Drug intelligence / Profile preview

estradiol + trimegestone

Development stage
Phase 4
Lead developer
Sanofi
Modality
Small Molecules
Administration
Oral
01

Overview

Estradiol + trimegestone is a fixed-dose combination of two hormones used primarily in menopausal hormone therapy. Estradiol is a natural estrogen that acts as an agonist at estrogen receptor alpha (ERα) and estrogen receptor beta (ERβ), alleviating vasomotor symptoms and preventing postmenopausal osteoporosis by regulating gene transcription in target tissues[3][4][5]. Trimegestone is a potent synthetic progestin (19-norpregnane derivative) with high affinity for the progesterone receptor and minimal activity at androgenic, glucocorticoid, or mineralocorticoid receptors[1][2]. In this combination, estradiol provides estrogenic effects while trimegestone counteracts the risk of endometrial hyperplasia associated with unopposed estrogen therapy. The product is indicated for the treatment of climacteric (menopausal) symptoms and prevention of post-menopausal bone loss[4][5].

Brand names
TotelleOndevaGinotexLovelleMinique
Other names
estradiol + trimegestone17-beta-estradiol + trimegestone
02

Targets

PR (Progesterone receptor)ESR1 (ERα)GPER1 (G protein-coupled estrogen receptor 1)ESR2 (ERβ)CYP2C19 (Cytochrome P450 2C19)

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