Cabotegravir is a potent HIV integrase inhibitor as an oral lead-in tablet and long-acting injectable for the treatment and prevention of HIV infection. Cabotegravir is an inhibitor of OAT1 (IC50 0.81 μM) and OAT3 (IC50 0.41 μM).
Cabotegravir (GSK-1265744) operates as an orally available, long-acting inhibitor of the HIV integrase strand transfer and the organic anion transporters 1 and 3 (OAT1/OAT3), with IC50s of 2.5 nM for HIVADA, 0.41 μM for OAT3, and 0.81 μM for OAT1. Its metabolism is mainly via the uridine diphosphate glucuronosyltransferase (UGT) 1A1, presenting minimal interaction risks with other antiretroviral drugs (ARVs), making it suitable for AIDS researc[1].[2].
体内研究
Cabotegravir administered intravenously at doses of either 25 or 50 mg/kg, once or twice, effectively shields Macaques from an intravenous SIVmac251 challenge[4].
体外研究
Cabotegravir (GSK-1265744) inhibits the HIV-1 integrase catalyzed strand transfer reaction with an IC50 of 3.0 nM in vitro.It shows antiviral activity with EC50 values ranging from 0.22 nM to 1.3 nM against various HIV-1 strains in different cellular assays. Additionally, it effectively shields Macaques from intravenous SIVmac251 challenges when administered as a single or double dose of 25 or 50 mg/kg intravenously[3].
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