Abstract
Anti-androgens are compounds which prevent androgens from expressing their activity at target sites (Dorfman 1970), and are therefore considered of potential therapeutic value in diseases where androgenic stimulation appears to play a pathogenic role. Thus, dermatological conditions involving hair follicles and sebaceous glands, such as androgenic alopecia, idiopathic hirsutism, acne and seborrhoea, where androgen involvement is recognised, should benefit from such therapy. Clinical experience in recent years, using systemic anti-androgens to treat females with these conditions, has been encouraging. In males, however, anti-androgen treatment has been restricted to male hypersexuality and tumours of the prostate (Neumann and Jacobi 1982) for obvious toxicological reasons.
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References
Adachi K, Kano M (1972) The role of receptor proteins in controlling androgen action in the sebaceous glands of hamsters. Steroids 19:567–574
Archibald A, Shuster S (1970) The measurement of sebum secretion in the rat. Br J Dermatol 82:146–151
Aydinlik S, Lachnit-Fixson U (1977) Diane — eine Gestagen-Östrogenkombination mit An-tiandrogenwirkung. Med Monatsschr 31:425–429
Baulieu EE, Jung I (1970) A prostatic cytosol receptor. Biochem Biophys Res Commun 38:599–606
Belham JE, Neal GE (1971) Testosterone action in rat ventral prostate. The effects of diethylstilboestrol and cyproterone acetate on the metabolism of [3H] testosterone and the retention of labelled metabolites by rat ventral prostate in vivo and in vitro. Biochem J 125:81–91
Bruchovsky N (1980) Molecular action of androgens and antiandrogens. In: Hammerstein J, Lachnit-Fixson U, Neumann F, Plewig G (eds) Androgenization in women. Acne, seborrhoea, androgenic alopecia and hirsutism. Symposium, Berlin. Excerpta Medica, Amsterdam, pp 7–20
Bruchovsky N, Wilson JC (1968) The conversion of testosterone to 5α-androstan-17β-ol-3-one by rat prostate in vivo and in vitro. J Biol Chem 243:2012–2021
Burdick KH, Hill R (1970) The topical effect of the antiandrogen Chlormadinone acetate and some of its chemical modifications on the hamster costovertebral organ. Br J Dermatol 82 [Suppl 6]: 19–25
Burton JL (1979) Antiandrogen therapy in dermatology: a review. Clin Exp Dermatol 4:501–507
Burton JL, Laschet U, Shuster S (1973) Reduction of sebum excretion in man by the antiandrogen cyproterone acetate. Br J Dermatol 89:487–490
Cooper MF, Hay JB, McGibbon D, Shuster S (1978) Correlations between androgen metabolism and sebaceous gland activity. Trans Biochem Soc 6:970–972
Cooper MF, McGibbon D, Wilson PD, Shuster S (1979) Androgenic control of the human sebaceous gland (abstr). J Invest Dermatol 72:267
Corvol P, Michaud A, Menard J, Freifeld M, Mahoudeau J (1975) Antiandrogenic effects of spirolactones: mechanism of action. Endocrinology 97:52–58
Cunliffe WJ, Shuster S, Casseis Smith AJ (1969) The effect of topical cyproterone acetate on sebum secretion in patients with acne. Br J Dermatol 81:200–201
Dorfman RI (1970) Biological activity of antiandrogens. Br J Dermatol 82 [Suppl 6]:3–8
Ebling FJ, Skinner J (1967) The measurement of sebum production in rats treated with testosterone and oestradiol. Br J Dermatol 79:386–392
Ebling FJ, Ebling E, Randall V, Skinner J (1975) The effects of hypophysectomy and of bovine growth hormone on the responses to testosterone of prostate, preputial, Harderian and lachrymal glands and of brown adipose tissue in the rat. J Endocrinol 66:401–406
