

Fulvestrant, the First SERD. In the 1980s, a series of steroidal 7α-alkylamide analogs of 17β-estradiol were developed that had pure antagonist actions at the ER, in contrast to tamoxifen which has mixed ER agonist and antagonist actions.3 The lead compound in this series was ICI 164,384 which achieved 89% ligand-ER binding …





The molecular pharmacology of SERDs in the setting of tamoxifen resistance. Upon binding tamoxifen ERα undergoes a specific conformational change that enables the presentation of protein-protein interaction surfaces for which in tamoxifen sensitive cells there are no compatible coregulators. Thus, tamoxifen binding commits ER down a "non ...





















SERDs are currently considered the effective therapy for treating ER+ breast cancer, as these are proficient in reducing and blocking ER signalling in early and advanced drug-resistant cases. This review seeks to outline the continuous development of novel oral SERDs from a practical therapeutic perspective and to make it easier to comprehend ...
























