Cabotegravir

Cabotegravir (GSK-1265744) is a orally active and long-acting HIV integrase strand transfer inhibitor and organic anion transporter 1/3 (OAT1/OAT3) inhibitor with IC₅₀ values of 2.5 nM, 0.41 μM and 0.81 μM for HIV_ADA, OAT3 and OAT1, respectively. Cabotegravir is primarily metabolized by uridine diphosphate glucuronosyltransferase (UGT) 1A1, with low potential to interact with other antiretroviral drugs (ARVs). Cabotegravir can be used to research AIDS^[1][2]. IC50 & Target:IC₅₀: 2.5 nM (HIV_ADA)^[1]
IC₅₀: 0.41 μM (OAT3), 0.81 μM (OAT1)^[2] In Vitro: Cabotegravir (GSK-1265744) inhibits the HIV-1 integrase catalyzed strand transfer reaction with an IC₅₀ of 3.0 nM in vitro. The antiviral EC₅₀ against HIV-1 Ba-L is 0.22 nM and that against NL432 is 0.34 nM in PBMCs, 0.57 nM using CellTiter-Glo and 1.3 nM using MTT in MT-4, and 0.5 nM in the PHIV assay, which uses a pseudotyped self-inactivating virus^[3]. In Vivo: The half-life of Cabotegravir is up to 54 days in mice^[1].
Cabotegravir (25 or 50 mg/kg; i.v.; single dose or twice) protects Macaques against intravenous challenge with SIVmac251^[4].