Cabotegravir

Summary

Cabotegravir (CHEMBL2403238) is an approved small-molecule HIV-1 integrase inhibitor (ATC J05AJ04); indicated across 3 conditions including hiv infectious disease and viral infectious disease.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: J05AJ04
• Indications: 3 conditions
• Clinical trials: 46
• Chemistry: 405.4 Da · C19H17F2N3O5

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL2403238
Name	Cabotegravir
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	54713659
ChEBI	CHEBI:172944
ATC	J05AJ04
Molecular formula	C19H17F2N3O5
Molecular weight	405.4
InChIKey	WCWSTNLSLKSJPK-LKFCYVNXSA-N

SMILES: C[C@H]1CO[C@H]2N1C(=O)C3=C(C(=O)C(=CN3C2)C(=O)NCC4=C(C=C(C=C4)F)F)O

IUPAC name: (3R,6S)-N-[(2,4-difluorophenyl)methyl]-10-hydroxy-6-methyl-8,11-dioxo-4-oxa-1,7-diazatricyclo[7.4.0.03,7]trideca-9,12-diene-12-carboxamide

ChEBI definition: A monocarboxylic acid amide obtained by formal condensation of the carboxy group of (3S,11aR)-6-hydroxy-3-methyl-5,7-dioxo-2,3,5,7,11,11a-hexahydro[1,3]oxazolo[3,2-a]pyrido[1,2-d]pyrazine-8-carboxylic acid with the amino group of 2,4-difluorobenzylamine. Used (as its sodium salt) for treatment of HIV-1.

Pharmacological roles (ChEBI): HIV-1 integrase inhibitor.

Also known as: Apretude, Cabotegravir, Cabotegravir component of cabenuva, Gsk-1265744, GSK-1265744A, GSK1265744, GSK1265744A, Gsk744, GSK744, S-265744, CABOTEGRAVIR, CABOTEGRAVIR (GSK744, GSK1265744)

Parent form; salt/anhydrous children: CHEMBL3137330

Patent coverage: 504 distinct patent families (1,482 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 1,315 (89%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

No target linkage available.

Bioactivity

No ChEMBL bioactivity rows at pChembl ≥ 5 (expected for biologics / antibodies).

Target pathways

No target-pathway data for this drug (no mapped target genes).

Indications & clinical

Indications

3 indications (3 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

Indication	Trial phase	MONDO	EFO
HIV infectious disease	4	MONDO:0005109	EFO:0000764
viral infectious disease	4	MONDO:0005108	EFO:0000763

1 further indication record had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 46.

