| Elvitegravir is an integrase inhibitor. Elvitegravir is predominantly metabolized via cytochrome P450 (CYP)3A4, along with minor pathways including glucuronidation via UGT1A1/3 and oxidative metabolism. Elvitegravir is metabolized into M1 and M4 (elvitegravir hydroxide and elvitegravir glucuronide) which have been shown to inhibit HIV-1 integrase in vitro.[1] Elvitegravir inhibits HIV-1IIIB, HIV-2EHO and HIV-2ROD with EC50 of 0.7, 2.8 an 1.4 nM, respectively. Elvitegravir suppresses the replication of all HIV-1 subtypes tested, with an antiviral EC50 ranging from 0.10 to 1.26 nM. Elvitegravir inhibits the synthesis of strand transfer products with IC50 values of 54 nM. Elvitegravir blocks the integration of HIV-1 cDNA through the inhibition of DNA strand transfer. Elvitegravir inhibits 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. Elvitegravir exerts potent anti-HIV activity against not only wild-type strains but also drug-resistant clinical isolates. Importantly, elvitegravir reveals antiviral activity against murine leukemia virus (MLV) and simian immunodeficiency virus (SIV).[2] The coadministration of elvitegravir with the protease inhibitor ritonavir (a substantial CYP3A4 inhibitor) results in significantly enhanced bioavailability and a longer half-life than with elvitegravir alone, allowing for the once-daily dosing of elvitegravir.[3] |
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