Male hormonal contraceptives: a potentially patentable and profitable product

Bibliography

• UNITED NATIONS FAMILY PLANNING ASSOCIATION: Report of the International Conference on Population Development. New York, United Nations (1994).
   Google Scholar
• MCLACHLAN RI, O'DONNEL L, MEACHEM SJ et al.: Identification of specific sites of hormonal regulation of spermatogenesis in rats, monkeys, and man. Recent Prog. Horm. Res. (2002) 57:149–179.
   Google Scholar
• WORLD HEALTH ORGANIZATION TASK FORCE ON METHODS FOR THE REGULATION OF MALE FERTILITY: Contraceptive efficacy of testosterone-induced azoospermia by testosterone enanthate in normal men. Lancet (1990) 336:995–999.
   Web of Science ®Google Scholar
• WORLD HEALTH ORGANIZATION TASK FORCE ON METHODS FOR THE REGULATION OF MALE FERTILITY: Contraceptive efficacy of testosterone-induced azoospermia or oligozoospermia by testosterone enanthate in normal men. Fend Steril. (1996) 65:821–829.
   PubMed Web of Science ®Google Scholar
• ••Landmark study that demonstrated thathigh-dosage testosterone provides efficacious contraception to nearly all men.
   Google Scholar
• HANDELSMAN DJ, FARLEY TM, PEREGOUDOVA, WAITES GM: Factors in nonuniform induction of azoospermia by testosterone enanthate in men. Fend Steril (1995) 63:125–133.
   PubMed Web of Science ®Google Scholar
• VON ECKARDSTEIN A, BUCHTER D, NIESCHLAG E: Successful treatment of male hypogonadism with testosterone undecanoate (TU) in extended intervals of 12 weeks. VIIth International Congress of Andrology. Montreal, Canada (2001).
   Google Scholar
• ZHANG GY, GU YQ, WANG XH, CUI Y, BREMNER WJ: A pharmacokinetic study of injectable testosterone undecanoate in hypogonadal men./ Andra (1998) 19:761–768.
   PubMed Web of Science ®Google Scholar
• BEHRE HM, ABSHAGEN K, OETTEL M, HUBLER D, NIESCHLAG E: Intramuscular injection of testosterone undecanoate for the treatment of male hypogonadism: Phase I studies. Eur. Endocrinol (1999) 140:414–419.
   PubMed Web of Science ®Google Scholar
• ANDERSON RA, ZHU H, CHENG L,BAIRD DT: Investigation of a novel preparation of testosterone decanoate in men: pharmacokinetics and spermatogenic suppression with etonorgestrel implants. Contraception (2002) 66:357–364.
   PubMed Web of Science ®Google Scholar
• HAY CJ, GRADY BM, ZITZMANN M et al.: A multicenter Phase IIb study of a novel combination of intramuscular androgen (testosterone decanoate) and oral progestogen (etonogestrel) for male hormonal contraception. J. Clin. Endocrinol Metab. (2005) 90:2042–2049.
   PubMed Web of Science ®Google Scholar
• HANDELSMAN DJ, CONWAY AJ, BOYLAN LM: Pharmacotherapy and pharmacokinetics of testosterone pellets in man. J. Clin. Endocrinol Metab. (1990) 71:216–22.
   PubMed Web of Science ®Google Scholar
• GU YQ, WANG XH, XU D et al.: A multicenter contraceptive efficacy study of injectable testosterone undecanoate in healthy Chinese men. J. Clin. Endocrinol Metab. (2003) 88:562-568. Contraceptive efficacy study that demonstrated a longer-acting, injectable testosterone formulation was efficacious.
   Google Scholar
• GU YQ, TONG QS, MA DZ et al.: Male hormonal contraception: effects of injections of testosterone undecanoate and depot medroxyprogesterone acetate at eight-week intervals in Chinese men. J. Clin. Endocrinol Metab. (2004) 89:2254–2262.
   PubMed Web of Science ®Google Scholar
• HEINEMANN K, SAAD F, WIESEMES M, WHITES, HEINEMANN L: Attitudes toward male fertility control: results of a multinational survey on four continents. Hum. Reprod. (2005) 20:549–556.
