HIV protease inhibitor
- Virions are made but stay immature and noninfectious
- High genetic barrier to resistance (darunavir, lopinavir)
- Lipodystrophy and insulin resistance of older agents are off-target host effects, not protease inhibition
- Blocks cleavage of viral polyprotein — non-infectious virions
- Potent CYP3A4 inhibition drives extensive drug interactions
- Metabolic effects (dyslipidemia, lipodystrophy) are off-target host effects of older agents, not protease inhibition
Drugs with this mechanism (7)
- Atazanavir — HIV protease inhibitor; causes benign indirect hyperbilirubinemia.
- Darunavir — HIV protease inhibitor with a high genetic barrier; boosted with ritonavir.
- Indinavir — Early HIV protease inhibitor; nephrolithiasis.
- Lopinavir — HIV protease inhibitor always co-formulated with ritonavir.
- Nelfinavir — Early HIV protease inhibitor.
- Ritonavir — HIV protease inhibitor used mainly as a potent CYP3A "booster".
- Saquinavir — The first HIV protease inhibitor.
All mechanisms · Open HIV protease inhibitor in the interactive console ↗