Drug intelligence / Profile preview

WT-IV-012

Development stage
Preclinical
Lead developer
The Ohio State University
Modality
Small Molecules
Administration
Oral
01

Overview

WT-IV-012 is a novel carborane-based selective estrogen receptor modulator (SERM) that acts as a potent and selective agonist of estrogen receptor beta (ERβ). Developed by the Ohio State University Drug Development Institute, it exhibits a Ki of 2.0 nM for human ERβ and demonstrates at least 200-fold functional selectivity for ERβ over ERα. In preclinical models of systemic lupus erythematosus (SLE), WT-IV-012 has shown efficacy comparable to prednisone in suppressing immune cell infiltration in the kidneys and heart, while also reducing proteinuria and pro-inflammatory cytokines such as IFNγ and TNFα. Its carborane-based structure is designed to provide a favorable selective estrogenic effect, potentially avoiding the pro-inflammatory or proliferative risks associated with ERα activation.

02

Targets

ESR2 (ERβ)

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