   PubMed Web of Science ®Google Scholar
• ••A large, cross-cultural survey of men thatshowed a high level of acceptance of a male hormonal contraceptive. An oral pill was the most desirable route of administration and once yearly injections or implants was preferred to shorter intervals.
   Google Scholar
• BUCHTER D, VON ECKARDSTEIN S, VON ECKARDSTEIN A et al.: Clinical trial of transdermal testosterone and oral levonorgestrel for male contraception. J. Clin. Endocrinol Metab. (1999) 84:1244–1249.
   Google Scholar
• GONZALO ITG, SWERDLOFF RS, NELSON AL et al.: Levonorgestrel implants (Norplant II) for male contraception clinical trials: combination with transdermal and injectable testosterone. J. Clin. Endocrinol Metab. (2002) 87:3562–3572.
   PubMedGoogle Scholar
• WANG C, CUNNINGHAM G, DOBS A et al.: Long-term testosterone gel (AndroGel) treatment maintains beneficial effects on sexual function and mood, lean and fat mass, and bone mineral density in hypogonadal men. J. Clin. Endocrinol Metab. (2004) 89:2085–2098.
   PubMed Web of Science ®Google Scholar
• BAGATELL CJ, BREMNER WJ: Androgens in men - uses and abuses. N Engl. J. Med. (1996) 334:707–714.
   PubMed Web of Science ®Google Scholar
• MERIGGIOLA MC, BREMNER WJ, CONSTANTINO A. PAVANI A. CAPELLI M, FLAMIGNI C: An oral regimen of cyproterone acetate and testosterone undecanoate for spermatogenic suppression in men. Fend Steril (1997) 68:844–850.
   Google Scholar
• AMORY JK, BREMNER WJ: Oral testosterone in oil plus dutasteride in men: a pharmacokinetic study. J. Clin. Endocrinol Metab. (2005) 90:2610–2617.
   PubMed Web of Science ®Google Scholar
• HELLER CG, LAIDLAW WM, HARVEY HT, NELSON WO: Effects of progestational compounds on the reproductive processes of the human male. Ann. NY Acad. Sci. (1958) 71:649–665.
   PubMed Web of Science ®Google Scholar
• BEBB RA, ANAWALT BD, CHRISTENSEN RB et al.: Combined administration of levonorgestrel and testosterone induces more rapid and effective suppression of spermatogenesis than testosterone alone: a promising male contraceptive approach./ Clin. Endocrinol Metab. (1996) 81:3018–3023.
   PubMedGoogle Scholar
• MERIGGIOLA MC, FARLEY TM, MBIZVO MT: A review of androgen-progestin combinations for male contraception. J. AndroL (2003) 24:466–483.
   PubMed Web of Science ®Google Scholar
• WORLD HEALTH ORGANIZATION TASK FORCE ON METHODS FOR THE REGULATION OF MALE FERTILITY: Comparison of two androgens plus depot-medroxyprogestrone acetate for suppression to azoospermia in Indonesian men. Fend Steril (1993) 60:1062–1068.
   PubMedGoogle Scholar
• TURNER L, CONWAY AJ, JIMENEZ M et al.: Contraceptive efficacy of a depot progestin and androgen combination in men. J. Clin. Endocrinol Metab. (2003) 88:4659–4667.
   PubMed Web of Science ®Google Scholar
• ••Contraceptive efficacy study thatdemonstrated that depot testosterone plus a depot progestogen (DMPA) was very efficacious and did not suppress HDL levels.
   Google Scholar
• KAMISCHKE A. VENHERM S, PLODGER D, VON ECKARDSTEIN S, NIESCHLAG E: Intramuscular testosterone undecanoate and norethisterone enanthate in a clinical trial for male contraception. J. Clin. Endocrinol Metab. (2001) 86:303–309.
   PubMed Web of Science ®Google Scholar
• KAMISCHKE A, HEUERMANN T, KRUGER K et al.: An effective hormonal male contraceptive using testosterone undecanoate with oral or injectable norethisterone preparations. J. Clin. Endocrinol Metab. (2002) 87:530–539.
   PubMed Web of Science ®Google Scholar
• MERIGGIOLA MC, CONSTANTINO A, SAAB F et al.: Norethisterone enanthate plus testosterone undecanoate for male contraception: effects of various injection intervals on spermatogenesis, reproductive hormones, testis and prostate. J. Clin. Endocrinol Metab. (2005) 90:2005–2014.
