramuscular extended-release cabotegravir in combination with rilpivirine is indicated as a complete regimen for the treatment of HIV-1 infection in adults and adolescents 12 years of age and older weighing at least 35 kg to replace the current antiretroviral regimen in those who are virologically suppressed (HIV-1 RNA <50 copies/mL) on a stable antiretroviral regimen with no history of treatment failure and with no known or suspected resistance to either cabotegravir or rilpivirine.
[L31193]
An extended-release injectable suspension formulation of cabotegravir is also indicated for the prevention of sexually-acquired HIV-1 infection (i.e. for pre-exposure prophylaxis, PrEP) in at-risk adults and adolescents weighing at least 35kg.
[L39548]
Also known as(58)
Cabotegravir
Integrase
Pr160Gag-Pol
Pr160Gag-Pol
2.4.1.17
Bilirubin-specific UDPGT isozyme 1
GNT1
hUG-BR1
Dosage forms(17)
(Intramuscular) — 600 mg
Injection, suspension, extended release; kit (Intramuscular) — 200 mg/1mL
Suspension (Intramuscular) — 600.000 mg
Suspension, extended release (Intramuscular) — 200 mg / mL
Tablet (Oral) — 31.620 mg
Suspension (Intramuscular) — 600 mg
Injection, suspension, extended release; kit (Intramuscular)
Kit; suspension, extended release (Intramuscular)
Molecular properties(17)
Drug interactions(162)
Known interactions with other medications. Always consult a healthcare professional.
Succinic acid
Unknown severity
The excretion of Succinic acid can be decreased when combined with Cabotegravir.
Citrulline
Unknown severity
The excretion of Citrulline can be decreased when combined with Cabotegravir.
Pravastatin
Unknown severity
The excretion of Pravastatin can be decreased when combined with Cabotegravir.
Oseltamivir
Unknown severity
The excretion of Oseltamivir can be decreased when combined with Cabotegravir.
The excretion of Cefotiam can be decreased when combined with Cabotegravir.
Conjugated estrogens
Unknown severity
The excretion of Conjugated estrogens can be decreased when combined with Cabotegravir.
Tenofovir disoproxil
Unknown severity
The excretion of Tenofovir disoproxil can be decreased when combined with Cabotegravir.
Piperacillin
Unknown severity
The excretion of Piperacillin can be decreased when combined with Cabotegravir.
Indomethacin
Unknown severity
The excretion of Indomethacin can be decreased when combined with Cabotegravir.
Aminohippuric acid
Unknown severity
The excretion of Aminohippuric acid can be decreased when combined with Cabotegravir.
Trifluridine
Unknown severity
The excretion of Trifluridine can be decreased when combined with Cabotegravir.
Allopurinol
Unknown severity
The excretion of Allopurinol can be decreased when combined with Cabotegravir.
Zidovudine
Unknown severity
The excretion of Zidovudine can be decreased when combined with Cabotegravir.
Cimetidine
Unknown severity
The excretion of Cimetidine can be decreased when combined with Cabotegravir.
The excretion of Cefdinir can be decreased when combined with Cabotegravir.
Methotrexate
Unknown severity
The excretion of Methotrexate can be decreased when combined with Cabotegravir.
Cephalexin
Unknown severity
The excretion of Cephalexin can be decreased when combined with Cabotegravir.
Valaciclovir
Unknown severity
The excretion of Valaciclovir can be decreased when combined with Cabotegravir.
Levocarnitine
Unknown severity
The excretion of Levocarnitine can be decreased when combined with Cabotegravir.
Leucovorin
Unknown severity
The excretion of Leucovorin can be decreased when combined with Cabotegravir.
Fluorescein
Unknown severity
The excretion of Fluorescein can be decreased when combined with Cabotegravir.
Hydrocortisone
Unknown severity
The excretion of Hydrocortisone can be decreased when combined with Cabotegravir.
Tetracycline
Unknown severity
The excretion of Tetracycline can be decreased when combined with Cabotegravir.
The excretion of Estradiol can be decreased when combined with Cabotegravir.
The excretion of Acyclovir can be decreased when combined with Cabotegravir.
The excretion of Cefaclor can be decreased when combined with Cabotegravir.
Ranitidine
Unknown severity
The excretion of Ranitidine can be decreased when combined with Cabotegravir.
The excretion of Quinapril can be decreased when combined with Cabotegravir.
Bumetanide
Unknown severity
The excretion of Bumetanide can be decreased when combined with Cabotegravir.
Dinoprostone
Unknown severity
The excretion of Dinoprostone can be decreased when combined with Cabotegravir.
Famotidine
Unknown severity
The excretion of Famotidine can be decreased when combined with Cabotegravir.
Fexofenadine
Unknown severity
The excretion of Fexofenadine can be decreased when combined with Cabotegravir.
