12 Treatment of hirsutism with 5α-reductase inhibitors

Anderson, 1968, Selective retention of dihydrotestosterone by prostatic nuclei, Nature, 219, 277, 10.1038/219277a0 Bardin, 1981, Testosterone: a major determinant of extragenital sexual dimorphism, Science, 211, 1285, 10.1126/science.7010603 Bardin, 1967, Testosterone and androstenedione production rates in normal women and in idiopathic hirsutism and polycystic ovary, Journal of Clinical Investigation, 46, 891, 10.1172/JCI105588 Baum, 1973, Copulation in castrated male rats following combined treatment with estradiol and dihydrotestosterone, Science, 182, 283, 10.1126/science.182.4109.283 Berkovitz, 1984, Inhibition of 5α-reductase activity and alteration of nuclear testosterone, Journal of Andrology, 5, 171, 10.1002/j.1939-4640.1984.tb02389.x Blohm, 1980, Inhibition of testosterone 5α-reductase by a proposed enzyme-activated, active site-directed inhibitor, Biochemical and Biophysical Research Communications, 95, 273, 10.1016/0006-291X(80)90735-4 Blohm, 1985, Pharmacologic induction of 5α-reductase deficiency in the postnatal rat, Pharmacologist, 27, 273 Brooks, 1981, Response of rat ventral prostate to a new and novel 5α-reductase inhibitor, Endocrinology, 109, 830, 10.1210/endo-109-3-830 Brooks, 1982, Effect of a new 5α-reductase inhibitor on size, histologic characteristics, and androgen concentrations of the canine prostate, Prostate, 3, 35, 10.1002/pros.2990030107 Brooks, 1982, Biological activities of a new steroidal inhibitor of Δ4-5α-reductase, 169, 67 Bruchovsky, 1968, The conversion of testosterone to 5α-androstan-17β-ol-3-one by rat prostate, Journal of Biological Chemistry, 243, 2012, 10.1016/S0021-9258(18)93542-8 Buvat, 1980, Physiopathology of the so-called idiopathic hirsutism, Nouvelle Presse Médicale, 31, 1699 Cameron, 1966, Transformation in vitro of (7α-3H)-dehydroepiandrosterone to (3H)-testosterone by skin from men, Journal of Endocrinology, 35, XIX Cantu, 1980, Post-pubertal female psychosexual orientation in incomplete male pseudohermaphroditism type 2 (5α-reductase deficiency), Acta Endocrinologica, 94, 273, 10.1530/acta.0.0940273 Cardinali, 1982, Norepinephrine stimulates testosterone aromatization and inhibits 5α-reduction via beta-adrenoceptors in rat pineal gland, Molecular and Cellular Endocrinology, 28, 199, 10.1016/0303-7207(82)90032-6 Dean, 1984, The effect of five synthetic progestational compounds on 5α-reductase activity in genital skin fibroblast monolayers, Steroids, 43, 13, 10.1016/0039-128X(84)90055-2 D'Occhio, 1980, Effects of androgenic and oestrogenic hormones on mating behaviour in rams castrated before or after puberty, Journal of Endocrinology, 86, 403, 10.1677/joe.0.0860403 Fisher, 1978, Clinical, endocrinological and enzymatic characterization of two patients with 5α-reductase deficiency: evidence that a single enzyme is responsible for the 5α-reduction of cortisol and testosterone, Journal of Clinical Endocrinology and Metabolism, 47, 653, 10.1210/jcem-47-3-653 Gallegos, 1967, Transformation and conjugation of dehydroepiandrosterone by human skin, Journal of Clinical Endocrinology and Metabolism, 27, 1214, 10.1210/jcem-27-8-1214 Golf, 1982, Affinity labeling of rat liver microsomal NADH-5a-reductase with a nucleotide analogue, Steroids, 40, 1, 10.1016/0039-128X(82)90108-8 Gomez, 1968, In vitro metabolism of testosterone-4-14C and Δ4-androstene-3,17-dione-4-14C in human skin, Biochemistry, 7, 24, 10.1021/bi00841a004 Goto, 1978, Synthesis and antiandrogenic activity of 16β-substituted-17β-hydroxysteroids, Chemical and Pharmaceutical Bulletin, 26, 1718, 10.1248/cpb.26.1718 Graef, 1976, Effect of 6β-methoxy-9β,10α-pregna-4,6-dione-3,20-dione (RO 6-1963) on the steroid reductases in rat liver, Experientia, 32, 1250, 10.1007/BF01953075 Hatch, 1981, Hirsutism: implications, etiology and management, American Journal of Obstetrics and Gynecology, 140, 815, 10.1016/0002-9378(81)90746-8 Hay, 1973, Metabolism of androgens in vitro by human facial and axillary skin, Journal of Endocrinology, 59, 475, 10.1677/joe.0.0590475 Hay, 1978, Distribution of androgen metabolizing enzymes in isolated tissues