   PubMed Web of Science ®Google Scholar
• ANDERSON RA, KINNIBURGH D, BAIRD DT: Suppression of spermatogenesis by etonogestrel implants with depot testosterone: potential for long-acting male contraception. J. Clin. Endocrinol Metab. (2002) 87:3640–3649.
   PubMed Web of Science ®Google Scholar
• BRADY BM, WALTON M, HOLLOW N, KICMAN AT, BAIRD DT, ANDERSON RA: Depot testosterone with etonorgestrel implants result in induction of azoospermia in all men for long-term contraception. Hum. Reprod. (2004) 19:2658–2667.
   PubMed Web of Science ®Google Scholar
• ANAWALT BD, BEBB RA, BREMNER WJ, MATSUMOTO AM: A lower dosage levonorgestrel and testosterone combination effectively suppresses spermatogenesis and circulating gonadotropin levels with fewer metabolic effects than higher dosage combinations. J. AndroL (1999) 20:407–413.
   PubMed Web of Science ®Google Scholar
• ANAWALT BD, AMORY JK, HERBST KLet al.: Intramuscular testosterone enanthate plus very low dosage oral levonorgestrel suppresses spermatogenesis without causing weight gain in normal young men: a randomized clinical trial. J. Androl (2005) 26:405–413.
   Google Scholar
• WU FCW, BALASUBRAMANIAN R, MULDERS TM, COELINGH-BENNICK HJ: Oral progestogen combined with testosterone as a potential male contraceptive: additive effects between desogestrel and testosterone enanthate in suppression of spermatogenesis, pituitary-testicular axis, and lipid metabolism. J. Clin. Endocrinol Metab. (1999) 84:112–122.
   PubMedGoogle Scholar
• ANAWALT BD, HERBST MATSUMOTO AM, MULDERS TM, COELINGH-BENNICK HJ, BREMNER WJ: Desogestrel plus testosterone effectively suppresses spermatogenesis but also causes modest weight gain and high-density lipoprotein suppression. Fend. Steril. (2000) 74:707–714.
   PubMed Web of Science ®Google Scholar
• KINNIBURGH D, ZHU H, CHENG L, KICMAN AT, BAIRD DT, ANDERSON RA: Oral desogestrel with testosterone pellets induces consistent suppression of spermatogenesis to azoospermia in both Caucasian and Chinese men. Hum. Reprod. (2002) 17:1490–1501.
   PubMed Web of Science ®Google Scholar
• ZHANG FP, PAKARAINEN T, POUTANEN M, TOPPARI J, HUHTANIEMI I: The low gonadotropin-independent constitutive production of testicular testosterone is sufficient to maintain spermatogenesis. Proc. Natl Acad. Sci. USA (2003) 100:13692–13697.
   PubMed Web of Science ®Google Scholar
• MERIGGIOLA MC, CONSTANTINO A, BREMNER WJ, MORSELLI-LABATE AM: Higher testosterone dose impairs sperm suppression induced by a combined androgen-progestin regimen. J. Androl. (2002) 23:684–689.
   PubMed Web of Science ®Google Scholar
• MERIGGIOLA MC, BREMNER WJ, PAULSEN C et al.: A combined regimen of cyproterone acetate and testosterone enanthate as a potentially highly effective male contraceptive. J. Clin. Endocrinol Metab. (1996) 81:3018–3023.
   PubMed Web of Science ®Google Scholar
• MERIGGIOLA MC, BREMNER WJ, CONSTANTINO k DI CINTIO G, FLAMIGNI C: Low dose cyproterone actetate and testosterone enanthate for contraception in men. Hum. Reprod. (1998) 13:1225–1229.
   PubMed Web of Science ®Google Scholar
• MERIGGIOLA MC, CONSTANTINO A, CERPOLINI Set al: Testosterone undecanoate maintains spermatogenic suppression induced by cyproterone acetate plus testosterone undecanoate in normal men. J. Clin. Endocrinol. Metab. (2003) 88:5818–5826.
