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ethinylestradiol + chlormadinone acetate + metformin

Development stage
Unknown
Lead developer
Universidade de São Paulo
Modality
Small Molecules
Administration
Oral
01

Overview

This combination therapy consists of the biguanide insulin sensitizer metformin and a combined oral contraceptive containing ethinylestradiol and chlormadinone acetate. It is being investigated by the University of Sao Paulo for the management of polycystic ovary syndrome (PCOS). Metformin works by activating AMP-activated protein kinase (AMPK), which improves insulin sensitivity and reduces hyperinsulinemia-driven androgen production. Ethinylestradiol, a synthetic estrogen, increases sex hormone-binding globulin (SHBG) levels to lower free testosterone, while chlormadinone acetate, a progestin with anti-androgenic properties, acts as an antagonist at the androgen receptor. Together, these agents aim to regulate the menstrual cycle, treat clinical symptoms of hyperandrogenism such as hirsutism and acne, and improve metabolic and cardiovascular risk markers in women with PCOS.

Other names
metformin + ethinylestradiol + chlormadinone acetatemetformin + EE/CMA
02

Targets

AMPK (Adenosine monophosphate–activated protein kinase)PR (Progesterone receptor)ER (Estrogen receptor)AR (Adrenergic receptors)

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