Drug intelligence / Profile preview

conjugated estrogens

Development stage
Approved
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral, Intravenous, Intramuscular, Vaginal
01

Overview

Conjugated estrogens are a standardized mixture of estrogen sulfate salts, historically derived from pregnant mare urine, with estrone sulfate and equilin sulfate among the principal components. They are systemic estrogen-replacement agents that activate estrogen receptor alpha and estrogen receptor beta, altering estrogen-responsive gene transcription in reproductive tissues, bone, vasculature, and other organs. Pfizer markets conjugated estrogens as Premarin in oral, vaginal, and intravenous formulations. Labeled uses include menopausal vasomotor symptoms, vulvar and vaginal atrophy, hypoestrogenism due to hypogonadism, castration, or primary ovarian failure, prevention of postmenopausal osteoporosis, palliative treatment of selected metastatic breast cancer and advanced androgen-dependent prostate cancer, and short-term treatment of abnormal uterine bleeding with the intravenous formulation.

Brand names
Premarin
Other names
conjugated equine estrogensCEEequine conjugated estrogens
02

Targets

ESR2 (ERβ)ESR1 (ERα)

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