S/GSK1349572 inhibits recombinant HIV-1 integrase-catalyzed strand transfer in vitro. S/GSK1349572 potently inhibits HIV replication in cells infected with a self-inactivating PHIV lentiviral vector, such as peripheral blood mononuclear cells (PBMCs), MT-4 cells and CIP4. S/GSK1349572 exhibits potent activity against five different nonnucleoside reverse transcription inhibitor--resistant or nucleoside reverse transcription inhibitor--resistant viruses in vitro. S/GSK1349572 shows equivalent activity against two protease inhibitor-resistant viruses similarly to that against wild-type virus.