In vitro
Elvitegravir (EVG, JTK-303/GS-9137) can inhibit HIV-1 IIIB, HIV-2 EHO and HIV-2 ROD with IC50 of 0.7 nM, 2.8 nM and 1.4 nM. Elvitegravir is predominantly metabolized via cytochrome P450 (CYP)3A4, along with minor pathways including glucuronidation via UGT1A1/3 and oxidative metabolism. Elvitegravir (EVG, JTK-303, GS-9137) currently being developed for the treatment of HIV-1 infection. Elvitegravir was more potent than raltegravir,a newly approved anti-AIDS drug. Elvitegravir can inhibit clinical HIV-2 isolates with IC50 of 0.7 nM while raltegravir inhibits those HIV-2 isolates with IC50 of 2.4 nM. Neither elvitegravir nor raltegravir could block disintegration. Elvitegravir (EVG) blocks the integration of HIV-1 cDNA through the inhibition of DNA strand transfer. Elvitegravir can inhibit the replication of HIV-1, including various subtypes and multiple-drug-resistant clinical isolates, and HIV-2 strains with a 50% effective concentration in the subnanomolar to nanomolar range. Clade-specific HIV-1 integrase polymorphisms do not reduce elvitegravir phenotypic susceptibility.
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