Darunavir: An overview of an HIV protease inhibitor developed to overcome drug resistance

Darunavir (TMC114) is a second-generation, sulfonamide, nonpeptidic protease inhibitor (PI) with a unique, flexible, 3-dimensional structure that contributes to its high potency and slow selection of resistant virus. Darunavir has to be coadministered with low-dose ritonavir and food to optimize its pharmacokinetics. Ritonavir-boosted darunavir is effective in many heavily pretreated patients, including those with multiple PI resistance mutations. In vitro, the coexistence of numerous PI mutations was required for its virological potency to be significantly reduced. Preliminary findings suggest that it is active against some tipranavir-resistant strains.