期刊
DRUG METABOLISM REVIEWS
卷 42, 期 1, 页码 196-208出版社
TAYLOR & FRANCIS LTD
DOI: 10.3109/03602530903210716
关键词
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资金
- National Health and Medical Research Council of Australia
- Pfizer Global Research
Major advances in the characterization of uridine diphosphate (UDP)-glucuronosyltransferase (UGT) enzyme substrate and inhibitor selectivities and the development of experimental paradigms to investigate xenobiotic glucuronidation in vitro now permit the prediction of a range of drug-glucuronidation parameters in humans. In particular, the availability of substrate and inhibitor probes for the major hepatic drug metabolizing UGTs together with batteries of recombinant enzymes allow the reaction phenotyping of drug glucuronidation reactions. Additionally, in vitro experimental approaches and scaling strategies have been successfully applied to the quantitative prediction of in vivo clearance via glucuronidation and drug-drug interaction potential.
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