Estramustine Phosphate: Metabolic Aspects Related to Its Action in Prostatic Cancer

Abstract

Estramustine phosphate, a drug effective in a substantial number of patients with cancer of the prostate who had failed on other forms of therapy, was split into its constituents, that is estradiol-17.beta. and the carbamate nitrogen mustard by non-cancerous and cancerous human prostatic tissues. This fact may explain, in part, the mechanism of action and efficacy of the drug in patients with cancer of the prostate. In addition to presenting results on the hydrolysis and its products accomplished by human prostatic tissues, the limitations of extrapolating animal results with estramustine phosphate to the human condition and possible parameters that bear on the insignificant toxic and estrogenic effects observed in patients given estramustine phosphate were discussed.