Rila Therapeutics Begins Phase 1 Trial of HIPK2 Inhibitor RLA-23174 for Chronic Kidney Disease and Fibrosis

SOUTH SAN FRANCISCO, Calif., May 20, 2024 -- Rila Therapeutics, Inc., a biotechnology firm dedicated to combating chronic fibrotic diseases, has announced a significant milestone in its research endeavors. The company's first cohort in a phase 1 clinical trial of RLA-23174 has been dosed in China, in partnership with Yingli Pharmaceutical. RLA-23174 is a pioneering small molecule that acts as an allosteric inhibitor of HIPK2, aiming to disrupt TGF-β signaling, which is a key player in fibrotic diseases such as FSGS.

The phase 1 trial is a placebo-controlled study focused on evaluating the safety, tolerability, food effects, and pharmacokinetics of RLA-23174 at various dosages. This single-center trial is currently enrolling healthy volunteers and includes both single ascending dose and multiple ascending dose cohorts. The study aims to enroll up to 80 participants, with completion anticipated by the end of the third quarter of 2024. Successful results will pave the way for subsequent phase 2 clinical trials.

RLA-23174 is designed to be a breakthrough treatment for fibrosis affecting multiple organs. Unlike other inhibitors that fully block HIPK2 or TGF-β receptor activities, RLA-23174 targets the interaction between HIPK2 and Smad3 without halting the kinase function of HIPK2 or the TGF-β receptor systems. This selective inhibition allows RLA-23174 to reduce TGF-β signaling, leading to anti-fibrotic effects while minimizing severe adverse reactions. Preclinical evaluations have demonstrated the compound's excellent anti-fibrotic effects, high in vivo activity, favorable pharmacokinetic properties in animal models, and a strong safety profile, making RLA-23174 a promising candidate for further development.

The successful dosing of the first cohort marks a pivotal moment for Rila Therapeutics. Robert Drakas, Ph.D., Chief Executive Officer of Rila Therapeutics, expressed that this milestone signifies the company's transition into a clinical development entity, bringing it closer to offering relief to patients with kidney diseases. Despite recent advancements in chronic kidney disease (CKD) treatments, a substantial number of patients still progress to kidney failure, necessitating dialysis or transplantation. This underscores the urgent need for more effective therapies to halt disease progression.

John He, MD, PhD, founder of Rila Therapeutics and Chief of Nephrology at Icahn Mount Sinai, highlighted the potential of RLA-23174 to provide additional renal protection alongside existing CKD therapies. He emphasized that the initiation of this phase 1 clinical trial demonstrates Rila's commitment to discovering and developing innovative precision medicines for severe chronic kidney diseases.

Rila Therapeutics, founded to explore new biological avenues in halting fibrosis progression, focuses on developing first-in-class medications to combat fibrotic diseases. The company's research targets key molecular pathways whose dysfunction is a hallmark of renal fibrosis. By leveraging insights into fibrosis progression, Rila is building a robust pipeline of therapeutics with unique mechanisms of action against fibrotic pathways.

This milestone for Rila Therapeutics heralds a new era in the treatment of chronic fibrotic diseases, particularly CKD, offering hope for more effective interventions that could significantly improve patient outcomes.

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