CureGene Completes First‑Participant Dose in Phase I Trial of CG‑0416, Advancing Clinical Development of Novel Oral Liver-Targeting THR-β Agonist

• Liver-targeting delivery: High intrahepatic release of active moiety to achieve low systemic exposures and minimize off-target effects in the tissues other than liver;
• Improving metabolic parameters: Significant reduction of liver fat along with favorable changes in lipid profile and glucose tolerance;
• Fat loss with muscle preservation: As a monotherapy, CG-0416 demonstrates weight-loss efficacy comparable to current GLP-1 receptor agonists (RA) (e.g., semaglutide) while preserving muscle mass. In combination with GLP-1 RA agents, CG-0416 exhibits strong synergistic effects for additional weight reduction with high quality muscle preservation.
• Non-CYP metabolism pathway: Hydrolysis-mediated activation avoids CYP450 oxidative metabolism, minimizing drug–drug interaction (DDI) and individual variability;
• High oral bioavailability: Up to 92% bioavailability with a favorable safety and tolerability profile, supporting long-term daily use.

These characteristics position CG-0416 as a promising oral therapy for chronic metabolic diseases, including obesity, metabolic dysfunction-associated steatohepatitis (MASH), etc.

Preclinical data demonstrated that CG-0416 potently activates lipid metabolism in the liver, markedly reduces liver fat accumulation, and consequently ameliorates inflammation and fibrosis. As a monotherapy, CG-0416 has a weight-loss efficacy comparable to that of mainstream GLP-1 receptor agonists but shows minimum muscle loss. When combined with GLP-1 RAs, CG-0416 exhibits a strong synergistic effect for reducing weight and improving metabolic parameters.

The FIH Phase I trial in Australia is a randomized, double-blind, placebo-controlled study in healthy participants, designed to evaluate the safety, tolerability, pharmacokinetics (PK) and pharmacodynamics (PD) of CG-0416 following single and multiple ascending doses. Leveraging Australia's well-established Phase I clinical infrastructure, this trial will generate critical data to support subsequent global development and indication expansion of CG-0416.

"The first subject dosed in our Phase I trial marks another solid step forward in CureGene's strategic expansion into cardiovascular and metabolism disease," said Dr. Gongxin He, Founder and Chief Executive Officer of CureGene. "Through continuous innovation using the prodrug technology, we are dedicated to bring safer, clinically valuable, and more convenient therapies to the patients worldwide."

About CG-0416‌

CG-0416 is a novel liver-targeted THR-β prodrug in development for MASH & obesity-related complications. Its tissue-selective activation mechanism simultaneously addresses hepatic lipid accumulation, inflammation, and fibrosis, while demonstrating superior metabolic control to resmetirom and VK-2809 in preclinical studies. As a potential oral adjunct to GLP-1 therapies, CG-0416 combines rapid fat reduction with muscle preservation, positioning it as a next-generation metabolic modulator.

About CureGene Pharmaceutical

Founded in 2018, CureGene Pharmaceutical possesses proprietary core platform technologies and independent high-efficiency innovation capabilities. The Company primarily focuses on therapeutic areas including cardiovascular & cerebrovascular diseases and antiviral therapies, striving to become a China-rooted, globally oriented innovative pharmaceutical enterprise.

Leveraging its proprietary platforms, CureGene has built a robust pipeline of innovative assets with broad market value and global independent intellectual property rights, with multiple candidates actively progressing through clinical development. Driven by its corporate mission and vision, the Company has assembled a high-caliber team of globally minded scientists and overseas returnees. Under its integrated strategic layout, CureGene achieves rapid and efficient R&D translation, with all pipeline candidates demonstrating strong potential to become first-in-class or best-in-class therapies.

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SOURCE CureGene