   PubMed Web of Science ®Google Scholar
• •Testosterone plus cyproterone is highly effective in inducing azoospermia with few adverse effects.
   Google Scholar
• SWERDLOFF RS, BAGATELL CJ, WANG C et al.: Suppression of spermatogenesis in man induced by Nal-Glu gonadotropin-releasing hormone antagonist and testosterone enanthate (TE) is maintained by TE alone. J. Clin. Endocrinol. Metab. (1998) 83:3527–3533.
   PubMed Web of Science ®Google Scholar
• SITRUK-WARE R: Pharmacolgical profile of progestins. Maturitas. (2004) 47:277–283.
   PubMed Web of Science ®Google Scholar
• KEAM SJ, WAGSTAFF AJ: Ethinylestradiol /drospirenone: a review of its use as an oral contraceptive. Treat. Endocrinol (2003) 2:49–70.
   PubMedGoogle Scholar
• MERIGGIOLA MC, BREMNER WJ, CONSTANTINO A et al: Twenty-one day administration of dienogest reversibly suppresses gonadotropins and testosterone in normal men. J. Clin. Endocrinol Metab. (2002) 87:2107–2113.
   PubMed Web of Science ®Google Scholar
• CUMMINGS DE, BREMNER WJ: Prospects for new hormonal male contraceptives. Endocrinol Metab. Clin. North Am. (1994) 23:893–922.
   PubMed Web of Science ®Google Scholar
• PAVLOU SN, BREWER K, FARLEY MG et al.: Combined administration of a gonadotropin-releasing antagonist and testosterone in men induces reversible azoospermia without loss of libido. J. Clin. Endocrinol. Metab. (1991) 73:1360–1369.
   PubMed Web of Science ®Google Scholar
• TOM L, BHASIN S, SALAMEH Wet al.:Induction of azoospermia in normal men with combined Nal-Glu gonadotropin-releasing hormone antagonist and testosterone enanthate. j Clin. Endocrinol Metab. (1992) 75:476–483.
   Google Scholar
• BAGATELL CJ, MATSUMOTO AM, CHRISTENSEN RB, RIVIER JE, BREMNER WJ: Comparison of a gonadotropin-releasing antagonist plus testosterone (T) versus testosterone alone as potential male contraceptive regimens. Clin. Endocrinol Metab. (1993) 77:427–432.
   Google Scholar
• HERBST KL, ANAWALT BD, AMORY JK, BREMNER WJ: Acyline: the first study in humans of a potent, gonadotropin-releasing hormone antagonist. j Clin. Endocrinol Metab. (2002) 87:3215–3220.
   PubMed Web of Science ®Google Scholar
• CHO N, HARADA M, IMEDA T et al: Discovery of a novel, potent, and orally active nonpeptide antagonist of the human luteinizing hormone-releasing hormone (LHRH) receptor. J. Med. Chem. (1998) 41:4190–4195.
   PubMed Web of Science ®Google Scholar
• BESECKE L, DIAZ G, SEGRETI T et al.: Pharmacological and endocrine characterization ofA-19840, an orally active GnRH antagonist in intact and castrate male rat models. Drug Dev. Res. (2001) 52:485–491.
   Web of Science ®Google Scholar
• HAMMAN LG, HIGUCHI RI, ZHI L et al.: Synthesis and biological activity of a novel series of nonsteroidal, peripherally selective, androgen receptor antagonists derived from 1,2-dihydropyridono [5,60-quinolines. J. Med. Chem. (1998) 41:623–639.
   PubMedGoogle Scholar
• HAMMAN LG, MANI NS, DAVIS RL et al.: Discovery of a potent orally active, nonsteroidal androgen receptor agonist: 4-ethy1-1,2,3,4-tetrahydro-6-(trifluormethyl)-8-pyridino [5,60 -quino line (LG121071). J. Med. Chem. (1999) 84:3459–3462.
   Google Scholar
• ANDERSON RA, WALLACE AM, SATTAR N, KUMAR N, SUNDARAM K: Evidence for tissue selectivity of the synthetic androgen 7-a-methy1-19-nortestosterone in hypogonadal men. Clin. Endocrinol Metab. (2003) 88:2784–2793.
