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 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.
Taiwo
Babafemi O
BO
Division of Infectious Diseases, Northwestern University, Feinberg School of Medicine, Chicago, Illinois, USA.
Hicks
Charles B
CB
D002986:Clinical Trials as Topic; D000069454:Darunavir; D004347:Drug Interactions; D024882:Drug Resistance, Viral; D017320:HIV Protease Inhibitors / Q000009:adverse effects / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use*; D006801:Humans; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000009:adverse effects / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use*; D013607:Tablets
D017320:HIV Protease Inhibitors; D013449:Sulfonamides; D013607:Tablets; D000069454:Darunavir