Dienogest

Dienogest is a synthetic progestin and progesterone receptor (PR) agonist (EC₅₀s = 3.4-10.5 nM in transactivation assays).¹ It is selective for PR over estrogen receptor α (ERα) and ERβ, as well as glucocorticoid and mineralocorticoid receptors (EC₅₀s = >3,000 nM for all), as well as sex hormone-binding globulin (SHBG) and cortisol-binding globulin (CBG; IC₅₀s = 900-950 and 7,970 nM, respectively, in radioligand binding assays). It also inhibits dihydrotestosterone-induced transactivation of the androgen receptor (EC₅₀s = 420.6-775 nM). Dienogest (0.1, 0.3, and 1 mg/kg per day for 21 days, p.o.) reduces lesion formation in a rat model of endometriosis.² It reduces 17β-estradiol benzoate-dependent tumor growth in an MCF-7 ovariectomized mouse xenograft model when administered at doses of 0.1 and 1 mg/kg per day for 28 days.³ Formulations containing dienogest in combination with estradiol valerate have been used as contraceptives.

WARNING This product is not for human or veterinary use.

1. Sasagawa, S., Shimizu, Y., Kami, H., et al. Dienogest is a selective progesterone receptor agonist in transactivation analysis with potent oral endometrial activity due to its efficient pharmacokinetic profile. Steroids 73(2), 222-231 (2008).

2. Katsuki, Y., Takano, Y., Futamura, Y., et al. Effects of dienogest, a synthetic steroid, on experimental endometriosis in rats. Eur. J. Endocrinol. 138(2), 216-226 (1998).

3. Katsuki, Y., Shibutani, Y., Aoki, D., et al. Dienogest, a novel synthetic steroid, overcomes hormone-dependent cancer in a different manner than progestins. Cancer 79(1), 169-176 (1997).