Ascletis Pharma-B (01672) has announced that it has submitted an Investigational New Drug (IND) application to the U.S. Food and Drug Administration (FDA) for ASC39 oral tablets.
ASC39 oral tablets are an oral small molecule selective amylin receptor agonist intended for the treatment of obesity. ASC39 possesses a unique chemical scaffold that was independently discovered by Ascletis using its structure-based AI-assisted drug discovery (AISBDD) technology.
In a head-to-head cyclic adenosine monophosphate (cAMP) activation assay comparing ASC39 with eloralintide, the EC50 (half-maximal effective concentration) values of ASC39 and eloralintide (a selective amylin peptide analog) against the human amylin type 1 receptor (hAMY1R) were 21.4 pM and 21.2 pM, respectively. The EC50 values of ASC39 and eloralintide against the human calcitonin receptor (hCTR) were 846.1 pM and 1,350.8 pM, respectively.
These data indicate that ASC39 is highly selective for hAMY1R over hCTR, and that the selectivity of ASC39 for hAMY1R is comparable to that of eloralintide. The selectivity of ASC39 and eloralintide for hAMY1R over hCTR was 40-fold and 64-fold higher, respectively.
In a head-to-head diet-induced obesity (DIO) rat study, once-daily oral administration of 5 mg/kg of ASC39 for 6 consecutive days produced a significant placebo-adjusted body weight reduction of 6.6% compared with obese rats receiving placebo. For more information on efficacy in preclinical models, please refer to the company's announcement dated March 17, 2026.
ASC39 has demonstrated favorable pharmacokinetic profiles in rats and non-human primates, supporting once-daily oral dosing in humans.
"ASC39 is currently the only oral small molecule selective amylin receptor agonist in development that selectively targets the amylin receptor rather than the calcitonin receptor. Unlike non-selective dual-target agonists, it can replicate the pharmacological properties of eloralintide. We believe that amylin selectivity will become a key driver of efficacy and tolerability in long-term weight management," said Dr. Wu Jinzi, Founder, Chairman of the Board, and Chief Executive Officer of Ascletis. "Following the progress of our Phase III incretin candidate ASC30, the IND submission for our non-incretin candidate ASC39 represents another important milestone for Ascletis and expands our oral metabolic disease pipeline beyond incretins."
ASC39 is a potent oral small molecule amylin receptor agonist selective for amylin, being developed both as a monotherapy and in combination with ASC30 (Ascletis's oral small molecule currently undergoing two pivotal global Phase III studies) for the treatment of metabolic diseases including obesity.
This novel oral small molecule selective amylin receptor agonist further expands Ascletis's existing amylin peptide pipeline, which includes ASC36 (a quarterly subcutaneous injection and weekly oral amylin agonist peptide).
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