Drug intelligence / Profile preview

estriol + trimegestone

Development stage
Preclinical
Lead developer
Evestra
Modality
Small Molecules
Administration
Oral, Vaginal (via Ring)[7]
01

Overview

Estriol + trimegestone is a combination drug consisting of estriol, a naturally occurring estrogen, and trimegestone, a synthetic progestin (progestogen). This combination is designed for use in hormone therapy regimens, particularly for menopausal symptoms and potentially as hormonal contraception. Estriol acts primarily as an agonist at estrogen receptors to alleviate vasomotor symptoms and urogenital atrophy associated with menopause. Trimegestone is a potent agonist of the progesterone receptor with weak antiandrogenic and antimineralocorticoid activity; it counteracts the proliferative effects of estrogens on the endometrium, reducing the risk of endometrial hyperplasia. The combination may be administered orally or via vaginal ring delivery systems. While combinations of trimegestone with other estrogens (notably estradiol) are approved for menopausal hormone therapy in Europe and Latin America, specific products containing estriol + trimegestone have been described in patent literature for potential use in contraception and menopausal cycle disorder management[7][1][2].

02

Targets

ESR1 (ERα)GR (Glucocorticoid receptor)RB1 (Retinoblastoma-associated Protein)ESR2 (ERβ)PR-A (Progesterone Receptor A)AR (Adrenergic receptors)MR (Mineralocorticoid receptor)

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