Cabotegravir is an inhibitor of HIV-1 integrase (IC50 = 3 nM in a strand transfer assay).1 It inhibits HIV replication in MT-4 cells and peripheral blood mononuclear cells (PBMCs; IC50s = 1.3 and 0.2 nM, respectively). Cabotegravir (50 mg/kg) is protective against simian/human immunodeficiency virus (SHIV) infection in macaques when administered 1 week prior to viral challenge.2
1.Johns, B.A., Kawasuji, T., Weatherhead, J.G., et al.Carbamoyl pyridone HIV-1 integrase inhibitors 3. A diastereomeric approach to chiral nonracemic tricyclic ring systems and the discovery of dolutegravir (S/GSK1349572) and (S/GSK1265744).J. Med. Chem.56(14)5901-5916(2013) 2.Andrews, C.D., Spreen, W.R., Mohri, H., et al.Long-acting integrase inhibitor protects macaques from intrarectal simian/human immunodeficiency virusScience343(6175)1151-1154(2014)