Effect of a new topically active antiandrogen (RU 38882) on the rat sebaceous gland: comparison with cyproterone acetate.

RU 38882 is a new antiandrogen. When given by subcutaneous or oral route, RU 38882 is about 25 times less potent than cyproterone acetate. However, when applied topically to the intact rat skin, RU 38882 (0.25-25 mg/rat/day for 5 days or 3 weeks) decreases, in a dose-related manner, the volume density of the smooth endoplasmic reticulum vesicles of the differentiating cells of the sebaceous gland, a structure directly involved in sebum lipid synthesis. Under these conditions RU 38882 is about 100 times more potent than cyproterone acetate and unlike cyproterone acetate, does not modify the prostate weight. The lack of efficacy of cyproterone acetate on the sebaceous gland could be due to its partial androgenic activity while RU 38882, under these conditions, acts as a pure antiandrogen which inhibits the nuclear androgen-receptor translocation.

[1]  M. Brienne,et al.  Antiandrogenic activity of a series of des-A-steroid derivatives. , 1985, Journal of medicinal chemistry.

[2]  Brant C. White,et al.  United States patent , 1985 .

[3]  P. Wise,et al.  Oral spironolactone improves acne vulgaris and reduces sebum excretion , 1984, The British journal of dermatology.

[4]  S. Shuster,et al.  INDIRECT EVIDENCE THAT THE ACTION OF CYPROTERONE ACETATE ON THE SKIN IS DUE TO A METABOLITE , 1983, Clinical endocrinology.

[5]  C. Manieri,et al.  A new therapeutic approach to acne: an antiandrogen percutaneous treatment with spironolactone , 1983 .

[6]  S. Shuster,et al.  Sex difference in response of the human sebaceous gland to topical flutamide , 1982, The British journal of dermatology.

[7]  J. Tamm,et al.  The effect of the antiandrogen IIα‐hydroxyprogesterone on sebum production and cholesterol concentration of sebum , 1982, The British journal of dermatology.

[8]  M. Bouton,et al.  Estrogen regulation of rat prostate androgen receptor. , 1981, Journal of steroid biochemistry.

[9]  J. Mornon,et al.  Steroid hormone receptors and pharmacology. , 1980, Journal of steroid biochemistry.

[10]  J. Raynaud,et al.  The relevance of interaction kinetics in determining biological response to estrogens. , 1979, Endocrinology.

[11]  F. Labrie,et al.  Action of a non-steroid anti-androgen, RU 23908, in peripheral and central tissues. , 1979, Journal of steroid biochemistry.

[12]  J. Saurat,et al.  Androgen receptor in human skin , 1977, The British journal of dermatology.

[13]  C. Bonne,et al.  Characterization and hormonal control of the androgen receptor in the hamster sebaceous glands. , 1977, The Journal of investigative dermatology.

[14]  K. Adachi Receptor proteins for androgen in hamster sebaceous glands. , 1974, The Journal of investigative dermatology.

[15]  J. Strauss,et al.  Endocrinologic Control to the Development and Activity of the Human Sebaceous Gland , 1974 .

[16]  S. Shuster,et al.  Reduction of sebum excretion in man by the antiandrogen, cyproterone acetate , 1973, The British journal of dermatology.

[17]  W. Cunliffe,et al.  THE EFFECT OF TOPICAL CYPROTERONE ACETATE ON SEBUM SECRETION IN PATIENTS WITH ACNE , 1969, The British journal of dermatology.

[18]  J. Strauss,et al.  The effect of androgens and estrogens on human sebaceous glands. , 1962, The Journal of investigative dermatology.

[19]  G. Scatchard,et al.  THE ATTRACTIONS OF PROTEINS FOR SMALL MOLECULES AND IONS , 1949 .