BioAge Labs, a clinical-stage biotechnology company based in Emeryville, California, has announced the initiation of a Phase 1 clinical study of BGE-102, an orally available, brain-penetrant small molecule NLRP3 inhibitor being developed for the treatment of obesity.

NLRP3 is a key driver of age-related inflammation and has been linked to a broad range of diseases, including neurodegenerative conditions and cardiovascular disease, as well as metabolic disorders such as obesity. BioAge identified NLRP3 as a promising therapeutic target for metabolic and age-related diseases and collaborated with Shanghai-based company HitGen to develop novel inhibitors.

BGE-102 was developed by BioAge from hit compounds identified in a screen using HitGen's DEL libraries. The companies first reported the successful identification of these compounds in April 2021, followed by a joint publication in Bioorganic & Medicinal Chemistry Letters in February 2024. Their partnership has also led to joint patent filings covering the structurally novel compounds discovered through the DEL platform.

Kristen Fortney, CEO and co-founder of BioAge, commented, "We're excited to reach this important clinical milestone with BGE-102. HitGen's DEL platform helped us identify structurally distinct NLRP3 inhibitors with a novel binding site and strong potency and brain penetration. Our collaboration demonstrates the value of combining HitGen's cutting-edge screening technology with insights from human aging biology to advance potentially transformative treatments for metabolic diseases."

The trial initiation also triggers an undisclosed milestone payment to HitGen under the companies’ collaboration agreement.

HitGen CEO Dr. Jin Li stated, "We extend our congratulations to the BioAge team on this exciting progress. The advancement of BGE-102 into clinical studies not only validates the power of HitGen's DEL platform to discover novel small molecules against challenging targets, but also reinforces the value of our partnership model. We look forward to continuing our collaboration and following the development of this promising candidate."

In preclinical studies, BGE-102 demonstrated significant weight-loss effects as both monotherapy and in combination with GLP-1 receptor agonists. Initial data from the Phase 1 single-ascending dose (SAD) trial are expected by the end of this year.