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

► We examined in vitro bioactivation of bazedoxifene and N-dealkylated fragment of bazedoxifene in HLM and with P450 isozymes. ► Bazedoxifene was not bioactivated under either conditions. ► An improved safety profile of bazedoxifene to available SERMs was discussed.