Ebling FJ, Randall VA, Skinner J (1981) Local suppression of sebum secretion in rats by topical cyproterone acetate in ethanol. J Invest Dermatol 77:458–463
Ewing L, Brown B, Irby DC, Jardine I (1975) Testosterone and 5α-reduced androgen secretion by rabbit testes-epididymides in vitro. Endocrinology 96:610–617
Fang S, Liao S (1969) Antagonistic action of antiandrogens on the formation of a specific dihydrotestosterone-receptor protein complex in rat ventral prostate. Mol Pharmacol 5:428–431
Fang S, Anderson KM, Liao S (1969) Receptor proteins for androgens: on the role of specific proteins in selective retention of 17βhydroxy-5α-androstan-3-one by rat ventral prostate in vivo and in vitro. J Biol Chem 244:6584–6595
Farnworth WE, Brown JR (1963) Metabolism of testosterone by the human prostate. JAMA 183:436–439
Ferrari RA, Chakrabarty K, Creange JE, Beyler AL, Potts GO, Schane HP (1980) Endocrine profile of Topterone, a topical antiandrogen, in three species of laboratory animals. Methods Find Exp Clin Pharmacol 2:65–69
Frost P, Giegel JL, Weinstein GD, Gomez EC (1973) Biodynamic studies of hamster flank organ growth: hormonal influences. J Invest Dermatol 61:159–167
Glenn EM, Gray J (1965) Effect of various hormones on the growth and histology of the gerbil (Meriones unguiculatus) abdominal sebaceous gland pad. Endocrinology 76:1115–1123
Hall DWR, Van der Hoven WE, Noordzij-Kamermans NJ, Jaitly KD (1983) Hormonal control of hamster ear sebaceous gland lipogenesis. Arch Dermatol Res 275:1–7
Hamada H, Neumann F, Junkmann K (1963) Intrauterine antimaskuline Beeinflussung von Rattenfeten durch ein stark gestagen wirksames Steroid. Acta Endocrinol (Copenh) 44:380–388
Hammerstein J, Meckies J, Leo-Rossberg I, Moltz L, Zielske F (1975) Use of cyproterone acetate (CPA) in the treatment of acne, hirsutism and virilism. J Steroid Biochem 6:827–836
Hay JB (1977) A study of the in vitro metabolism of androgens by human scalp and pubic skin. Br J Dermatol 97:237–246
Hsia SL, Voigt W (1974) Inhibition of dihydrotestosterone formation: an effective means of blocking androgen action in hamster sebaceous glands. J Invest Dermatol 62:224–227
Imperato-McGinley J, Guerrero L, Gautier T, Peterson RE (1974) Steroid 5α-reductase deficiency in man; an inherited form of male pseudohermaphroditism. Science 186:1213–1215
Ismail AAA, Davidson DW, Souka AR, Barnes EW, Irvine WJ, Kilimnik H, Vanderbeeken Y (1974) The evaluation of the role of androgens in hirsutism and the use of a new antiandrogen “cyproterone acetate” for therapy. J Clin Endocrinol Metab 39:81–95
Jeffcoates WJ, Edwards CRW, Rees LH, Besser GM (1976) Cyproterone acetate. Lancet 2:1140
Jenkins JS, Ash S (1973) The metabolism of testosterone by human skin in disorders of hair growth. J Endocrinol 59:345–351
Katchen B, Buxbaum S (1975) Disposition of a new, non-steroid, antiandrogen, α, α, α-tri-fluoro-2-methyl-4′-nitro-m-propionotoluidide (flutamide) in men following a single oral 200 mg dose. J Clin Endocrinol Metab 41:373–379
Krähenbühl C, Desaulles PA (1969) Interactions between α-MSH and sex steroids on the preputial glands of female rats. Experientia 25:1193–1195
Liao S, Liang T, Tymoczko JL (1972) Structural recognitions in the interactions of androgens and receptor proteins in their association with nuclear acceptor components. J Steroid Biochem 3:401–408
