Drug intelligence / Profile preview

mestranol

Development stage
Unknown
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

Mestranol is a synthetic estrogen and the 3-methyl ether of ethinylestradiol. It is a biologically inactive prodrug that is demethylated in the liver to form ethinylestradiol, its active metabolite. Mestranol was one of the first estrogens used in combination oral contraceptives and has also been used for menopausal hormone therapy and treatment of menstrual disorders. Its primary mechanism involves binding to and activating estrogen receptors after conversion to ethinylestradiol, leading to suppression of gonadotropins (FSH and LH), inhibition of ovulation, changes in cervical mucus viscosity, and endometrial alterations that prevent pregnancy[2][4][7]. Mestranol has also been studied as a male contraceptive but was not pursued due to unacceptable side effects[4].

Brand names
EnovidEnavidDevocinFemigenNorbiogestOrtho-NovinOrtho-NovumOvastolTranelLutedionNeconNorinylSophia
Other names
mestranol [USAN:USP:INN:BAN:JAN]mestranolo (DCIT)Estra‑1,3,5(10)‑trien‑17β‑ol, 17‑ethynyl‑3‑methoxy-
02

Targets

ESR1 (ERα)ESR2 (ERβ)

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