Drug intelligence / Profile preview

norethynodrel

Development stage
Discontinued
Lead developer
Pfizer
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

Norethynodrel (also spelled noretynodrel) is a synthetic progestin, structurally related to 19-nortestosterone, and was the progestin component of the first marketed oral contraceptive. It was primarily used in combination with the estrogen mestranol for contraception and in the treatment of gynecological disorders such as functional uterine bleeding and endometriosis. Norethynodrel acts as a progestogen agonist with very weak estrogenic activity. Due to its rapid metabolism and low receptor affinity, it is considered a prodrug that is quickly converted into active metabolites after oral administration—possibly including norethisterone—though this remains debated. The drug has been discontinued and is no longer marketed or used medically[1][2][4][6][7].

Brand names
Enovid
Other names
noretynodrel
02

Targets

ESR2 (ERβ)ESR1 (ERα)PR (Progesterone receptor)

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