Drug intelligence / Profile preview

norethynodrel + mestranol

Development stage
Phase 3
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

**Norethynodrel + mestranol** is the first approved combined oral contraceptive pill (COCP), consisting of the progestin norethynodrel and the estrogen mestranol. It acts primarily by suppressing gonadotropins through estrogenic and progestational activities, inhibiting ovulation, and secondarily altering cervical mucus and endometrial receptivity to prevent pregnancy. Initially developed by G.D. Searle & Company and approved by the FDA in 1957 for menstrual disorders, it gained contraceptive indication in 1960; various formulations ranged from 2.5-10 mg norethynodrel with 0.075-0.15 mg mestranol, though higher early doses were linked to thromboembolic risks, prompting dose reductions in modern equivalents.[1][3][4]

Brand names
Norinyl 1/50
Other names
mestranol/norethynodrelnorethindrone and mestranol
02

Targets

ER (Estrogen receptor)PR (Progesterone receptor)AR (Adrenergic receptors)

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