   Google Scholar
• VON ECKARDSTEIN S, NOW G, BRACHE Vet al.: A clinical trial of 7-a-methy1-19-nortestosterone implants for possible use as a long-acting contraceptive for men. J. Clin. Endocrinol Metab. (2003) 88:5232–5239.
   Google Scholar
• CHEN J, HWANG DJ, BOHL CE, MILLER DD, DALTON JT: A selective androgen receptor modulator for hormonal male contraception./ Pharmacol Exp. Ther. (2005) 312:546–553.
   PubMed Web of Science ®Google Scholar
• ANDERSON R, WALLACE A, WU FC: Comparison between testosterone enanthate-induced azoospermia and oligozoospermia in a male contraceptive. III. Higher 5a-reductase activity in oligozoospermic men administered supraphysiological doses of testosterone. Clin. Endocrinol Metab. (1996) 81:902–908.
   Google Scholar
• THOMPSON IM, GOODMAN PJ, TANGEN CM et al.: The influence of finasteride on the development of prostate cancer. N Engl. J. Med. (2003) 349:215–224.
   PubMed Web of Science ®Google Scholar
• MCLACHLAN RI, MCDONALD J, RUSHFORD D et al.: Efficacy and acceptability of testosterone implants, alone or in combination with a 5a-reductase inhibitor, for male hormonal contraception. Fend. Steril. (2000) 62:73–78.
   Google Scholar
• KINNIBURGH D, ANDERSON R, BAIRD D: Suppression of spermatogenesis with desogestrel pellets is not enhanced by the addition of finasteride. J. Andra (2001) 22:88–95.
   PubMed Web of Science ®Google Scholar
• O'DONNELL L, STANTON PG, WREFORD NG, ROBERTSON DM, MCLACHLAN RI: Inhibition of 5a-reductase activity impairs the testosterone-dependent restoration of spermiogenesis in adult rats. Endocrinology (1996) 137:2703–2710.
   PubMed Web of Science ®Google Scholar
• O'DONNELL L, PRATIS K, STANTON PG, ROBERTSON DM, MCLACHLAN RI: Testosterone-dependent restoration of spermiogenesis in adult rats is impaired by a 5-a-reductase inhibitor./ Andra (1999) 20:109–117.
   PubMedGoogle Scholar
• ROEHRBORN CG, BOYLE P, NICKEL JC, HOEFNER K, ANDRIOLE G: Efficacy and safety of a dual inhibitor of 5-a-reductase types I and II (dutasteride) in men with benign prostatic hypertrophy. Urology (2002) 60:434–441.
   PubMed Web of Science ®Google Scholar
• MATTHIESSON KL, AMORY JK, BERGER R, UGONI A, MCLACHLAN RI, BREMNER WJ: Novel male hormonal contraceptive combinations: the hormonal and spermatogenic effects of testosterone and levonorgestrel combined with a 5-a-reductase inhibitor or gonadotropin-releasing hormone antagonist. J. Clin. Endocrinol Metab. (2005) 90:91–97.
   PubMed Web of Science ®Google Scholar
• O'DONNELL L, ROBERTSON KM, JONES ME, SIMPSON ER: Estrogen and spermatogenesis. Endocr. Rev. (2001) 22:289–318.
   PubMed Web of Science ®Google Scholar
• DE RONDE W, POLS HAP, VAN LEEUWEN JP, DE JONG FH: The importance of oestrogens in males. Clin . Endocrinol (2003) 58:529–542.
   PubMedGoogle Scholar
• HANDELSMAN DJ, WISHART S, CONWAY AJ: Oestradiol enhances testosterone-induced suppression of human spermatogenesis. Hum. Reprod. (2000) 15:672–679.
   PubMed Web of Science ®Google Scholar
• MARTIN CW, ANDERSON RA, CHENG Let al.: Potential implications of hormonal male contraception: cross-cultural implications for development of novel preparations. Hum. Reprod. (2000) 15:637–645.
   Google Scholar
• GLASIER AF, ANAKWE R, EVERINGTON D et al: Would women trust their partners to use a male pill? Hum. Reprod. (2000) 15:646–649.
   Web of Science ®Google Scholar
• •A survey of women in Scotland, South Africa and China that indicated women thought male hormonal contraception was a good idea and would trust their partner to use it.
   Google Scholar