HIV protease inhibitor
- Virions are made but stay immature and noninfectious
- Blocks cleavage of viral polyprotein
- High genetic barrier to resistance (darunavir, lopinavir)
- Lipodystrophy and insulin resistance of older agents are off-target host effects, not protease inhibition
- Potent CYP3A4 inhibition drives extensive drug interactions
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.
Self-check
- Are virions still produced during HIV protease inhibition?
Yes, but they remain immature and noninfectious. - What drives extensive drug interactions with HIV protease inhibitors?
Potent CYP3A4 inhibition.
All mechanisms · Open HIV protease inhibitor in the interactive console ↗