Biological Activity
Dienogest-d8 is intended for use as an internal standard for the quantification of dienogest by GC- or LC-MS. 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.
References
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 profileSteroids73(2)222-231(2008)
2.Katsuki, Y., Takano, Y., Futamura, Y., et al.Effects of dienogest, a synthetic steroid, on experimental endometriosis in ratsEur. 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 progestinsCancer79(1)169-176(1997)
