HIV protease inhibitors, saquinavir, indinavir and ritonavir: inhibition of CYP3A4-mediated metabolism of testosterone and benzoxazinorifamycin, KRM-1648, in human liver microsomes.

Article Details

Citation

Inaba T, Fischer NE, Riddick DS, Stewart DJ, Hidaka T

HIV protease inhibitors, saquinavir, indinavir and ritonavir: inhibition of CYP3A4-mediated metabolism of testosterone and benzoxazinorifamycin, KRM-1648, in human liver microsomes.

Toxicol Lett. 1997 Dec;93(2-3):215-9. doi: 10.1016/s0378-4274(97)00098-2.

PubMed ID
9486958 [ View in PubMed
]
Abstract

The protease inhibitors, ritonavir, indinavir and saquinavir, the most potent anti-HIV drugs developed to date, interact with many drugs by competing for CYP3A4, an enzyme central to the metabolism of a wide variety of compounds. Human liver microsomes were used to compare inhibition by these three protease inhibitors. The inhibition was the greatest with ritonavir and indinavir and less potent with saquinavir.

DrugBank Data that Cites this Article

Drug Enzymes
DrugEnzymeKindOrganismPharmacological ActionActions
IndinavirCytochrome P450 3A4ProteinHumans
Unknown
Substrate
Inhibitor
Details
Drug Interactions
DrugsInteraction
Colchicine
Indinavir
The serum concentration of Colchicine can be increased when it is combined with Indinavir.
Voriconazole
Amprenavir
The serum concentration of Voriconazole can be increased when it is combined with Amprenavir.
Voriconazole
Fosamprenavir
The serum concentration of Voriconazole can be increased when it is combined with Fosamprenavir.
Voriconazole
Tipranavir
The serum concentration of Voriconazole can be increased when it is combined with Tipranavir.
Voriconazole
Asunaprevir
The serum concentration of Voriconazole can be increased when it is combined with Asunaprevir.