Gestodene(SHB 331;WL 70) is a progestogen hormonal contraceptive.Target: Estrogen Receptor/ERRGestodene is androgenically neutral, meaning that contraceptive pills containing gestodene do not exhibit the androgenic side effects (e.g. acne, hirsutism, weight gain) often associated with second-generation contraceptive pills, such as those containing levonorgestrel. When 40 micrograms of gestodene was taken, six out of seven women did not ovulate, and one out of seven had a cycle with luteal insufficiency. These data indicate that 40 micrograms of gestodene is the borderline dose for inhibition of ovulation. A combination of 75 micrograms gestodene with 30 micrograms ethinyl estradiol was found to inhibit ovulation in ten subjects, and no follicular maturation was noted [1]. gestodene bound with high affinity to the progesterone receptor, as did other synthetic and natural progestogens. However, gestodene did not bind to the estradiol receptor. The relative binding affinities of all tested synthetic and natural ligands showed no organ-specific differences and no differences between neoplastically transformed and normal tissues [2].Clinical indications: Female contraception
References:
[1]. Spona, J. and J. Huber, Pharmacological and endocrine profiles of gestodene. Int J Fertil, 1987. 32 Suppl: p. 6-14.
[2]. Pollow, K., et al., Lack of binding of gestodene to estrogen receptor in human breast cancer tissue. Eur J Cancer, 1990. 26(5): p. 608-10.