Clinical Medicine Reviews in Therapeutics

Darunavir is a next-generation protease inhibitor that demonstrates potent in vitro activity against wild type strains of HIV type-1, as well as against numerous strains resistant to available protease inhibitors. Numerous trials conducted in naïve and in the treatment-experienced HIV-infected individuals have significantly demonstrated greater virological suppression when darunavir was added to an optimized background treatment compared with a control protease inhibitors. The drug is taken as two 400 mg tablets once daily plus 100 mg of ritonavir in naïve patients, while is taken as two 300 mg tablets plus 100 mg of ritonavir twice daily in experienced patients. Darunavir has a high genetic barrier and has a distinct resistance profile. Darunavir resistance associated mutations have been defined as V11I, V32I, L33F, I47V, I50V, I54L/M, T74P, L76V, I84V, and L89V. The major adverse effects of darunavir therapy are nausea, diarrhea and rash; and as others protease inhibitors, increase of triglycerides and total cholesterol.