RLA-23174

RLA-23174 is a first-in-class small molecule allosteric inhibitor of homeodomain interacting protein kinase 2 (HIPK2), developed for the treatment of chronic kidney disease (CKD), renal fibrosis, and pan-organ fibrosis. Its mechanism involves selectively inhibiting the interaction between HIPK2 and Smad3, thereby reducing TGF-β/Smad3 signaling without blocking the kinase activity of HIPK2 or TGF-β receptor systems. This selective inhibition is designed to provide anti-fibrotic effects while minimizing adverse effects associated with complete pathway blockade. Preclinical studies have demonstrated superior anti-fibrotic efficacy, significant in vivo activity, favorable pharmacokinetics, and a good safety profile. The drug is currently in Phase 1 clinical trials to assess its safety, tolerability, food effect, and pharmacokinetics in healthy subjects.

Other names

Homeodomain interacting protein kinase 2 inhibitor - Rila Therapeutics