Metabolism and metabolite profiles in vitro and in vivo of ospemifene in humans and preclinical species.

BACKGROUND Metabolite profiles of ospemifene, a novel nonsteroidal selective estrogen receptor modulator, were surveyed as part of its development. METHODS The pharmacokinetics of ospemifene and its two major, pharmacologically active metabolites 4-hydroxyospemifene and 4'-hydroxyospemifene, was elucidated in studies of volunteer humans given various… (More)