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Erteberel (LY500307) is a potent and selective ERβ (estrogen receptor beta) agonist (EC50 = 0.66 nM). [1]

Estrogen receptors are nuclear hormone receptors that act as a ligand-activated transcription factor. It regulates gene expression, cell proliferation and differentiation in target tissues and involved in breast cancer, endometrial cancer and osteoporosis etc. [1]

In transcription assay of cotransfected human prostate cancer cell line, Erteberel showed potency (EC50 = 0.66 nM), selectivity (32-fold) and full agonist function (>90% relative efficacy) to ERβ than to ERα. [1]

In mouse model, prostate wet weight of CD-1 mice were measured following oral daily doses of Erteberel for 7 days. Results showed reduction on prostate weight in a dose-dependent manner (0.01 mg/kg – 0.05 mg/kg), and no effect on testes/seminal vesicle weight and androgens testosterone/dihydrotestosterone circulating level. [1]

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