After the identification of E-diethylstilbestrol (DES)-glucuronide-sulphate-bis-conjugate in the plasma of patients suffering from metastatic prostatic cancer for the first time we have registered the plasma concentration-time curves of fosfestrol (Honvan) and its monophosphate as well as E-DES and its 3 conjugates over 8 h with a further 10 patients. Maximum concentrations fluctuate between 1 and 32 micrograms/ml plasma. Therefore the greatest amount of E-DES formed by hydrolysis and its conjugates are hidden in deeper compartments, probably in the lung. The oxidative metabolism of E-DES compared with its conjugation reactions is less important. Only E-DES monoglucuronide and small amounts of E-DES-glucuronide-sulphate-bis-conjugate are detectable in urine. Renal excretion of those metabolites which are in the enterohepatic circle in form of E-DES-glucuronide and E-DES-glucuronide-sulphate-bis-conjugate could be observed even over a period of 72 h.

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