GSK1265744 (Cabotegravir) is a potent inhibitor of HIV-1 clinical isolates (47.0 (triple RAMs); 9.5 (double RAMs); 3.3 (single RAMs)), OAT1 (0.81 µM), OAT3 (0.41 µM). GSK1265744 (Cabotegravir) exhibits the greatest inhibitory potency toward OAT3 (IC50 = 410 nM).