Drug intelligence / Profile preview

chlormadinone acetate

Development stage
Phase 4
Lead developer
Bayer
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

Chlormadinone acetate is a synthetic progestin and antiandrogen used primarily in combination with estrogens for hormonal contraception and menopausal hormone therapy. It acts as a potent agonist of the progesterone receptor (PR), a partial antagonist of the androgen receptor (AR), and a weak antagonist of the glucocorticoid receptor (GR). Its main mechanism involves suppressing ovulation by inhibiting gonadotropin secretion from the pituitary gland. Chlormadinone acetate also exhibits antiandrogenic effects by blocking androgen receptors and reducing testosterone levels. Developed in 1961 by Schering, now part of Bayer, it was withdrawn from the US market due to safety concerns but remains widely used in other countries for its contraceptive efficacy and tolerability[2][3][5].

Brand names
BelaraEstalor-21Estalor21Estalor 21C-Quens
Other names
6-chloro-Δ6-dehydro-17α-acetoxyprogesterone17α-acetoxy-6-chloro-pregna-4,6-diene-3,20-dione
02

Targets

GR (Glucocorticoid receptor)PR (Progesterone receptor)AR (Adrenergic receptors)

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