Drug intelligence / Profile preview

desogestrel + ethinylestradiol + metformin

Development stage
Preclinical
Lead developer
Organon
Modality
Small Molecules
Administration
Oral
01

Overview

Desogestrel + ethinylestradiol + metformin is a combination therapy consisting of two hormonal agents (desogestrel, a progestin; and ethinylestradiol, an estrogen) and metformin, an oral antihyperglycemic agent. This combination is primarily studied for the management of polycystic ovary syndrome (PCOS), particularly in women with metabolic disturbances such as insulin resistance. Desogestrel and ethinylestradiol act by inhibiting ovulation through suppression of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), altering endometrial lining, and increasing cervical mucus viscosity to prevent pregnancy. Metformin improves insulin sensitivity by decreasing hepatic glucose production and increasing peripheral glucose uptake. The combined use aims to address both reproductive symptoms (irregular cycles, hyperandrogenism) via hormonal regulation and metabolic features via improved insulin sensitivity[1][3][5]. Clinical studies suggest that this combination may improve endothelial function more than oral contraceptives alone in overweight women with PCOS[1], while also providing benefits on metabolic parameters such as insulin resistance compared to monotherapy[3][5].

02

Targets

PR (Progesterone receptor)ER (Estrogen receptor)ND1 (Mitochondrial electron transport chain complex I)PRKAA2 (AMPK alpha-2)

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