of human forehead and axillary skin, Journal of Endocrinology, 79, 29, 10.1677/joe.0.0790029 Horton, 1966, Androstenedione production and interconversion rates measured in peripheral blood and studies on the possible site of its conversion to testosterone, Journal of Clinical Investigation, 45, 301, 10.1172/JCI105344 Horton, 1967, In vivo conversion of dehydroisoandrosterone to plasma androstenedione and testosterone in man, Journal of Clinical Endocrinology and Metabolism, 27, 79, 10.1210/jcem-27-1-79 Horton, 1982, 3α,17β-Androstanediol glucuronide in plasma, a marker of androgen action in idiopathic hirsutism, Journal of Clinical Investigation, 69, 1203, 10.1172/JCI110558 Imperato-Mcginley, 1976, Male pseudohermaphroditism: the complexities of male phenotypic development, American Journal of Medicine, 61, 251, 10.1016/0002-9343(76)90175-3 Imperato-Mcginley, 1974, Steroid 5α-reductase deficiency in man: an inherited form of male pseudohermaphroditism, Science, 186, 1213, 10.1126/science.186.4170.1213 Imperato-Mcginley, 1985, The development of a male pseudohermaphroditic rat using an inhibitor of the enzyme 5a-reductase, Endocrinology, 116, 807, 10.1210/endo-116-2-807 James, 1974, Androgen metabolism in the human female, 23 Kadohama, 1983, Inhibitor effects of some steroidal 6-methylene derivatives on 5α-reductase activity in human and rat prostate, Journal of Steroid Biochemistry, 18, 551, 10.1016/0022-4731(83)90130-9 Kadohama, 1985, Retardation of prostate tumor progression in the Noble rat by 4-methyl-4-aza-steroidal inhibitors of 5α-reductase, Journal of the National Cancer Institute, 74, 475 Karpas, 1984, Effect of acute and chronic androgen suppression by glucocorticoids on gonadotropin levels in hirsute women, Journal of Clinical Endocrinology and Metabolism, 59, 780, 10.1210/jcem-59-4-780 Kirschner, 1984, Hirsutism and virilism in women, Special Topics in Endocrinology and Metabolism, 6, 55 Kirschner, 1971, Combined ovarian and adrenal vein catheterization to determine the site(s) of androgen overproduction in hirsute women, Journal of Clinical Endocrinology and Metabolism, 33, 199, 10.1210/jcem-33-2-199 Kirschner, 1973, The production, origin and role of dehydroepiandrosterone and Δ5-androstenediol as androgen prehormones in hirsute women, Journal of Clinical Endocrinology and Metabolism, 37, 188, 10.1210/jcem-37-2-183 Kuttenn, 1977, Androgen production and skin metabolism in hirsutism, Journal of Endocrinology, 75, 83, 10.1677/joe.0.0750083 Kuttenn, 1979, Male pseudohermaphroditism: a comparative study of one patient with 5α-reductase deficiency and three patients with the complete form of testicular feminization, Journal of Clinical Endocrinology and Metabolism, 49, 861, 10.1210/jcem-49-6-861 Kuttenn, 1980, Androgen metabolism in human skin, 99 Leshin, 1982, Inhibition of steroid 5α-reductase from human skin fibroblasts by 17β-N,N-diethylcarbamoyl-4-methyl-4-aza-5α-androstan-3-one, Journal of Steroid Biochemistry, 17, 245, 10.1016/0022-4731(82)90196-0 Liang, 1981, Inhibition of 5α-reductase, receptor binding and nuclear uptake of androgens in the prostate by a 4-methyl-4-aza-steroid, Journal of Biological Chemistry, 256, 7998, 10.1016/S0021-9258(18)43378-9 Liang, 1983, Biochemical and biological studies with 4-aza-steroidal 5α-reductase inhibitors, Journal of Steroid Biochemistry, 19, 385, 10.1016/S0022-4731(83)80051-X Liang, 1984, 4-Azasteroidal 5α-reductase inhibitors without affinity for the androgen receptor, Journal of Biological Chemistry, 259, 734, 10.1016/S0021-9258(17)43519-8 Liang, 1985, Species differences in prostatic steroid 5α-reductases of rat, dog and human, Endocrinology, 117, 571, 10.1210/endo-117-2-571 MacIndoe, 1984, Comparative studies of 5α-reductase inhibitors within MCF-7 human breast cancer cells, Journal of Steroid Biochemistry, 20, 1095, 10.1016/0022-4731(84)90349-2 MacLusky, 1981, Sexual differentiation of the central nervous system, Science, 211, 1294, 10.1126/science.6163211 Mauvais-Jarvis, 1977, Androgen metabolism in human skin: mechanisms of control, 229 Neri, 1972, Effects of a novel nonsteroidal antiandrogen on canine prostatic hyperplasia, Investigative