Selective estrogen receptor modulator (ER-Beta Agonist) targets cancer

The estrogen receptors, alpha and beta, are both responsive to endogenous estrogen, but modulate different biological processes.

Evidence suggests selective activation of ER-beta signaling may be an effective strategy for treating multiple precancerous and cancerous conditions, as well as non-cancerous conditions.

The Ohio State University’s Drug Development Institute (DDI) is developing a novel series of orally available, brain penetrant, and highly selective estrogen receptor beta agonists for use in various indications. The DDI will report in vivo efficacy results of its lead compound in multiple models of liver fibrosis, a well-established precursor to liver cancer. Benchmarked against Ely Lilly’s clinical ER-beta agonist, the DDI’s lead compound also failed to generate known side effects of the competitor’s compound.