Gyre Therapeutics has achieved a significant milestone by successfully dosing the first volunteer in a Phase 1 clinical trial evaluating F230, a novel endothelin A (ETA) receptor antagonist, for the treatment of pulmonary arterial hypertension (PAH). This development marks the company's strategic entry into the PAH therapeutic space, targeting a rare, progressive, and high-mortality cardiovascular condition with limited treatment options.
Novel Mechanism Targets Key PAH Pathway
F230, originally discovered by Eisai Co., Ltd. and exclusively licensed by GNI Group Ltd. to Gyre, represents a fully synthetic small molecule designed to selectively block the ETA receptor. By targeting this specific pathway, F230 is engineered to reduce pulmonary vascular remodeling and lower pulmonary pressure, which are key contributors to PAH progression.
The drug's mechanism of action addresses fundamental pathophysiological processes underlying PAH, potentially offering a new therapeutic approach for patients with this challenging condition. PAH is recognized in China's National Rare Disease Catalog, underscoring its significance in public health and the urgent need for effective treatments.
Expanding Market Opportunity in China
The Phase 1 trial represents Gyre's strategic expansion into China's growing PAH market. According to Frost & Sullivan data, China's PAH market was valued at $370 million in 2023 and is projected to grow to $480 million by 2031, indicating substantial commercial potential for effective PAH therapies.
The trial is designed to evaluate safety, tolerability, and pharmacokinetics in healthy volunteers, following standard Phase 1 protocols. This study represents the latest expansion of Gyre's fibrosis-first strategy beyond the liver, leveraging the company's robust clinical development platform and commercial infrastructure in China.
Broader Pipeline Development
F230 joins Gyre's expanding pipeline alongside lead candidate Hydronidone (F351), which recently met the primary endpoint in a pivotal Phase 3 trial for CHB-fibrosis. The company has planned a New Drug Application (NDA) submission to China's National Medical Products Administration (NMPA) for the third quarter of 2025, while also preparing for a pre-IND meeting with the U.S. Food and Drug Administration for an expected Phase 2 trial in metabolic dysfunction-associated steatohepatitis (MASH) fibrosis.
Strategic Focus on Fibrosis-First Approach
Gyre Therapeutics, headquartered in San Diego, California, maintains its primary focus on developing and commercializing Hydronidone for liver fibrosis, including MASH, in the U.S. The company's strategy builds on extensive experience in mechanistic studies using MASH rodent models and clinical studies in CHB-induced liver fibrosis.
In China, Gyre advances a broad pipeline through its indirect controlling interest in Gyre Pharmaceuticals, including therapeutic expansions of ETUARY and development programs for F573, F528, and F230. This diversified approach positions the company to address multiple fibrotic conditions across different organ systems, potentially maximizing the therapeutic impact of its fibrosis-first strategy.
