Metabolites of Tamoxifen as the Basis of Drug Development

摘要: By the early 1970s, a number of metabolites tamoxifen had been identified in animals and following administration to few patients. The hydroxylated metabolite tamoxifen, 4-hydroxytamoxifen, proved be most interesting. discovery its high binding affinity for estrogen receptor made it new laboratory tool all future vitro studies antiestrogen action also provided clue structure-function relationships antiestrogens. These compounds would subsequently developed as selective modulators (SERMs). Tamoxifen is prodrug but 4-hydroxy-N-desmethyltamoxifen or endoxifen that has attracted pharmacogenetic interest. Mutations CYP2D6 gene control production have associated with drug efficacy some clinical trials.