Cabotegravir (GSK-1265744) is a potent, selective HIV-1 integrase inhibitor with IC50 of 3 nM in biochemical integrase strand transfer assay (INST). Cabotegravir (GSK-1265744) shows IC50 of 1.3 nM in MT-4 cell assays, and a pHIV IC50 of <2 nM against the Q148K variant, IC50 of 0.2 nM in peripheral blood mononuclear cell (PBMC) HIV multiround replication assays. Cabotegravir (GSK-1265744) formulated as a long-acting (LA) injectable protects macaques from intrarectal simian/human immunodeficiency virus.
