OSU-ERβ-12 is a highly selective estrogen receptor beta (ERβ) full agonist which is under investigation for potential medical use, such as treatment of fibrosis.
Pharmacology While OSU-ERβ-12 displays only a 3-fold binding selectivity for ERβ over the estrogen receptor alpha (ERα), it shows more than a 100-fold functional selectivity for ERβ over ERα, with EC50Tooltip half-maximal effective concentration values of 19–78 nM and 3,828–30,000 nM, respectively. The drug shows good drug-like properties and had superior pharmacokinetic properties to those of the earlier ERβ agonist erteberel (LY-500307) in preclinical research. It produces anti-fibrotic effects in rodents.
Chemistry The chemical synthesis of OSU-ERβ-12 has been described. Various analogues of OSU-ERβ-12 have been described. OSU-ERβ-12 has an unusual para-carborane chemical structure.
History It was first described in the scientific literature by 2020. The drug was developed by W. Tjarks and colleagues at Ohio State University.
See also List of investigational sex-hormonal agents § Estrogenics Estrogen receptor beta § Agonists
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