Drug intelligence / Profile preview

asoprisnil + conjugated estrogens

Development stage
Discontinued
Lead developer
TAP Pharmaceutical
Modality
Small Molecules
Administration
Oral
01

Overview

**Asoprisnil + conjugated estrogens** is a combination drug composed of asoprisnil—a selective progesterone receptor modulator—and conjugated estrogens—a mixture of estrogen hormones. Asoprisnil acts as a partial agonist and antagonist at the progesterone receptor, exhibiting tissue selectivity and direct inhibitory effects on the endometrium and leiomyoma. Clinically, asoprisnil suppresses menstruation and reduces uterine fibroid size, with minimal estrogen deprivation symptoms. Conjugated estrogens serve as estrogen replacement therapy; they act as agonists for estrogen receptors alpha and beta, thereby modulating synthesis of DNA, RNA, and proteins, leading to reduced gonadotropin-releasing hormone, follicle-stimulating hormone, and luteinizing hormone. The combination is conceptually intended for gynecological diseases, especially those involving uterine fibroids and menopause management, though there is no evidence this exact combination is approved or marketed. Asoprisnil was developed by TAP Pharmaceutical Products, while approved conjugated estrogens products are manufactured by other companies such as Pfizer[1][2][4][5][6].

Brand names
Premarin
Other names
Asoprisnil/PremarinJ867 + Premarin
02

Targets

ESR2 (ERβ)PR (Progesterone receptor)ESR1 (ERα)

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