Urology, 10, 123 Neri, 1968, Effects of an anti-androgen, SH714 (6-chlor-Δ6-1,2α-methylen-17α-hydroxyprogesterone acetate, cyproterone acetate) on canine prostatic hyperplasia, Endocrinology, 82, 311, 10.1210/endo-82-2-311 Peterson, 1977, Male pseudohermaphroditism due to steroid 5α-reductase deficiency, American Journal of Medicine, 62, 170, 10.1016/0002-9343(77)90313-8 Petrow, 1981, Prostatic cancer. I. 6-Methylene-4-pregnen-3-ones as irreversible inhibitors of rat prostatic Δ4-3-ketosteroid 5α-reductase, Steroids, 38, 121, 10.1016/0039-128X(81)90027-1 Petrow, 1982, Inhibition of prostatic growth in rats by 6-methylene-4-20-dione, Journal of Endocrinology, 95, 311, 10.1677/joe.0.0950311 Petrow, 1983, Prostatic cancer. II. Inhibitors of rat prostatic 4-ene-3-ketosteroid 5a-reductase derived from 6-methylene-4-androsten-3-ones, Journal of Steroid Biochemistry, 19, 1491, 10.1016/0022-4731(83)91125-1 Pugeat, 1982, Evidence of excessive androgen secretion by both the ovary and the adrenal in patients with idiopathic hirsutism, Obstetrics and Gynecology, 59, 46 Rasmusson, 1984, Azasteroids as inhibitors of rat prostatic 5α-reductase, Journal of Medicinal Chemistry, 27, 1690, 10.1021/jm00378a028 Resko, 1980, Sex steroids in the umbilical circulation of fetal rhesus monkeys from the time of gonadal differentiation, Journal of Clinical Endocrinology and Metabolism, 50, 900, 10.1210/jcem-50-5-900 Robaire, 1977, Selective inhibition of rat epididymal steroid Δ4-5α-reductase by conjugated allenic 3-oxo-5,10-seco-steroids, Journal of Steroid Biochemistry, 8, 307, 10.1016/0022-4731(77)90024-3 Sansone, 1971, Differential rates of conversion of testosterone to dihydrotestosterone in acne and in normal human skin-a possible pathogenic factor in acne, Journal of Investigative Dermatology, 56, 366, 10.1111/1523-1747.ep12261252 Serafini, 1985, Increased 5α-reductase activity in idiopathic hirsutism, Fertility and Sterility, 43, 74, 10.1016/S0015-0282(16)48320-2 Serafini, 1985, 5α-Reductase activity in the genital skin of hirsute women, Journal of Clinical Endocrinology and Metabolism, 60, 349, 10.1210/jcem-60-2-349 Sudo, 1981, 5α-Reduction of an anti-androgen TSAA-291, 16β-ethyl-17β-hydroxy-4-estren-3-one, by nuclear 5α-reductase in rat prostates, Steroids, 38, 55, 10.1016/0039-128X(81)90021-0 Takayasu, 1972, The in vivo and in vitro conversion of testosterone to 17β-hydroxy-5α-androstan-3-one (dihydrotestosterone) by the sebaceous gland of hamsters, Endocrinology, 90, 73, 10.1210/endo-90-1-73 Takayasu, 1980, Activity of testosterone 5α-reductase in various tissues of human skin, Journal of Investigative Dermatology, 74, 187, 10.1111/1523-1747.ep12541698 Toscano, 1983, Is hirsutism an evolving syndrome?, Journal of Endocrinology, 97, 379, 10.1677/joe.0.0970379 Vermorken, 1980, The antiandrogenic effect of progesterone on the hamster flank organ, British Journal of Dermatology, 102, 455, 10.1111/j.1365-2133.1980.tb06560.x Voigt, 1973, The antiandrogenic action of 4-androstan-3-one-17β-carboxylic acid and its methyl ester on hamster flank organ, Endocrinology, 92, 1216, 10.1210/endo-92-4-1216 Voigt, 1970, Transformation of testosterone into 17β-hydroxy-5α-androstan-3-one by microsomal preparations of human skin, Journal of Biological Chemistry, 245, 5594, 10.1016/S0021-9258(18)62696-1 Voigt, 1978, Inhibition of testosterone 5a-reductase by and antiandrogenicity of allenic 3-keto-5,10-secosteroids, Acta Endocrinologica, 87, 668, 10.1530/acta.0.0870668 Weintraub, 1984, Preparation of 20-(hydroxy-methyl)-4-methyl-4-aza-2-oxa-5α-pregnan-3-one as an inhibitor of testosterone 5α-reductase, Journal of Medicinal Chemistry, 28, 831, 10.1021/jm00383a026 Wenderoth, 1983, The effect of a 5a-reductase inhibitor on androgen-mediated growth of the dog prostate, Endocrinology, 113, 569, 10.1210/endo-113-2-569 Wilson, 1969, The conversion of testosterone to 5α-androstan-17β-ol-3-one (dihydrotestosterone) by skin slices of man, Journal of Clinical Investigation, 48, 371, 10.1172/JCI105994 Wilson, 1980, Sexual differentiation: early hormone synthesis and action, Biology of Reproduction, 22, 9, 10.1095/biolreprod22.1.9