Estramustine phosphate: metabolic aspects related to its action in prostatic cancer.
Estramustine phosphate, a drug effective in a substantial number of patients with cancer of the prostate who had failed on other forms of therapy, has been shown to be split into its constituents, that is estradiol-17beta 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 we discuss the limitations of extrapolating animal results with estramustine phosphate to the human condition and possible parameters that bear upon the insignificant toxic and estrogenic effects observed in patients given estramustine phosphate.
D000230:Adenocarcinoma / Q000188:drug therapy; D000818:Animals; D002219:Carbamates / Q000378:metabolism / Q000627:therapeutic use; D046508:Culture Techniques; D004958:Estradiol / Q000031:analogs & derivatives / Q000378:metabolism; D004961:Estramustine / Q000378:metabolism* / Q000494:pharmacology / Q000627:therapeutic use; D006801:Humans; D006868:Hydrolysis; D008297:Male; D009588:Nitrogen Mustard Compounds / Q000009:adverse effects / Q000378:metabolism* / Q000627:therapeutic use; D011467:Prostate / Q000378:metabolism; D011471:Prostatic Neoplasms / Q000188:drug therapy / Q000378:metabolism*; D011960:Receptors, Estrogen
D002219:Carbamates; D009588:Nitrogen Mustard Compounds; D011960:Receptors, Estrogen; D004961:Estramustine; D004958:Estradiol