Ascletis Pharma-B (01672) has announced the initiation of its Phase I clinical study in the United States for ASC36, an oral amylin receptor agonist peptide designed to treat obesity, following recent approval of an Investigational New Drug (IND) application by the US Food and Drug Administration (FDA).
The Phase I trial aims to evaluate the safety, tolerability, pharmacokinetics, and pharmacodynamics of ASC36 following single and multiple ascending oral doses in 86 obese (BMI ≥ 30.0 kg/m²) or overweight (BMI ≥ 27.0 kg/m²) participants.
In 2026, we initiated four Phase I studies across our peptide pipeline, with the ASC36 oral tablet being the fourth and latest, marking a significant milestone for Ascletis' peptide portfolio and further validating our proprietary POTENT oral peptide delivery technology, stated Dr. Johnny Wu, Founder, Chairman, and CEO of Ascletis. ASC36 has demonstrated encouraging weight loss efficacy, favorable oral bioavailability, and an extended half-life in preclinical studies. We believe that an effective oral amylin receptor agonist has the potential to offer a convenient and differentiated treatment option for individuals with obesity. Alongside our oral small molecule and long-acting injectable programs, ASC36 further strengthens our diversified pipeline to address the evolving treatment needs of patients with obesity and other metabolic diseases.
ASC36 is a self-developed amylin receptor agonist peptide utilizing Ascletis' proprietary structure-based AI-assisted drug discovery (AISBDD) technology. The oral tablet formulation has been optimized using Ascletis' proprietary Peptide Oral Transport Enhancement Technology (POTENT), designed to enable effective oral peptide delivery.
In non-human primates, a 10 mg oral dose of ASC36 administered once daily for seven days achieved an absolute oral bioavailability of 8% at steady state, with an elimination half-life reaching 116 hours. A 25 mg oral dose, similarly administered once daily for seven days, achieved an absolute oral bioavailability of 6% and an elimination half-life extending to 167 hours. The extended elimination half-life of ASC36 oral tablets supports once-daily or even less frequent oral dosing schedules.
Both the oral tablet and subcutaneous injection formulations of ASC36 have demonstrated significant weight reduction in non-human primates and diet-induced obesity (DIO) rat models. In non-human primates, once-daily oral administration of ASC36 for seven days led to a mean body weight reduction of up to 13.2% from baseline. The tablet also markedly reduced food intake.
In a head-to-head DIO rat model, after seven days of treatment, the subcutaneous ASC36 injection achieved relative weight loss improvements of approximately 32% and 91% compared to eloralintide and petrelintide injections, respectively. Based on potentially superior oral bioavailability and efficacy, compared to a recently FDA-approved GLP-1R agonist peptide, the ASC36 oral tablet is expected to require a lower administration dose. The per-milligram superior weight loss effect of the ASC36 peptide may also confer scalability advantages in manufacturing, resulting in lower production costs.
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