Inaba T, Fischer N E, Riddick D S, Stewart D J, Hidaka T
Department of Pharmacology, Faculty of Medicine, University of Toronto, Canada.
Toxicol Lett. 1997 Dec;93(2-3):215-9. doi: 10.1016/s0378-4274(97)00098-2.
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.
蛋白酶抑制剂利托那韦、茚地那韦和沙奎那韦是迄今为止研发出的最有效的抗HIV药物，它们通过与细胞色素P450 3A4（CYP3A4）竞争，与许多药物相互作用，CYP3A4是多种化合物代谢的关键酶。使用人肝微粒体来比较这三种蛋白酶抑制剂的抑制作用。利托那韦和茚地那韦的抑制作用最强，而沙奎那韦的抑制作用较弱。
