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

Elvitegravir抑制MLV感染的复制,IC50为5.8 nM,也抑制灵长类动物的逆转录病毒SIV,IC50为0.5 nM,说明IN抑制剂具有抗多种逆转录病毒的活性。Elvitegravir 抑制整合酶活性,IC50为 6 nM。Elvitegravir 抑制PBMC和PA,IC50 分别为0.89和20 nM。Elvitegravir抑制链转移产物的合成,IC50为54 nM。Elvitegravir通过抑制IN-调节的链转移而抑制整合。EVG具有无血清抗病毒活性,IC50为0.3-0.9 nM,作用于外周血单个核细胞,有效作用于HIV-1和 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].