[Plasma concentrations of fosfestrol as well as diethylstilbestrol on their conjugates following intravenous administration on prostatic carcinoma patients].
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.
D000368:Aged; D000970:Antineoplastic Agents / Q000097:blood* / Q000627:therapeutic use; D004054:Diethylstilbestrol / Q000031:analogs & derivatives* / Q000097:blood* / Q000627:therapeutic use; D006801:Humans; D007262:Infusions, Intravenous; D007275:Injections, Intravenous; D007700:Kinetics; D008297:Male; D008875:Middle Aged; D011471:Prostatic Neoplasms / Q000097:blood* / Q000188:drug therapy
D000970:Antineoplastic Agents; D004054:Diethylstilbestrol; C004955:fosfestrol
Plasmakonzentrationen von Fosfestrol sowie von Diethylstilbestrol und seinen Konjugaten nach intravenöser Gabe an Prostatakarzinom-Patienten.