ABSORPTION, METABOLISM, AND EXCRETION OF ESTRACYT (NSC 89199) IN PATIENTS WITH PROSTATIC CANCER

  • 1 January 1976
    • journal article
    • research article
    • Vol. 14  (2) , 128-131
Abstract
Estramustine phosphate (estradiol, 3-N-[bis(2-chloroethyl)-] carbamate-17.beta.-dihydrogenphosphate (Estracyt) labeled with 3H in the estradiol moiety and 14C in the carbamate moiety was synthesized, and its absorption, metabolism and excretion were studied after oral administration to 3 patients with prostatic carcinoma. One of the patients was also given the same dose by i.v. injection. In addition to monitoring isotope levels in peripheral blood, urine and feces, samples of portal vein blood were obtained through a catheter in the umbilical vein. Analyses of portal blood samples revealed that most of the estramustine phosphate was dephosphorylated to estramustine during absorption. Estramustine was the major metabolite in peripheral blood after oral and i.v. administration. The urinary excretion data appeared to warrant the conclusion that most of the carbamate ester of estramustine is hydrolyzed before it is excreted. In the patient given estramustine phosphate by both routes absorption of the compound when given by mouth was .apprx. 75%.

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