A New Class of Estrogen Receptor Beta–Selective Activators

Table 1

Classification of ERβ-Selective Compounds

	Classes of ERβ-Selective Compounds
	I. ERβ-selective binder	II. ERβ-selective activator	III. Ligand-independent ERβ selective activator
Properties	Highly selective binding to ERβ	Binds ERα and ERβ; induces a transcriptionally active form of ERβ	Does not bind ERβ selectively; activates ERβ via cellular kinases
Example compound	ERB-041	liquiritigenin (component of MF101)	3,3′-diindolylmethane (DIM)
Origin	Synthetic	Glycyrrhiza uralensis	Brassica vegetables
Ongoing or completed clinical trials	7	3	9
Conditions or indications	Interstitial Cystitis, Crohn’s Disease, Endometriosis, Rheumatoid Arthritis	Menopausal Symptoms: Hot flashes	Prostate Cancer, Cervical Dysplasia, Cervical Cancer, Breast Cancer, Papilloma