Cabotegravir (GSK744, GSK1265744) - CAS 1051375-10-0
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Not Intended for Therapeutic Use. For research use only.
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HIV Integrase
Cabotegravir (GSK744, GSK1265744) is a long-acting HIV integrase inhibitor against a broad range of HIV subtypes, and inhibits the HIV-1 integrase catalyzed strand transfer reaction with IC50 of 3.0 nM. Phase 2.
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1.Cabotegravir plus rilpivirine, once a day, after induction with cabotegravir plus nucleoside reverse transcriptase inhibitors in antiretroviral-naive adults with HIV-1 infection (LATTE): a randomised, phase 2b, dose-ranging trial.
Margolis DA1, Brinson CC2, Smith GH3, de Vente J4, Hagins DP5, Eron JJ6, Griffith SK7, St Clair MH7, Stevens MC8, Williams PE8, Ford SL7, Stancil BS7, Bomar MM7, Hudson KJ7, Smith KY9, Spreen WR7; LAI116482 Study Team. Lancet Infect Dis. 2015 Oct;15(10):1145-55. doi: 10.1016/S1473-3099(15)00152-8. Epub 2015 Jul 19.
BACKGROUND: In phase 1 trials, the HIV-1 integrase strand transfer inhibitor cabotegravir (GSK1265744) was well tolerated, both alone, and in combination with the non-nucleoside reverse transcriptase inhibitor rilpivirine. We assessed cabotegravir plus rilpivirine, as a two-drug oral antiretroviral regimen, for the maintenance of viral suppression in antiretroviral-naive HIV-1-infected individuals.
2.Drug interaction profile of the HIV integrase inhibitor cabotegravir: assessment from in vitro studies and a clinical investigation with midazolam.
Reese MJ1, Bowers GD1, Humphreys JE1, Gould EP2, Ford SL2, Webster LO1, Polli JW1. Xenobiotica. 2016 May;46(5):445-56. doi: 10.3109/00498254.2015.1081993. Epub 2015 Sep 4.
1. Cabotegravir (CAB; GSK1265744) is a potent HIV integrase inhibitor in clinical development as an oral lead-in tablet and long-acting injectable for the treatment and prevention of HIV infection. 2. This work investigated if CAB was a substrate for efflux transporters, the potential for CAB to interact with drug-metabolizing enzymes and transporters to cause clinical drug interactions, and the effect of CAB on the pharmacokinetics of midazolam, a CYP3A4 probe substrate, in humans. 3. CAB is a substrate for Pgp and BCRP; however, its high intrinsic membrane permeability limits the impact of these transporters on its intestinal absorption. 4. At clinically relevant concentrations, CAB did not inhibit or induce any of the CYP or UGT enzymes evaluated in vitro and had no effect on the clinical pharmacokinetics of midazolam. 5. CAB is an inhibitor of OAT1 (IC50 0.81 µM) and OAT3 (IC50 0.41 µM) but did not or only weakly inhibited Pgp, BCRP, MRP2, MRP4, MATE1, MATE2-K, OATP1B1, OATP1B3, OCT1, OCT2 or BSEP.
3.Cabotegravir long-acting for HIV-1 prevention.
Andrews CD1, Heneine W. Curr Opin HIV AIDS. 2015 Jul;10(4):258-63. doi: 10.1097/COH.0000000000000161.
PURPOSE OF REVIEW: Preexposure prophylaxis (PrEP) with daily Truvada has demonstrated clinical efficacy against HIV-1 acquisition that correlates with high adherence. Long-acting antiretroviral drugs offer an alternative to daily regimens and may improve PrEP adherence. This review summarizes the preclinical nonhuman primate studies for evaluating the efficacy of cabotegravir long-acting as PrEP and the ongoing phase 2a studies assessing safety, tolerability, and acceptability of cabotegravir long-acting.
4.Formulation and pharmacology of long-acting cabotegravir.
Trezza C1, Ford SL, Spreen W, Pan R, Piscitelli S. Curr Opin HIV AIDS. 2015 Jul;10(4):239-45. doi: 10.1097/COH.0000000000000168.
PURPOSE OF REVIEW: Long-acting cabotegravir may provide a novel therapeutic option for both the treatment and prevention of HIV-1 infection that does not necessitate adherence to a daily regimen. The present review will highlight the unique formulation properties and pharmacologic attributes of long-acting cabotegravir nanosuspension.
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CAS 1051375-10-0 Cabotegravir (GSK744, GSK1265744)

Cabotegravir (GSK744, GSK1265744)
(CAS: 1051375-10-0)

Cabotegravir (GSK744, GSK1265744) is a long-acting HIV integrase inhibitor against a broad range of HIV subtypes, and inhibits the HIV-1 integrase catalyzed str...

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CAS 1051375-10-0 Cabotegravir (GSK744, GSK1265744)

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