Drug intelligence / Profile preview

raloxifene + 17 beta-estradiol

Development stage
Phase 2
Lead developer
Eli Lilly
Modality
Small Molecules
Administration
Oral
01

Overview

**Raloxifene + 17 beta-estradiol** is a non-standardized combination of two active pharmaceuticals: **raloxifene**, a selective estrogen receptor modulator (SERM), and **17 beta-estradiol**, a natural estrogen. This combination has been studied in postmenopausal women primarily to alleviate vasomotor symptoms (menopausal hot flashes) and potentially improve endometrial safety and bone health. Raloxifene acts as an estrogen receptor agonist on bone and lipid tissue and antagonist on uterine and breast tissues, while 17 beta-estradiol acts as an agonist at estrogen receptors throughout the body. The goal of combining these drugs is to utilize the beneficial effects of estrogens (alleviating menopausal symptoms) while reducing risks associated with unopposed estrogen, such as endometrial hyperplasia, by leveraging raloxifene’s antagonistic action on endometrial tissue. Clinical studies have shown the combination more effectively reduces vasomotor symptoms than raloxifene alone, but may increase endometrial thickness and carry a low risk of endometrial hyperplasia in some patients[1][3][4].

Other names
raloxifene and 17 beta-estradiolraloxifene and estrogen combinationraloxifene HCl and 17 beta-estradiol
02

Targets

ESR1 (ERα)ESR2 (ERβ)

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