Elvitegravir (JTK-303) is a Human Immunodeficiency Virus Integrase Strand Transfer Inhibitor. The mechanism of action of elvitegravir is as an HIV Integrase Inhibitor, and Cytochrome P450 2C9 Inducer.

HIV-2 (ROD):1.4 nM, HIV-1 (IIIB):0.7 nM, HIV-2 (EHO):2.8 nM

Elvitegravir inhibits the replication of MLV infection with an IC50 of 5.8 nM and also suppresses the primate retrovirus SIV with an IC50 of 0.5 nM, demonstrating its activity against multiple retroviruses due to IN inhibitor properties. It inhibits integrase activity with an IC50 of 6 nM and affects PBMC and PA with IC50 values of 0.89 nM and 20 nM, respectively. Additionally, Elvitegravir blocks the synthesis of chain transfer products with an IC50 of 54 nM by inhibiting integration via IN-regulated chain transfer. EVG exhibits antiviral activity without serum, with IC50 values ranging from 0.3 to 0.9 nM, targeting peripheral blood mononuclear cells and effectively inhibiting HIV-1 and HIV-2.

Elvitegravir (EVG) is prepared in DMSO and stored, and then diluted with appropriate medium before use[1]. MT-2 cells (2×105 cells) are infected with HIV-1 IIIB and then cultured in the presence of 0.5 nM or 0.1 nM Elvitegravir. Cultures are incubated at 37°C until an extensive cytopathic effect (CPE) is observed, and the culture supernatant is then harvested for further passage in fresh MT-2 cells. The concentration of Elvitegravir is increased when a significant CPE is observed. At the indicated passages, proviral DNA is extracted from infected MT-2 cells and then subjected to PCR, followed by direct population-based sequencing. Susceptibility to Elvitegravir at the indicated passages is determined using the MAGI assay or p24 production[1].