SOUTH SAN FRANCISCO, CA, USA I May 20, 2024 I Rila Therapeutics, Inc., A biotechnology company focused on addressing the burden of chronic fibrotic diseases, today announced that the first cohort of subjects was dosed in a phase 1 trial of RLA-23174 in China in collaboration with our development partner, Yingli Pharmaceutical. RLA-23174 is a first-in-class small molecule allosteric inhibitor of HIPK2 which inhibits TGF-β signaling to address FSGS and other fibrotic diseases. The phase 1 placebo-controlled study for RLA-23174 is designed to assess its safety at multiple dose levels, tolerability, food effect, and pharmacokinetics. The single-center trial is enrolling healthy subjects and consists of staggered single ascending dose and multiple ascending dose cohorts. The trial will enroll up to 80 patients with expected completion by the end of 3Q2024 to support advancement into the Phase 2 clinical program.

About RLA-23174
RLA-23174 is a new small molecule allosteric inhibitor of HIPK2 and a potential first-in-class treatment for pan-organ fibrosis. RLA-23174 inhibits the TGF-β/Smad3 signaling pathway by affecting the interaction between HIPK2 and Smad3, without inhibiting the kinase activity of HIPK2 or TGF-β receptor systems. Therefore, RLA-23174 exerts anti-fibrotic effects by reducing TGF-β signaling without serious adverse effects caused by complete HIPK2 or TGF-β signaling blockade. Preclinical studies have shown that RLA-23174 has superior anti-fibrotic effects, significant in vivo activity, excellent pharmacokinetic properties in animals, and a good safety profile. RLA-23174 demonstrates good druggability and excellent development potential.

“Dosing of the first cohort in this first human study with RLA-23174 is a meaningful milestone for Rila Therapeutics. It signifies our evolution into a clinical development company bringing us closer to helping patients with kidney disease,” stated Robert Drakas, Ph.D., Chief Executive Officer of Rila Therapeutics.

“Regardless of several newly approved therapies for chronic kidney disease (CKD), many patients still progress to kidney failure, requiring dialysis or transplantation. Therefore, there is an urgent need to develop more effective drugs to halt disease progression, and we strongly believe that anti-fibrosis drug is one of the most promising drugs for such therapy. We are hopeful that HIPK2 inhibitor molecules/RLA-23174 could provide additional renal protection in conjunction with the current therapies for CKD. The Initiation of the phase 1 clinical trial of RLA-23174 is an important milestone for Rila. RLA-23174 exemplifies Rila’s commitment to discovering and developing novel precision medicines for severe chronic kidney diseases,” said founder John He, MD, PhD, Chief of Nephrology at Icahn Mount Sinai and key opinion leader at one of the largest medical centers in the US. 

About Rila Therapeutics
Rila Therapeutics is focused on developing first-in-class medicines to treat fibrotic diseases. Rila was founded on exploring novel areas of biology focused on stopping fibrosis progression. Rila’s programs target key molecular pathways whose dysfunction are hallmarks of renal fibrosis. Rila is building its pipeline by leveraging insights into the dynamic process of fibrosis progression to discover and develop therapeutics with differentiating mechanisms of action against fibrotic pathways.
For more information, please visit

SOURCE: Rila Therapeutics