erteberel

Erteberel is a synthetic, nonsteroidal small molecule that acts as a potent and selective agonist of the estrogen receptor beta (ERβ). It was developed by Eli Lilly for oral administration and investigated primarily for the treatment of schizophrenia—specifically targeting negative symptoms and cognitive impairment—as well as benign prostatic hyperplasia. Erteberel reached phase II clinical trials in both indications but failed to demonstrate sufficient efficacy; development has since been discontinued. The drug has also been proposed as a potential novel treatment for glioblastoma. Mechanistically, erteberel selectively activates ERβ-mediated signaling pathways with high affinity (Ki = 1.54 nM), modulating gene transcription relevant to neuronal survival and anti-tumor activity[1][2][3][5].

Brand names

Erteberel

Other names

(3aS,4R,9bR)-4-(4-hydroxyphenyl)-1,2,3,3a,4,9b-hexahydrocyclopenta[c]chromen-8-ol