Mestranol is a synthetic estradiol found in oral contraceptive pills for contraception and the treatment of other conditions in the female reproductive system, such as dysmenorrhea and dysfunctional uterine bleeding. The 3-methyl ether of ethinyl estradiol.
- Mechanism
- Curator reviewed
Mestranol is the 3-methyl ether of ethinylestradiol. Ethinylestradiol, is a synthetic derivative of estradiol. Ethinylestradiol is orally bio-active and the estrogen used in almost all modern formulations of combined oral contraceptive pills. It binds to (and activates) the estrogen receptor. Mestranol is a biologically inactive prodrug of ethinylestradiol to which it is demethylated in the liver with a conversion efficiency of 70%.
Estrogens diffuse into their target cells and interact with a protein receptor. Target cells include the female reproductive tract, the mammary gland, the hypothalamus, and the pituitary. Estrogens increase the hepatic synthesis of sex hormone binding globulin (SHBG), thyroid-binding globulin (TBG), and other serum proteins and suppress follicle-stimulating hormone (FSH) from the anterior pituitary. The combination of an estrogen with a progestin suppresses the hypothalamic-pituitary system, decreasing the secretion of gonadotropin-releasing hormone (GnRH).
- Primary indication
- Mestranol was used as one of the first oral contraceptives.Curator reviewed · 6 structured indications
- Formula / weight
- C21H26O2 · 310.4299 g/mol (avg)
- First approval
- Canada, 1999 · United States, 1967
- Code names
- 33355
Resolves to
IMSSROKUHAOUJS-MJCUULBUSA-NSMILES[H][C@@]12CC[C@@](O)(C#C)[C@@]1(C)CC[C@]1([H])C3=C(CC[C@@]21[H])C=C(OC)C=C3What you can answer from here — as of September 23, 2026
Which drugs share a target with Mestranol, and which of those have an active Phase 3 trial?
Create a free account or log in to explore the full data card.
Create Account