Lyons F, Shuster S (1981) Effect of topical 17α-propyltestosterone on sebum excretion in man. Br J Dermatol 104:685–686
Lyons F, Shuster S (1982) Sex difference in response of the human sebaceous gland to topical flutamide. Br J Dermatol 107:697–699
Lyons F, Shuster S (1983) Indirect evidence that the action of cyproterone acetate on the skin is due to a metabolite. Clin Endocrinol 19i:53–55
Mainwaring WIP, Jones DM (1975) Influence of receptor complexes on the properties of prostate chromatin, including its transcription by RNA polymerase. J Steroid Biochem 6:475–481
Marsden JR, Shuster S, Lyons F (1983) Is low dose cyproterone acetate and ethinyl oestradiol (“Diane”) effective in acne? (letter) Lancet 2:215
Marsden JR, Shuster S, Lyons F (1984) Effect of 13-cis-retinoic acid and cyproterone acetate on acne severity, sebum excretion rate, dermal and epidermal lipogenesis, serum lipids and liver function tests. In: Cunliffe WJ, Miller A J (eds) Retinoid therapy — a review of clinical and laboratory research. MTP, Boston, pp 267–276
Mauvais-Jarvis P (1977) Androgen metabolism in human skin: mechanisms of control. In: Martini L, Motta M (eds) Androgens and antiandrogens. Raven, New York, pp 229–245
Mauvais-Jarvis P, Kuttenn F, Baudot N (1974) Inhibition of testosterone conversion to dihydrotestosterone in men treated percutaneously by progesterone. J Clin Endocrinol Metab 38:142–147
Neri R, Florance K, Koziol P, Van Cleave S (1972) A biological profile of a nonsteroidal antiandrogen SCH 13521 (4′-nitro-3′-trifluoromethylisobutyranilide). Endocrinology 91:427–437
Neumann F, Jacobi GH (1982) Antiandrogens in tumour therapy. In: Furr BJA (ed) Clinics in oncology, Ed. by vol 1. Saunders, Philadelphia, pp 41–64
Neumann F, Schleusener A (1981) Pharmacology of cyproterone acetate with special reference to the skin. In: Vokaer R, Fanta D (eds) Combined antiandrogen-estrogen therapy in dermatology, proc of the Diane symposium. Excerpta Medica, Amsterdam, pp 19–51
Neumann F, Schleusener A, Albring M (1980) Pharmacology of antiandrogens. In: Hammerstein J, Lachnit-Fixson U, Neumann F, Plewig G (eds) Androgenization in women. Acne, seborrhoea, androgenic alopecia and hirsutism. Symposium, Berlin. Excerpta Medica, Amsterdam, pp 147–192
Nikkari T (1965) Composition and secretion of the skin surface lipids of the rat; effects of dietary lipids and hormones. Scand J Clin Lab Invest 17 [Suppl 85]: 1–140
Peets EA, Henson MF, Neri R (1974) On the mechanism of the antiandrogenic action of flutamide (α-α-α-trifluoro-2-methyl-4′-nitro-m-propionotoluidide) in the rat. Endocrinology 94:532–540
Peterson RE, Imperato-McGinley J, Gautier T, Sturla E (1977) Male pseudohermaphroditism due to steroid 5α-reductase deficiency. Am J Med 62:170–191
Plewig G, Luderschmidt C (1977) Hamster ear model for sebaceous glands. J Invest Dermatol 68:171–176
Price VH (1975) Testosterone metabolism in the skin, a review of its function in androgenetic alopecia, acne vulgaris and idiopathic hirsutism including recent studies with antiandrogens. Arch Dermatol 111:1496–1502
Pye RJ, Burton JL, Harris JI (1976) Effect of 1% cyproterone acetate in cetomacrogol cream BPC (Formula A) on sebum excretion rate in patients with acne. Br J Dermatol 95:427–428
Raynaud JP, Azadian-Boulanger G, Bonne C, Perronet J, Sakiz E (1977) Present trends in antiandrogen research. In: Martini L, Motta M (eds) Androgens and antiandrogens. Raven, New York, pp 281–293
