DB11751ApprovedInvestigationalSmall moleculeAnti-Retroviral AgentsHIV Integrase InhibitorsHuman Immunodeficiency Virus Integrase Strand Transfer Inhibitor
Cabotegravir is an HIV-1 integrase inhibitor used for treatment and pre-exposure prophylaxis of HIV-1 infection. Cabotegravir, or GSK1265744, is an HIV-1 integrase inhibitor that is prescribed with the non-nucleoside reverse transcriptase inhibitor, rilpivirine.
- Mechanism
- Curator reviewed · 2 references
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.
- Primary 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...Curator reviewed · 5 structured indications
- Formula / weight
- C19H17F2N3O5 · 405.358 g/mol (avg)
- First approval
- Canada, 2020 · United States, 2021 · European Union, 2021
- Code names
- 744 LA · GSK 1265744 · GSK-1265744A · GSK 744 · GSK744 LA · GSK744 LAP · S-265744 · S/GSK1265744
- Brand names
Resolves to
Clinical / RWD
Structure
InChIKey
WCWSTNLSLKSJPK-LKFCYVNXSA-NSMILES[H][C@@]12CN3C=C(C(=O)NCC4=C(F)C=C(F)C=C4)C(=O)C(O)=C3C(=O)N1[C@@H](C)CO2Targets
Transporters
What you can answer from here — as of September 23, 2026
2Protein targetsEach mapped to UniProt, with action and pharmacological actionListed above
4TransportersSubstrate / inhibitor direction, not just membershipListed above
Which drugs share a target with Cabotegravir, and which of those have an active Phase 3 trial?
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