Benzylpenicillin
Unknown severity
The excretion of Benzylpenicillin can be decreased when combined with Cabotegravir.
Rosuvastatin
Unknown severity
The excretion of Rosuvastatin can be decreased when combined with Cabotegravir.
The excretion of Captopril can be decreased when combined with Cabotegravir.
Sitagliptin
Unknown severity
The excretion of Sitagliptin can be decreased when combined with Cabotegravir.
The excretion of Cefazolin can be decreased when combined with Cabotegravir.
Ceftizoxime
Unknown severity
The excretion of Ceftizoxime can be decreased when combined with Cabotegravir.
Cefacetrile
Unknown severity
The excretion of Cefacetrile can be decreased when combined with Cabotegravir.
Ceftibuten
Unknown severity
The excretion of Ceftibuten can be decreased when combined with Cabotegravir.
Tazobactam
Unknown severity
The excretion of Tazobactam can be decreased when combined with Cabotegravir.
Cyclic adenosine monophosphate
Unknown severity
The excretion of Cyclic adenosine monophosphate can be decreased when combined with Cabotegravir.
Cholic Acid
Unknown severity
The excretion of Cholic Acid can be decreased when combined with Cabotegravir.
Glutaric Acid
Unknown severity
The excretion of Glutaric Acid can be decreased when combined with Cabotegravir.
Oxalic Acid
Unknown severity
The excretion of Oxalic Acid can be decreased when combined with Cabotegravir.
Taurocholic acid
Unknown severity
The excretion of Taurocholic acid can be decreased when combined with Cabotegravir.
The excretion of Doripenem can be decreased when combined with Cabotegravir.
Saxagliptin
Unknown severity
The excretion of Saxagliptin can be decreased when combined with Cabotegravir.
Ellagic acid
Unknown severity
The excretion of Ellagic acid can be decreased when combined with Cabotegravir.
Cefaloridine
Unknown severity
The excretion of Cefaloridine can be decreased when combined with Cabotegravir.
Showing 50 of 162 interactions
Food & lifestyle interactions
Advice
Take at the same time every day. Take the oral tablets at the same time every day.
Take With Food
Take with food. Take the oral tablets with a meal.
Toxicity & overdose
Data regarding the toxicity of cabotegravir is not readily available.
[L31188][L31193][L31203]
In the event of overdose, patients should have their vital signs monitored, including an ECG to monitor the QT interval.
[L31188][L31193]
Treat patients symptomatically and supportively.
[L31188][L31193]
As cabotegravir is highly protein bound, dialysis is not expected to remove a significant amount of the drug from plasma.
[L31188][L31193]
[L31188][L31193][L31203]
In the event of overdose, patients should have their vital signs monitored, including an ECG to monitor the QT interval.
[L31188][L31193]
Treat patients symptomatically and supportively.
[L31188][L31193]
As cabotegravir is highly protein bound, dialysis is not expected to remove a significant amount of the drug from plasma.
[L31188][L31193]
How it works
Mechanism of action
Cabotegravir binds to the active site of HIV integrase, preventing strand transfer of the viral genome into the host genome, and preventing replication of the virus.[L31188][L31193]
Pharmacodynamics
Cabotegravir is an inhibitor of HIV integrase, which reduces viral replication.[L31188][L31193] It has a long duration of action as the oral tablet is given daily and the intramuscular suspension is given monthly.[L31188][L31193] Patients should be counselled regarding the risk of hypersensitivity, hepatotoxicity, and depression.[L31188][L31193]
Pharmacokinetics
How the body processes this drug — absorption, distribution, metabolism, and elimination
Absorption
Oral cabotegravir has a Tmax of 3 hours, reaches a Cmax of 8.0 µg/mL, and has an AUC of 145 µg\*h/mL.
[L31188]
Intramuscular extended-release cabotegravir has a Tmax of 7 days, reaches a Cmax of 8.0 µg/mL, and has an AUC of 1591 µg\*h/mL.
[L31193]
[L31188]
Intramuscular extended-release cabotegravir has a Tmax of 7 days, reaches a Cmax of 8.0 µg/mL, and has an AUC of 1591 µg\*h/mL.
[L31193]
Half-life
The mean half life of oral cabotegravir is 41 hours.
[L31188]
The mean half life of intramuscular extended-release cabotegravir is 5.6-11.5 weeks.
[L31193]
[L31188]
The mean half life of intramuscular extended-release cabotegravir is 5.6-11.5 weeks.
[L31193]
Protein binding
Cabotegravir is >99.8% bound to proteins in plasma, usually alubmin.
[A227643][L31188]
[A227643][L31188]
Volume of distribution
Data regarding the volume of distribution of cabotegravir is not readily available.
[A227663][L31193][L31203]
[A227663][L31193][L31203]
Metabolism
Cabotegravir is O-glucuronidated to the M1 and M2 metabolites, with 67% of glucuronidation performed by UGT1A1, and 33% by UGT1A9.
