Darunavir: an overview of an HIV protease inhibitor developed to overcome drug resistance
Taiwo, B.O.; Hicks, C.B.
Aids Reader 17(3): 151-156; 159-161
2007
ISSN/ISBN: 1053-0894 PMID: 17396332 Document Number: 605615
Darunavir (TMC114) is a second-generation, sulfonamide, nonpeptidic protease inhibitor (PI) with a unique, flexible, 3-dimensional structure that contributes to it 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.