Cabotegravir sodium (GSK-1265744) is an orally active, membrane-permeable HIV integrase inhibitor (IC₅₀ = 2.5 μM) and also an OAT1/OAT3 inhibitor (IC₅₀ = 0.81/0.41 μM). It inhibits HIV replication and may be used in AIDS research.

OAT1:0.81 μM, HIV (ADA):2.5 nM, OAT3:0.41 μM

In vitro experiments demonstrated that Cabotegravir sodium inhibits the strand transfer reaction catalyzed by HIV-1 integrase, with a half-maximal inhibitory concentration (IC₅₀) of 3.0 nM. In PBMCs (peripheral blood mononuclear cells), the drug exhibited antiviral half-maximal effective concentrations (EC₅₀) of 0.22 nM against the HIV-1 Ba-L strain and 0.34 nM against the NL432 strain. In MT-4 cells, EC₅₀ values were determined as 0.57 nM by the CellTiter-Glo method and 1.3 nM by the MTT method, while the EC₅₀ measured in the pseudotyped self-inactivating virus PHIV assay was 0.5 nM [3].

The half-life of Cabotegravir sodium in mice is 54 days, demonstrating a prolonged duration [1].
Cabotegravir (25 or 50 mg/kg, administered intravenously as a single or double dose) can protect Macaca mulatta (macaques) from SIVmac251 virus infection [4].