Description
Gestrinone is a synthetic anti-progestin hormone that acts as an antagonist at estrogen and progesterone receptors and as an agonist at androgen receptors. Gestrinone is primarily used to treat endometriosis in clinical settings; it is also in clinical trials for potential use as an emergency contraceptive. This compound also exhibits some potential anticancer activity as well, downregulating expression of the progesterone receptor, estrogen receptor, and p-Src, inhibiting growth of uterine leiomyoma cells.
References
Zhu Y, Zhang T, Xie S, et al. Gestrinone inhibits growth of human uterine leiomyoma may relate to activity regulation of ERα, Src and P38 MAPK. Biomed Pharmacother. 2012 Dec;66(8):569-77. PMID: 23102719.
Wu S, Dong J, Cong J, et al. Gestrinone compared with mifepristone for emergency contraception: a randomized controlled trial. Obstet Gynecol. 2010 Apr;115(4):740-4. PMID: 20308833.
Ohno Y, Kitagawa I, Tamura H, et al. Antiestrogenic effect of gestrinone as an inhibitor of [3H]-estradiol binding to nuclear type II sites. Gynecol Obstet Invest. 1991;31(2):97-101. PMID: 2037266.
Venturini PL, Bertolini S, Brunenghi MC, et al. Endocrine, metabolic, and clinical effects of gestrinone in women with endometriosis. Fertil Steril. 1989 Oct;52(4):589-95. PMID: 2806598.
Tamaya T, Fujimoto J, Watanabe Y, et al. Gestrinone (R2323) binding to steroid receptors in human uterine endometrial cytosol. Acta Obstet Gynecol Scand. 1986;65(5):439-41. PMID: 3490730.
Kauppila A, Isomaa V, Rönnberg L, et al. Effect of gestrinone in endometriosis tissue and endometrium. Fertil Steril. 1985 Oct;44(4):466-70. PMID: 2996949.
