Estramustine revisited.

Abstract

Estramustine phosphate (Emcyt, Estracyt, estradiol-3-bis (2 chloroethyl) carbamate-17-dihydrogen monophosphate), synthesized in the 1960s [1], was designed and developed for the treatment of breast cancer following the observation of the presence of estrogen receptors in normal breast tissue and tumors [2]. The design of the drug was based on the hypothesis that conjugation of 17-B estradiol with the alkylating agent nor-nitrogen mustard would allow the transport of the cytotoxic agent directly to the steroiddependent tumor cells by virtue of binding to estrogen receptors. This mechanism would then result in improved specificity for the target cells, and at the same time, reduce bone marrow and liver toxicity [3]. The concept leading to synthesis of estramustine phosphate was also based on the beneficial effect observed in prostate cancer of a polyestrodiol phosphate (Estradurin) [4].KeywordsProstate CancerMetastatic Prostate CancerCyproterone AcetateNitrogen MustardLHRH AgonistThese keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.