Ascletis Pharma Inc. has initiated a US Phase 1 clinical study of ASC36 oral tablets, an investigational amylin receptor peptide agonist being developed for the treatment of obesity, following Investigational New Drug (IND) clearance from the US Food and Drug Administration (FDA).

The Phase 1 study will evaluate the safety, tolerability, pharmacokinetics and pharmacodynamics of ASC36 following single and multiple ascending oral doses. The trial will enrol 86 participants with obesity (BMI ≥30.0 kg/m²) or overweight (BMI ≥27.0 kg/m²).

ASC36 was discovered and developed in-house using Ascletis’ Artificial Intelligence-assisted Structure-Based Drug Discovery (AISBDD) platform. Its oral tablet formulation was developed using the company’s proprietary Peptide Oral Transport Enhancement Technology (POTENT) for oral delivery of peptide-based medicines.

Preclinical studies have demonstrated weight-loss activity for ASC36. In non-human primates (NHPs), once-daily administration of ASC36 oral tablets for seven days resulted in up to 13.2 percent mean body-weight reduction from baseline, along with a significant reduction in food intake.

Pharmacokinetic studies in NHPs also showed absolute oral bioavailability of 6–8 percent and an elimination half-life of 116–167 hours at steady state, supporting the potential for once-daily or less frequent oral dosing.

Ascletis said ASC36 has demonstrated weight-loss efficacy in both oral and subcutaneous formulations across NHP and diet-induced obese animal models. In a head-to-head study in diet-induced obese rats, ASC36 subcutaneous injection produced greater relative body-weight reduction than comparator amylin-based therapies after seven days of treatment.

The company believes the oral formulation’s potential bioavailability and efficacy could support lower dosing requirements and provide manufacturing scalability advantages.

Jinzi Jason Wu, Ph.D., Founder, Chairman and CEO of Ascletis, said the initiation of the ASC36 Phase 1 study marks a milestone for the company’s peptide pipeline and highlights the potential of its oral peptide delivery technology.

The Phase 1 study will provide the first clinical assessment of ASC36 in humans and will generate safety and pharmacokinetic data needed to determine its further clinical development in obesity.