Non-steroidal estrogen

Fosfestrol is indicated in the treatment of carcinoma of the prostate. It is a synthetic non-steroidal estrogen which is dephosphorylated to stilboestrol. Polyestradiol phosphate is an oestrogen with sustained activity that is exclusively used for prostate cancer. It is stored in tissues and slowly dephosphorylated to estrogen. 

Fosfestrol is a synthetic non-steroidal estrogen which is activated by the enzyme acid phosphatase to produce stilboestrol. 

Clomiphene is a very weak non-steroidal estrogen it blocks the feedback effect of endogenous estrogens on the pituitary, promoting the further secretion of gonadotropins. The primary use of clomiphene in women is in the induction of ovulation. In men, it has been used to treat infertility in view of its ability to increase endogenous production of testosterone (1). 

Cyclofenil is a weak non-steroidal estrogen related to diethylstilbestrol. For a number of years it was used for inducing ovulation, but has lost favor more recently there have been studies of its possible effects in Raynaud s phenomenon secondary to scleroderma (1). 

The non-steroidal estrogens diethylstilbestrol (rINN) and cyclofenine (rINN) are covered in separate monographs. 

Drug Class Non-steroidal estrogen Water Retention High High Blood Pressure Yes DHT Conversion Does not apply HPTA Suppression Severe... 

The reason this non-steroidal estrogenic fungus based drug has been included is simple Some dealers have claimed it to be a Mexican methandriol. Yes, it would have similar effects such as better androgen receptor-site sensitivity and elevated IGF-1 levels, but so does some oral female contraceptives. Worse yet is the bad bogus versions of Zeranabol that were floating around. Bottom line, do not do it ... 

Y Hori, Y Abe, M Ezaki, T Goto, M Okuhara, M Kohsaka. R1128 substances, novel non-steroidal estrogen-receptor antagonists produced by a Streptomyces. I. Taxonomy, fermentation, isolation, and biological properties. J Antibiot 46 1055-1062, 1993. 

In utero exposure of men to DES, a synthetic non-steroid estrogen, has been linked to increased incidence of meatal stenosis, epididymal cysts, testicular hypoplasia, cryptorchidism, microphallus, and sperm abnormalities (Henderson et al., 1976 Gill et al., 1977, 1979 Stillman, 1982). In females, adenosis, clear cell adenocarcinoma, and structural defects of the cervix, vagina, uterus, and fallopian tubes have been linked to in utero exposure to DES (Stillman, 1982). 

Willson TM, Henke BR, Momtahen TM, Charifson PS, Batchelor KW, Lubahn DB, Moore LB, Oliver BB, Sauls FIR, Triantafillou JA, Wolfe SG, Baer PG (1994) 3-[4-(l,2-Diphenylbut-l-enyl)phenyl]acrylic acid a non-steroidal estrogen with functional selectivity for bone over uterus in rats. J Med Chem 37 1550-1552... 

Facile geometric isomerization of phenolic non-steroidal estrogens and antiestrogens limitations to the interpretation of experiments characterizing the activity of individual isomers. Journal of Steroid Biochemistry, 22, 589-596. 

Zearalenone (ZEN), known as F2 toxin,is a non-steroidal estrogenic metabolites produced by Fusarium species, and was isolated by Christensen et. al. from a culture of Fusarium. Urry et. al. elucidated the chemical structure of... 

Modifying influences on immune responses have been reported for the sex steroids 17(i-estradiol and testosterone. 17 5-Estradiol and synthetic non-steroidal estrogenic compounds such as diethylstilbestrol are potent modulators of immunity. The effects observed in rodents include thymic atrophy, suppression of thymus-dependent cellular immune responses, acceleration of autoimmune diseases, suppression of NK cell activity, myelotoxicity, and stimulation of the mononuclear phagocyte system (see Luster et al., 1984 Holladay, 1999). However, the immune effects described for diethylstilbestrol depend largely on the age of the animals at treatment, exposure to diethylstilbestrol, and sex. 

Thomson MA, Lasley BL, Rideout BA, Kasman WH. Characterization of the estrogenic properties of a non-steroidal estrogen, equol, extracted from the urine of pregnant macaques. Biol Reprod 1984 31 705-713. 

Setchell KDR. Non-steroidal estrogens of dietary origin possible roles in health and disease, metabolism and physiological effects. Proc. Nutr. Soc. NZ 20, 1-21, 1995. 

Diethylstilbestrol and other non-steroidal estrogens Novel class of store-operated calcium channel modulators... 

J. H. Al-Rifai, C. L. Gabelish and A. I. Schafer, Oeeurrenee of pharmaceutically active and non-steroidal estrogenic compounds in three different wastewater recycling schemes in Australia, Chemosphere, 2007, 69, 803-815. 

Hori Y, Abe Y, Shigematsu N, Goto T, Okuhara M, Kohsaka M. Napyradiomycins A and Bl non-steroidal estrogen-receptor antagonists produced by a Streptomyces. J. Antibiot. 1993 46(12) 189(U1893. 

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