[A227653][A227658]
[A227653][A227658]
Route of elimination
An oral radiolabelled dose of cabotegravir is 58.5% recovered in the feces and 26.8% recovered in the urine.
[A227653][A227658][L31188]
[A227653][A227658][L31188]
Clearance
Data regarding the clearance of cabotegravir is not readily available.
[A227663][L31193][L31203]
Clearance in dogs was 0.34 mL/min/kg and in cynomolgus monkeys was 0.32 mL/min/kg.
[A227668]
[A227663][L31193][L31203]
Clearance in dogs was 0.34 mL/min/kg and in cynomolgus monkeys was 0.32 mL/min/kg.
[A227668]
Metabolizing enzymes(2)
Enzymes involved in drug metabolism — important for understanding drug interactions
Enzyme activity key
substrate
inhibitor
inducer
UGT1A1UDP-glucuronosyltransferase 1A1
substrate
UGT1A9UDP-glucuronosyltransferase 1A9
substrate
Transporters(4)
Proteins that transport this drug across cell membranes
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)
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
Broad substrate specificity ATP-binding cassette transporter ABCG2
ABCG2
substrate
Specific functionABC-type xenobiotic transporter activity
Cellular location
Cell membrane
General function & pharmacology
Broad substrate specificity ATP-dependent transporter of the ATP-binding cassette (ABC) family that actively extrudes a wide variety of physiological compounds, dietary toxins and xenobiotics from cells .
PMID:11306452 PMID:12958161 PMID:19506252 PMID:20705604 PMID:28554189 PMID:30405239 PMID:31003562
Involved in porphyrin homeostasis, mediating the export of protoporphyrin IX (PPIX) from both mitochondria to cytosol and cytosol to extracellular space, it also functions in the cellular export of heme .
PMID:20705604 PMID:23189181
Also mediates the efflux of sphingosine-1-P from cells .
PMID:20110355
Acts as a urate exporter functioning in both renal and extrarenal urate excretion .
PMID:19506252 PMID:20368174 PMID:22132962 PMID:31003562 PMID:36749388
In kidney, it also functions as a physiological exporter of the uremic toxin indoxyl sulfate (By similarity). Also involved in the excretion of steroids like estrone 3-sulfate/E1S, 3beta-sulfooxy-androst-5-en-17-one/DHEAS, and other sulfate conjugates .
PMID:12682043 PMID:28554189 PMID:30405239
Mediates the secretion of the riboflavin and biotin vitamins into milk (By similarity). Extrudes pheophorbide a, a phototoxic porphyrin catabolite of chlorophyll, reducing its bioavailability (By similarity).
Plays an important role in the exclusion of xenobiotics from the brain (Probable). It confers to cells a resistance to multiple drugs and other xenobiotics including mitoxantrone, pheophorbide, camptothecin, methotrexate, azidothymidine, and the anthracyclines daunorubicin and doxorubicin, through the control of their efflux .
PMID:11306452 PMID:12477054 PMID:15670731 PMID:18056989 PMID:31254042
In placenta, it limits the penetration of drugs from the maternal plasma into the fetus (By similarity). May play a role in early stem cell self-renewal by blocking differentiation (By similarity).
In inflammatory macrophages, exports itaconate from the cytosol to the extracellular compartment and limits the activation of TFEB-dependent lysosome biogenesis involved in antibacterial innate immune response
PMID:11306452 PMID:12958161 PMID:19506252 PMID:20705604 PMID:28554189 PMID:30405239 PMID:31003562
Involved in porphyrin homeostasis, mediating the export of protoporphyrin IX (PPIX) from both mitochondria to cytosol and cytosol to extracellular space, it also functions in the cellular export of heme .
PMID:20705604 PMID:23189181
Also mediates the efflux of sphingosine-1-P from cells .
PMID:20110355
Acts as a urate exporter functioning in both renal and extrarenal urate excretion .
PMID:19506252 PMID:20368174 PMID:22132962 PMID:31003562 PMID:36749388
In kidney, it also functions as a physiological exporter of the uremic toxin indoxyl sulfate (By similarity). Also involved in the excretion of steroids like estrone 3-sulfate/E1S, 3beta-sulfooxy-androst-5-en-17-one/DHEAS, and other sulfate conjugates .
PMID:12682043 PMID:28554189 PMID:30405239
Mediates the secretion of the riboflavin and biotin vitamins into milk (By similarity). Extrudes pheophorbide a, a phototoxic porphyrin catabolite of chlorophyll, reducing its bioavailability (By similarity).
Plays an important role in the exclusion of xenobiotics from the brain (Probable). It confers to cells a resistance to multiple drugs and other xenobiotics including mitoxantrone, pheophorbide, camptothecin, methotrexate, azidothymidine, and the anthracyclines daunorubicin and doxorubicin, through the control of their efflux .
