Title : Impact of UGT2B17 Gene Deletion on the Pharmacokinetics of 17-Hydroexemestane in Healthy Volunteers.

Pub. Date : 2016 Jul

PMID : 26608382






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1 Impact of UGT2B17 Gene Deletion on the Pharmacokinetics of 17-Hydroexemestane in Healthy Volunteers. 17-hydroexemestane UDP glucuronosyltransferase family 2 member B17 Homo sapiens
2 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. 17-hydroexemestane UDP glucuronosyltransferase family 2 member B17 Homo sapiens
3 Previous microsomal studies have shown that UGT2B17 gene deletion affects the intrinsic hepatic clearances of 17-hydroexemestane in vitro. 17-hydroexemestane UDP glucuronosyltransferase family 2 member B17 Homo sapiens
4 In this open-label study we set out to assess the effect of UGT2B17 gene deletion on the pharmacokinetics of 17-hydroexemestane in healthy female volunteers with and without UGT2B17. 17-hydroexemestane UDP glucuronosyltransferase family 2 member B17 Homo sapiens
5 Our results showed that there were statistically significant differences in plasma 17-hydroexemestane AUC0- (P = .0007) and urine 17-hydroexemestane C24h (P = .001) between UGT2B17 genotype groups. 17-hydroexemestane UDP glucuronosyltransferase family 2 member B17 Homo sapiens
6 Our results showed that there were statistically significant differences in plasma 17-hydroexemestane AUC0- (P = .0007) and urine 17-hydroexemestane C24h (P = .001) between UGT2B17 genotype groups. 17-hydroexemestane UDP glucuronosyltransferase family 2 member B17 Homo sapiens
7 Our data suggest that UGT2B17 gene deletion influences 17-hydroexemestane pharmacokinetics in humans. 17-hydroexemestane UDP glucuronosyltransferase family 2 member B17 Homo sapiens