Impact of UGT2B17 Gene Deletion on the Pharmacokinetics of 17-Hydroexemestane in Healthy Volunteers.
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ABSTRACT:
SUBMITTER: Chen SM
PROVIDER: S-EPMC4882280 | biostudies-literature | 2016 Jul
REPOSITORIES: biostudies-literature
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Impact of UGT2B17 Gene Deletion on the Pharmacokinetics of 17-Hydroexemestane in Healthy Volunteers.
Chen Shanly M SM Atchley Daniel H DH Murphy Michael A MA Gurley Bill J BJ Kamdem Landry K LK
Journal of clinical pharmacology 20151231 7
Exemestane is an aromatase inhibitor drug used for the treatment of hormone-dependent breast cancer. 17-Hydroexemestane, the major and biologically active metabolite of exemestane in humans, is eliminated via glucuronidation by the polymorphic UGT2B17 phase II drug-metabolizing enzyme. Previous microsomal studies have shown that UGT2B17 gene deletion affects the intrinsic hepatic clearances of 17-hydroexemestane in vitro. In this open-label study we set out to assess the effect of UGT2B17 gene d ...[more]
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