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- Title
Effects of cytochrome P450 3A (CYP3A) and the drug transporters P-glycoprotein (MDR1/ABCB1) and MRP2 (ABCC2) on the pharmacokinetics of lopinavir.
- Authors
van Waterschoot, R A B; ter Heine, R; Wagenaar, E; van der Kruijssen, C M M; Rooswinkel, R W; Huitema, A D R; Beijnen, J H; Schinkel, A H
- Abstract
Lopinavir is extensively metabolized by cytochrome P450 3A (CYP3A) and is considered to be a substrate for the drug transporters ABCB1 (P-glycoprotein) and ABCC2 (MRP2). Here, we have assessed the individual and combined effects of CYP3A, ABCB1 and ABCC2 on the pharmacokinetics of lopinavir and the relative importance of intestinal and hepatic metabolism. We also evaluated whether ritonavir increases lopinavir oral bioavailability by inhibition of CYP3A, ABCB1 and/or ABCC2.
- Publication
British journal of pharmacology, 2010, Vol 160, Issue 5, p1224
- ISSN
1476-5381
- Publication type
Journal Article
- DOI
10.1111/j.1476-5381.2010.00759.x