Saenger P, Goldman AS, Levine LS, Korthschutz S, Muecke EC, Katsumata M, Doberne Y, New MI (1978) Prepubertal diagnosis of steroid 5α-reductase deficiency. J Clin Endocrinol Metab 46:627–634
Sansone G, Reisner RM (1971) Differential rates of conversion of testosterone to dihydrotesterone in acne and in normal human skin. A possible pathogenic factor in acne. J Invest Dermatol 56:366–372
Saunders HL, Holden K, Kerwin JF (1964) The antiandrogenic activity of 17α-methyl-β-nortestosterone (SKF-7690). Steroids 3:687–698
Schmidt-Elmendorff H, Steyer M (1977) Klinische Erfahrungen mit einem niedrigdosierten Antiandrogen (Cyproteron-azetat) und Äthinylöstradiol bei Frauen mit Virilisierungserscheinungen. Geburtshilfe Frauenheilkd 37:297–299
Shuster S (1982) The sebaceous glands and primary cutaneous virilism. In: Jeffcoate SL (ed) Androgen sand anti-androgen therapy. Wiley, Chichester, pp 1–21
Simpson NB, Bowden PE, Forster FA, Cunliffe WJ (1979) The effect of topically applied progesterone on sebum excretion rate. Br J Dermatol 100:687–692
Stewart ME, Pochi PE (1978) Antiandrogens and the skin. Int J Dermatol 17:167–179
Strauss JS, Pochi PE (1961) The quantitative gravimetric determination of sebum production. J Invest Dermatol 36:293–298
Szalay R, Krieg M, Schmidt H, Voigt KD (1975) Metabolism and mode of action of androgens in target tissues of male rats. V. Uptake and metabolism of cyproterone acetate and its influence on the uptake and metabolism of testosterone in target organs and peripheral tissues. Acta Endocrinol (Copenh) 80:592–602
Takayasu S (1979) Metabolism and action of androgens in the skin. Int J Dermatol 18:681–692
Takayasu S, Adachi K (1970) Hormonal control of metabolism in hamster costovertebral glands. J Invest Dermatol 55:13–19
Takayasu S, Wakimoto H, Itami S, Sano S (1980) Activity of testosterone 5α-reductase in various tissues of human skin. J Invest Dermatol 74:187–191
Thomas JP, Oake RJ (1974) Androgen metabolism in the skin of hirsute women. J Clin Endocrinol Metab 38:19–22
Voigt W, Hsia SL (1973 a) Further studies on testosterone 5α-reductase of human skin: structural features of steroid inhibitors. J Biol Chem 248:4280–4285
Voigt W, Hsia SL (1973 b) The antiandrogenic action of 4-androsten-3-one-17β-carboxylic acid and its methyl ester on hamster flank organ. Endocrinology 92:1216–1222
Voigt W, Fernandez EP, Hsia SL (1970) Transformation of testosterone into 17β-hydroxy-5α-androstan-3-one by microsomal preparations of human skin. J Biol Chem 245:5594–5599
Von Muhlendahl KE, Korth-Schultz S, Muller-Hess R, Helge H, Webb B (1977) Cyproterone acetate and adrenocortical function. Lancet 1:1160–1161
Walsh PC, Madden JD, Harrod MJ, Goldstein JL, MacDonald PC, Wilson JD (1974) Familial incomplete male pseudohermaproditism type 2: decreased dihydrotestosterone formation in pseudovaginal perineoscrotal hypospadias. N Engl J Med 291:944–949
Wilson JD, Walker JD (1969) The conversion of testosterone to 5α-androstan-17β-ol-3-one (dihydrotestosterone) by skin slices of man. J Clin Invest 48:371–379
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Thomson, D.S. (1989). Pharmacology of Anti-androgens in the Skin. In: Greaves, M.W., Shuster, S. (eds) Pharmacology of the Skin II. Handbook of Experimental Pharmacology, vol 87 / 2. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-642-74054-1_36
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DOI: https://doi.org/10.1007/978-3-642-74054-1_36
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