Ascletis Files FDA IND for ASC39, a Highly Selective Oral Amylin Receptor Agonist Aimed at Obesity Treatment

Bulletin Express10-26

Ascletis Pharma Inc. (Ascletis; HKEX: 01672) has submitted an Investigational New Drug (IND) application to the U.S. Food and Drug Administration for ASC39, an orally administered, small-molecule amylin receptor agonist intended for the treatment of obesity.

ASC39 Overview • Molecule profile: First-in-class oral small molecule designed to selectively activate the human amylin 1 receptor (hAMY1R) while sparing the human calcitonin receptor (hCTR). • In-house discovery: Built on Ascletis’ AI-assisted Structure-Based Drug Discovery (AISBDD) platform.

Selectivity and Potency Data • cAMP activation assay (head-to-head with eloralintide): – EC50 for hAMY1R: 21.4 pM (ASC39) vs. 21.2 pM (eloralintide). – EC50 for hCTR: 846.1 pM (ASC39) vs. 1,350.8 pM (eloralintide). • Resulting selectivity: 40-fold higher affinity for hAMY1R over hCTR, comparable to eloralintide’s 64-fold ratio.

Pre-clinical Efficacy and PK • Diet-induced obese (DIO) rat model: daily oral dosing of 5 mg/kg ASC39 for six days achieved a placebo-adjusted weight reduction of 6.60%. • Favorable pharmacokinetics in rats and non-human primates support a once-daily oral regimen in humans.

Strategic Positioning • Differentiator: Unlike other oral amylin programs in development that are dual amylin–calcitonin receptor agonists, ASC39 is amylin-selective, aiming to enhance both efficacy and tolerability in chronic weight control. • Pipeline integration: ASC39 is intended for use as monotherapy or in combination with ASC30, Ascletis’ oral small-molecule incretin currently in two global Phase III trials. It complements the company’s amylin peptide assets, including subcutaneous and oral candidate ASC36.

Next Steps • Ascletis plans to initiate a Phase I clinical trial of ASC39 in the fourth quarter of 2026, pending regulatory clearance.

Regulatory Note Ascletis reiterates that successful development, manufacturing or commercialization of ASC39, ASC30 and ASC36 cannot be guaranteed, in accordance with Rule 18A.05 of the Hong Kong Stock Exchange Listing Rules.

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