Fosfestrol, sold under the brand nameHonvan and also known asdiethylstilbestrol diphosphate (DESDP), is anestrogen medication which is used in the treatment ofprostate cancer in men.[1][2][3] It is given by slowintravenous infusion once per day to once per week orby mouth once per day.[3][2]
Fosfestrol was patented in 1941 and was introduced for medical use in 1955.[6] It was previously marketed widely throughout the world, but now remains available in only a few countries.[7][8][6][3]
Fosfestrol sodium is given at a dosage of 600 to 1200 mg/day by slowintravenous infusion over a period of 1 hour for a treatment duration of 5 to 10 days in men with prostate cancer.[3][2] Following this, it is given at a dose of 300 mg/day for 10 to 20 days.[3] Maintenance doses of fosfestrol sodium of 300 to 600 mg may be given four times per week.[3] This may be gradually reduced to one 300 to 600-mg dose per week over a period of several months.[3]
Fosfestrol sodium is also used to a lesser extent byoral administration initially at a dosage of 360 to 480 mg three times per day in the treatment of prostate cancer.[3][2] Maintenance doses of 120 to 240 mg three times per day may be used and can be gradually reduced to 240 mg/day.[3][2]
Testosterone levels with no treatment and with various estrogens in men with prostate cancer.[11] Determinations were made with an earlyradioimmunoassay (RIA).[11] Source was Shearer et al. (1973).[11]
Fosfestrol is provided both as thefree base and as atetrasodium salt.[2][3] In terms of dose equivalence, 300 mg anhydrous fosfestrol sodium is equal to about 250 mg fosfestrol.[3]
Fosfestrol was firstpatented in 1941 and was mentioned in the literature by Huggins.[6][22]Conjugated estrogens anddiethylstilbestrol sulfate, which arewater-soluble estrogens, were first reported to be effective in the treatment of prostate cancer viaintravenous administration in 1952.[23][22] Starting in October 1952, Flocks and colleagues studied intravenous fosfestrol in the treatment of prostate cancer, publishing their findings in 1955.[22] Fosfestrol was first introduced for medical use in 1955 under the brand names Stilphostrol and ST 52 in theUnited States andFrance, respectively.[6]
Fosfestrol is thegeneric name of the drug and itsINNTooltip International Nonproprietary Name,BANTooltip British Approved Name, andJANTooltip Japanese Accepted Name, whilediethylstilbestrol diphosphate is itsUSANTooltip United States Adopted Name andfosfestrolo is itsDCITTooltip Denominazione Comune Italiana.[15][7][8][3] It is also known asstilbestrol diphosphate.[15][7][8]Fosfestrol sodium is itsINNMTooltip International Nonproprietary Name andBANMTooltip British Approved Name.[15][7][8][3]
Brand names of fosfestrol include Cytonal, Difostilben, Honovan, Honvan, Honvol, Honvon, Fosfostilben, Fostrolin, ST 52, Stilbetin, Stilbol, Stilbostatin, Stilphostrol, and Vagestrol, among others.[15][7][8][6]
^abcShearer RJ, Hendry WF, Sommerville IF, Fergusson JD (December 1973). "Plasma testosterone: an accurate monitor of hormone treatment in prostatic cancer".British Journal of Urology.45 (6):668–677.doi:10.1111/j.1464-410x.1973.tb12238.x.PMID4359746.
^Tunn UW, Senge T, Neumann F (1981). "Effekt von Diäthylstilböstroldiphosphat auf die Serumkonzentration von Testosteron und Luteinisierungshormon beim M1-Prostatakarzinom".Verhandlungsbericht der Deutschen Gesellschaft für Urologie. Vol. 32. pp. 447–449.doi:10.1007/978-3-642-81706-9_133.ISBN978-3-540-11017-0.ISSN0070-413X.
^Oelschläger H, Rothley D, Dunzendorfer U (1988). "New Results on the Pharmacokinetics of Fosfestrol".Urologia Internationalis.43 (1):15–23.doi:10.1159/000281427.ISSN1423-0399.
^Bengtsson G, Ullberg S, Perklev T (August 1963). "Autoradiographic Distribution Studies after Administration of a Macromolecular Synthetic Oestrogen (14C-Polydiethylstilboestrol Phosphate)".Acta Endocrinologica.43 (4):571–580.doi:10.1530/acta.0.0430571.PMID14059878.
^Perklev T (November 1964). "Distribution and Excretion of Radioactivity after Parenteral Administration of Radioactive Polydiethylstilbestrol Phosphate to Rats and a Cow".Proceedings of the Society for Experimental Biology and Medicine.117 (2):394–398.doi:10.3181/00379727-117-29590.PMID14233451.S2CID28242978.
^Perklev T, Gassner FX, Martin RP, Huseby RA, Shimoda W (1965). "Excretion of radioactivity by human subjects after ingestion of liver from cattle treated with labeled polydiethylstilbestrol phosphate".Proceedings of the Society for Experimental Biology and Medicine.119 (4):996–998.doi:10.3181/00379727-119-30359.PMID5891085.S2CID43341013.
^Perklev T, Gassner FX, Hopwood ML (September 1967). "Distribution and excretion of 14C-labeled polydiethylstilbestrol phosphate in a steer".Journal of Animal Science.26 (5):1094–1100.doi:10.2527/jas1967.2651094x.PMID6077168.
Honda M, Umeda H, Yoshida K (August 1998). "[High-dose intravenous diethylstilbestrol diphosphate therapy for hormone refractory prostate cancer]".Nihon Rinsho. Japanese Journal of Clinical Medicine (in Japanese).56 (8):2145–2149.PMID9750524.
Nakagawa M (December 2002). "[Estrogen therapy--high-dose intravenous diethylstilbestrol diphosphate therapy for advanced or hormone refractory prostate cancer]".Nihon Rinsho. Japanese Journal of Clinical Medicine (in Japanese).60 (Suppl 11):199–204.PMID12599571.
