Darunavir Ethanolate (TMC114), a phenylalanine mimic, is a potent inhibitor of HIV-1 protease with EC50 activity against the wild type IIIB strain of 4 nM and an average EC50 activity against mutant protease inhibitor strains M1-M5 of 5 nM. [1] Furthermore, fof 150 protease inhibitor-resistant viruses tested, 75% were inhibited by darunavir with a EC50 of
Darunavir exhibits no cytotoxicity at concentrations up to 100 uM and has been shown to be synergistic with a variety of other protease inhibitors and reverse transcriptase inhibitors. [3]