Gestodene

Gestodene is a progestin.¹ It selectively binds to the progesterone receptor over the estrogen receptor.² Gestodene induces transcriptional activity mediated by the progesterone receptor, and, weakly, the androgen receptor in reporter assays.³ It increases the growth of MCF-7 cells when used at concentrations ranging from 0.1 to 1 µM.⁴ In contrast, gestodene (0.1 mg/kg) reduces tumor growth in an estrogen-dependent model of rat mammary tumors induced by DMBA (Item No. 30383). Formulations containing gestodene, in combination with ethynyl estradiol have been used as oral contraceptives.

WARNING This product is not for human or veterinary use.

1. Stanczyk, F.Z. All progestins are not created equal. Steroids 68(10-13), 879-890 (2003).

2. Pollow, K., Juchem, M., Grill, H.J., et al. Lack of binding of gestodene to estrogen receptor in human breast cancer tissue. Eur. J. Cancer 26(5), 608-610 (1990).

3. Fuhrmann, U., Slater, E.P., and Fritzemeier, K.H. Characterization of the novel progestin gestodene by receptor binding studies and transactivation assays. Contraception 51(1), 45-52 (1995).

4. Kloosterboer, H.J., Schoonen, W.G., Deckers, G.H.J., et al. Effects of progestagens and Org OD14 in in vitro and in vivo tumor models. J. Steroid Biochem. Mol. Biol. 49(4-6), 311-318 (1994).