[CAS NO. 635728-49-3]  Darunavir Ethanolate

Darunavir displays potent activity against HIV strains resistant to other available protease inhibitor. Darunavir inhibits P-glycoprotein-mediated efflux of calcein-acetoxymethyl ester in L-MDR1 cells with the inhibitory potency of 121 mM. Darunavir is a protein inhibits that mimics the phenylalanine sequences at positions 167 and 168 of the gag-pol polypeptide and binds to the active sites of the HIV protease, thereby inhibiting its activity. Darunavir blocks the infectivity and replication of each of the HIV-1 variants at concentrations up to 5 μM. Darunavir shows strong ARV activity against a selected panel of 19 recombinant clinical isolates carrying multiple protease mutations conferring resistance to an average of five other protien inhibitors. Darunavir inhibits 75% of 1501 PI-resistant viruses tested with a half maximal effective concentration (EC50) of < 10 nM.