Ascletis Announces First Participants with Obesity or Overweight Dosed in Its U.S. 12-week Phase IIa Study Evaluating Once-Monthly Subcutaneous Depot Formulation of Small Molecule GLP-1R Agonist ASC30

-          First participants with obesity or overweight with at least one weight-related comorbidity have been dosed in a U.S. 12-week Phase IIa study with once-monthly subcutaneous (SQ) depot formulation of small molecule GLP-1 receptor agonist ASC30.

-          Ultra-long-acting SQ depot formulation of small molecule ASC30 demonstrated a 36-day half-life in participants with obesity in the Phase Ib study, supporting once monthly administration.

-          Phase Ib study also demonstrated that compared to the trough concentration of ASC30 at Day 29, the ultra-long-acting SQ depot formulation showed a peak-to-trough ratio less than 2:1.

-          Topline data from the 12-week Phase IIa study of ASC30 once-monthly SQ depot formulation are expected in the first quarter of 2026.

HONG KONG, July 27, 2025 /PRNewswire/ -- Ascletis Pharma Inc. (HKEX: 1672, "Ascletis") announces today that the first participants with obesity or overweight with at least one weight-related comorbidity have been dosed in its U.S. 12-week Phase IIa study with once-monthly subcutaneous (SQ) depot formulation of small molecule GLP-1 receptor (GLP-1R) agonist ASC30 for the treatment of obesity (NCT06679959).

In the completed U.S. Phase Ib single ascending dose (SAD) study, the ultra-long-acting SQ depot formulation of small molecule ASC30 demonstrated a 36-day half-life in participants with obesity, supporting once monthly administration (Press Release). Furthermore, the U.S. Phase Ib SAD study demonstrated that compared to the trough concentration of ASC30 at Day 29, the ultra-long-acting SQ depot formulation showed a peak-to-trough ratio less than 2:1. The proprietary SQ depot slow-release formulation of ASC30 was developed by Ascletis' Ultra-Long-Acting Platform (ULAP). Utilizing this innovative platform, Ascletis has successfully designed and developed two small molecule SQ compounds for obesity with half-lives of 36 days (ASC30) and 40 days (ASC47) in participants with obesity. Ascletis' ULAP technology does not have the limitations of albumin-dependent half-life extension technology, currently being applied to many incretins, which limits half-life extension to the half-life of albumin (approximately 20 days).

In order to achieve acceptable tolerability for SQ dosing of incretin drugs, the peak-to-trough ratio during the intended dosing interval should be equal to or less than 2:1. The peak-to-trough ratios of marketed semaglutide and tirzepatide are approximately 2:1 during their intended dosing interval. Achieving optimal tolerability of a once-monthly SQ incretin requires a half-life equal to or greater than the intended dosing interval. "A half-life less than the intended dosing interval will most likely result in a peak-to-trough ratio much greater than 2:1, negatively impacting tolerability. Among incretin drugs in clinical development or with market authorizations, ASC30 once-monthly SQ depot formulation is the only once-a-month incretin with a half-life greater than the intended dosing interval." said Jinzi Jason Wu, Ph.D., Founder, Chairman and CEO of Ascletis.  

The Phase IIa study of ASC30 once-monthly SQ depot formulation is a 12-week, randomized, double-blind, placebo-controlled and multi-center study to evaluate the safety, tolerability and efficacy in participants with obesity (body mass index (BMI) ≥ 30 kg/m²) or overweight (BMI ≥ 27 kg/m² but < 30 kg/m²) with at least one weight-related comorbidity. The study consists of three cohorts of different doses, with a total of approximately 65 participants. Topline data are expected in the first quarter of 2026. 

ASC30 was discovered and developed in-house at Ascletis as a first and only investigational small molecule GLP-1R biased agonist designed to be dosed once daily orally and once monthly subcutaneously for the treatment of obesity.

About ASC30

ASC30 is an investigational GLP-1R biased small molecule agonist and has unique and differentiated properties that enable the same small molecule for both oral tablet and subcutaneous injection administrations. ASC30 is a new chemical entity (NCE), with U.S. and global compound patent protection until 2044 without patent extensions. 

About Ascletis Pharma Inc.

Ascletis Pharma Inc. is a fully integrated biotechnology company focused on the development and commercialization of potential best-in-class and first-in-class therapeutics to treat metabolic diseases. Utilizing its proprietary Artificial Intelligence-Assisted Structure-Based Drug Discovery (AISBDD) Platform and Ultra-Long-Acting Platform (ULAP), Ascletis has developed multiple drug candidates in-house, including its lead program, ASC30, a small molecule GLP-1R agonist in development as a once-daily oral tablet and once-monthly subcutaneous injection for weight management. Ascletis is listed on the Hong Kong Stock Exchange (1672.HK).

To learn more about Ascletis, please visit www.ascletis.com.

Contact：
Peter Vozzo
ICR Healthcare
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Ascletis Pharma Inc. PR and IR teams
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SOURCE Ascletis Pharma Inc.