PMID:11306452 PMID:12477054 PMID:15670731 PMID:18056989 PMID:31254042
In placenta, it limits the penetration of drugs from the maternal plasma into the fetus (By similarity). May play a role in early stem cell self-renewal by blocking differentiation (By similarity).
In inflammatory macrophages, exports itaconate from the cytosol to the extracellular compartment and limits the activation of TFEB-dependent lysosome biogenesis involved in antibacterial innate immune response
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
Scientific references(5)
Bowers G.D., Culp A., Reese M.J., Tabolt G., Moss L., Piscitelli S., Huynh P., Wagner D., Ford S.L., Gould E.P., Pan R., Lou Y., Margolis D.A., Spreen W.R.
Disposition and metabolism of cabotegravir: a comparison of biotransformation and excretion between different species and routes of administration in humans.
Xenobiotica
201646(2):147-62. doi: 10.3109/00498254.2015.1060372. Epub 2015 Jul 1
Patel M., Eberl H.C., Wolf A., Pierre E., Polli J.W., Zamek-Gliszczynski M.J.
Mechanistic Basis of Cabotegravir-Glucuronide Disposition in Humans.
Journal of Pharmacology and Experimental Therapeutics
2019 Aug370(2):269-277. doi: 10.1124/jpet.119.258384. Epub 2019 Jun 7
Spreen W., Min S., Ford S.L., Chen S., Lou Y., Bomar M., St Clair M., Piscitelli S., Fujiwara T.
Pharmacokinetics, safety, and monotherapy antiviral activity of GSK1265744, an HIV integrase strand transfer inhibitor.
HIV Clinical Trials
2013 Sep-Oct14(5):192-203. doi: 10.1310/hct1405-192
Johns B.A., Kawasuji T., Weatherhead J.G., Taishi T., Temelkoff D.P., Yoshida H., Akiyama T., Taoda Y., Murai H., Kiyama R., Fuji M., Tanimoto N., Jeffrey J., Foster S.A., Yoshinaga T., Seki T., Kobayashi M., Sato A., Johnson M.N., Garvey E.P., Fujiwara T.
Carbamoyl pyridone HIV-1 integrase inhibitors 3.
A diastereomeric approach to chiral nonracemic tricyclic ring systems and the discovery of dolutegravir (S/GSK1349572) and (S/GSK1265744)
J Med Chem. 2013 Jul 2556(14):5901-16. doi: 10.1021/jm400645w. Epub 2013 Jul 11
Shaik J.S.B., Ford S.L., Lou Y., Zhang Z., Bakshi K.K., Tenorio A.R., Trezza C., Spreen W.R., Patel P.
A Phase 1 Study to Evaluate the Pharmacokinetics and Safety of Cabotegravir in Patients With Hepatic Impairment and Healthy Matched Controls.
Clinical Pharmacology Drug Development
2019 Jul8(5):664-673. doi: 10.1002/cpdd.655. Epub 2019 Feb 27
ATC classification(1 code)
ATC J05AJ04
International brands(1)
Salt forms(1)
Cabotegravir sodium(DBSALT002064)
Commercial products(17)
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)
Cabotegravir
Additional database identifiers
Drugs Product Database (DPD)
23435
ChemSpider
30829503
BindingDB
50492496
ZINC
ZINC000096927633
UniProt Accession
Q7ZJM1_HV1
GenBank Gene Database
M15654
GenBank Protein Database
326388
UniProt Accession
POL_HV1B1
HUGO Gene Nomenclature Committee (HGNC)
HGNC:12530
GeneCards
UGT1A1
GenBank Gene Database
M57899
GenBank Protein Database
184473
Guide to Pharmacology
2990
UniProt Accession
UD11_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:399
GenAtlas
ALB
GeneCards
ALB
GenBank Gene Database
V00494
GenBank Protein Database
28590
UniProt Accession
ALBU_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: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:74
GenAtlas
ABCG2
GeneCards
ABCG2
GenBank Gene Database
AF103796
GenBank Protein Database
4185796
Guide to Pharmacology
792
UniProt Accession
ABCG2_HUMAN
Patent information
8 active patents, 3 expired
12178815
United States
Approved 18 Jul 2018 · Expires 18 Jul 2038
12y 3m
11389448
United States
Approved 13 Apr 2012 · Expires 13 Apr 2032
6 years
RE50189
United States
Approved 29 Oct 2024 · Expires 27 Nov 2031
5y 7m
11224597
United States
Approved 18 Jan 2022 · Expires 15 Sept 2031
5y 5m
12138264
United States
Approved 12 Nov 2024 · Expires 15 Sept 2031
5y 5m
The earliest active patent expires April 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 30 days ago(4 Mar 2026)