Phase distribution

Phase	Trials
PHASE1	15
Not specified	10
PHASE2	8
PHASE3	7
PHASE4	4
PHASE2/PHASE3	1
PHASE1/PHASE2	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT06854029	PHASE4	NOT_YET_RECRUITING	NOTRE: Optimizing Long-Acting Pre-Exposure Prophylaxis and Medications for Opioid Use Disorder Interventions in Carceral Settings
NCT07199335	PHASE4	RECRUITING	Long-acting Cabotegravir Injectable Pre-exposure Prophylaxis for People Who Inject Drugs
NCT05374525	PHASE4	COMPLETED	A Study Evaluating Implementation Strategies for the Delivery of Cabotegravir in Low and High-Volume PrEP Site in the United States
NCT05514509	PHASE4	COMPLETED	A Study Evaluating Implementation Strategies for the Delivery of APRETUDE for Black cis-and Transgender Women in United States EHE Territories
NCT03299049	PHASE3	ACTIVE_NOT_RECRUITING	Efficacy, Safety and Tolerability Study of Long-acting Cabotegravir Plus Long-acting Rilpivirine (CAB LA + RPV LA) in Human-immunodeficiency Virus-1 (HIV-1) Infected Adults
NCT05515770	PHASE3	RECRUITING	The Implementation of Pre-exposure Prophylaxis of Injectable Cabotegravir
NCT05546242	PHASE3	ACTIVE_NOT_RECRUITING	Improving HIV-1 Control in Africa with Long Acting Antiretrovirals
NCT06273943	PHASE3	NOT_YET_RECRUITING	Impact of Long-acting Injectable Cabotegravir for HIV PrEP in MSM in France.
NCT06507059	PHASE3	RECRUITING	Outcomes of the PLHIV With Suboptimal Viral Suppression to Injectable Long-acting Antiretrovirals
NCT02720094	PHASE2/PHASE3	COMPLETED	Injectable Cabotegravir Compared to TDF/FTC For PrEP in HIV-Uninfected Men and Transgender Women Who Have Sex With Men
NCT04542070	PHASE3	COMPLETED	A Study to Evaluate Efficacy and Safety of Cabotegravir (CAB) Long Acting (LA) Plus (+) Rilpivirine (RPV) LA Versus BIKTARVY® (BIK) in Participants With Human Immunodeficiency Virus (HIV)-1 Who Are Virologically Suppressed
NCT05154747	PHASE3	UNKNOWN	Long-Acting Treatment in Adolescents (LATA)
NCT05996471	PHASE2	ACTIVE_NOT_RECRUITING	A Study to Investigate the Virologic Efficacy and Safety of VH3810109 + Cabotegravir Compared to Standard of Care (SOC) in Male and Female Adults Living With Human Immunodeficiency Virus (HIV)
NCT06411223	PHASE2	ACTIVE_NOT_RECRUITING	Pharmacist-led Intervention for Injectable HIV Treatment for Women With Health-related Social Needs
NCT00920426	PHASE2	COMPLETED	Study to Compare the Safety and Anti-HIV Effect of GSK1265744 Versus Placebo in HIV-1 Infected Adults (ITZ112929)
NCT01641809	PHASE2	COMPLETED	Dose Ranging Study of GSK1265744 Plus Nucleoside Reverse Transcriptase Inhibitors for Induction of Human Immunodeficiency Virus-1 (HIV-1) Virologic Suppression Followed by Virologic Suppression Maintenance by GSK1265744 Plus Rilpivirine
NCT02178800	PHASE2	COMPLETED	Evaluating the Safety, Tolerability, and Pharmacokinetics of an Investigational, Injectable HIV Medicine (GSK1265744) in HIV-Uninfected Adults
NCT02462772	PHASE2	WITHDRAWN	Safety and Acceptability of Cabotegravir in HIV Uninfected Women in KwaZulu-Natal, South Africa
NCT03497676	PHASE1/PHASE2	COMPLETED	More Options for Children and Adolescents (MOCHA): Oral and Long-Acting Injectable Cabotegravir and Rilpivirine in HIV-Infected Children and Adolescents
NCT03739996	PHASE2	COMPLETED	Long-Acting Cabotegravir Plus VRC-HIVMAB075-00-AB (VRC07-523LS) for Viral Suppression in Adults Living With HIV-1
NCT04824131	PHASE2	COMPLETED	Safety, Tolerability and Acceptability of Long-Acting Cabotegravir (CAB LA) for the Prevention of HIV Among Adolescent Females
NCT05418868	PHASE1	RECRUITING	A Study to Investigate Pharmacokinetics, Safety and Tolerability of Long-Acting Cabotegravir Plus Recombinant Human Hyaluronidase PH20 in Healthy Adult Participants
NCT06970223	PHASE1	ACTIVE_NOT_RECRUITING	A Study to Investigate if Long Acting Cabotegravir (CAB) and Lenacapavir (LEN) Injections Are Tolerable and Acceptable When Administered to Healthy Adults Without HIV
NCT00659191	PHASE1	COMPLETED	A Healthy Volunteer And Patient Study To Assess The Safety, Tolerability And Pharmacokinetics Of GSK1265744
NCT00920296	PHASE1	COMPLETED	DDI Study of Etravirine and GSK1265744
NCT01467531	PHASE1	COMPLETED	A Study to Evaluate the Pharmacokinetics and Safety of GSK1265744 and Rilpivirine and Dolutegravir and Rilpivirine in Healthy Adult Subjects
NCT01593046	PHASE1	COMPLETED	A Study to Investigate the Safety, Tolerability and Pharmacokinetics of Repeat Dose Administration of Long-Acting GSK1265744 and Long-Acting TMC278 Intramuscular and Subcutaneous Injections in Healthy Adult Subjects
NCT01648257	PHASE1	COMPLETED	Relative Bioavailability Study of GSK1265744 Formulations
NCT02027454	PHASE1	COMPLETED	Study to Evaluate the Effect of GSK1265744 on Cardiac Conduction
NCT02159131	PHASE1	COMPLETED	Study to Evaluate the Pharmacokinetics of an Oral Contraceptive Containing Levonorgestrel and Ethinyl Estradiol When Co-administered With GSK1265744 in Healthy Adult Female Subjects
NCT02354937	PHASE1	COMPLETED	Pharmacokinetics Study of GSK1265744 in Subjects With Severe Renal Impairment
NCT02354950	PHASE1	COMPLETED	A Study to Evaluate Pharmacokinetic (PK) and Safety of GSK1265744 in Subjects With Hepatic Impairment and Control Healthy Volunteers
NCT02799264	PHASE1	COMPLETED	A Study to Evaluate the Effect of High Fat Meal on Cabotegravir
NCT03149848	PHASE1	COMPLETED	Effect of Rifabutin on the Pharmacokinetics of Oral Cabotegravir in Healthy Subjects
NCT04371380	PHASE1	COMPLETED	Pharmacokinetic Study of Cabotegravir and Rilpivirine Long-acting Intramuscular Injections in Healthy Adult Participants
NCT04484337	PHASE1	COMPLETED	Study to Evaluate Pharmacokinetic (PK), Safety and Tolerability of Cabotegravir (CAB) 400 Milligrams Per Milliliter (mg/mL) Formulation in Healthy Adult Participants
NCT03462810	Not specified	AVAILABLE	GSK1265744 (Cabotegravir, CAB) for Named Patient/Compassionate Use in HIV
NCT05044962	Not specified	RECRUITING	Kuwa Free! - Live Free!
NCT05663580	Not specified	RECRUITING	Cohort Study of HIV-positive People, Treated With Long Acting Antiretroviral Therapy
NCT06403865	Not specified	NOT_YET_RECRUITING	Patient-Reported Outcomes in Real-life of Cabotegravir and Rilpivirine

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline or drug-level clinical/variant annotations in PharmGKB for this molecule.

Related molecules

Related molecules

No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).