In vitro bioactivation of bazedoxifene and 2-(4-hydroxyphenyl)-3-methyl-1H-indol-5-ol in human liver microsomes

TT Lušin, T Tomašić, J Trontelj, A Mrhar…

Index: Lusin, Tina Trdan; Tomasic, Tihomir; Trontelj, Jurij; Mrhar, Ales; Peterlin-Masic, Lucija Chemico-Biological Interactions, 2012 , vol. 197, # 1 p. 8 - 15

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Citation Number: 6

Abstract

Bazedoxifene is a selective estrogen receptor modulator (SERM) that has been developed for use in post-menopausal osteoporosis. However, it contains a potentially toxic 5-hydroxy- 3-methylindole moiety. Previous studies on the 5-hydroxyindole and the 3-alkylindole- containing drugs indometacine, zafirlukast and MK-0524 structural analogs have shown that they are bioactivated by cytochrome P450s through a dehydrogenation process to form ...