Oral Small Molecule Amylin Receptor Agonist ASC39 Demonstrated Eloralintide-like Amylin Selectivity and Efficacy in Preclinical Models - Thailand PR News

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# Oral Small Molecule Amylin Receptor Agonist ASC39 Demonstrated Eloralintide-like Amylin Selectivity and Efficacy in Preclinical Models

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  Published on 17 March 2026 #####  Author

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![](https://mma.prnasia.com/media2/2935737/Ascletis_Pharma_Logo.jpg?p=medium600 "logo")*– In a head-to-head cyclic adenosine monophosphate (cAMP) activation assay vs. eloralintide, oral small molecule amylin receptor agonist ASC39 demonstrated similar selectivity and potency to that of eloralintide. EC50*  *for human amylin 1 receptor (hAMY1R) was 21.4 pM and 21.2 pM for ASC39 and eloralintide, respectively. EC50 for human calcitonin receptor (hCTR) was 846.1 pM and 1,350.8 pM for ASC39 and eloralintide, respectively. These data indicate ASC39 and eloralintide have similar selectivity for hAMY1R over hCTR.*

*– In a head-to-head diet-induced obese (DIO) rat study vs. eloralintide, efficacy of ASC39 oral dosing was comparable to that of eloralintide, demonstrating significant placebo adjusted weight loss of 6.6% and 5.6% for ASC39 and eloralintide, respectively.*

*– Submission of an Investigational New Drug Application (IND) to the U.S. Food and Drug Administration (FDA) for ASC39 oral tablets is expected in the third quarter of 2026.*

HONG KONG, March 17, 2026 /PRNewswire/ — Ascletis Pharma Inc. (HKEX: 1672, "Ascletis") announces that it has selected ASC39, a potent and amylin-selective oral small molecule amylin receptor agonist, as a clinical development candidate. Ascletis expects to submit an Investigational New Drug Application (IND) to the U.S. Food and Drug Administration (FDA) for ASC39 oral tablets for the treatment of obesity in the third quarter of 2026.

ASC39 has a unique chemical scaffold that was discovered in-house utilizing Ascletis’ Artificial Intelligence-assisted Structure-Based Drug Discovery (AISBDD) technology. In a head-to-head cyclic adenosine monophosphate (cAMP) activation assay comparing ASC39 to eloralintide, EC50 (half maximal effective concentration) for human amylin 1 receptor (hAMY1R) was 21.4 pM and 21.2 pM for ASC39 and eloralintide (an amylin peptide analog), respectively. EC50 for human calcitonin receptor (hCTR) was 846.1 pM and 1,350.8 pM for ASC39 and eloralintide, respectively. These data indicate that ASC39 is highly selective for hAMY1R over hCTR with comparable selectivity to eloralintide. ASC39 and eloralintide were 40-fold and 64-fold, respectively more selective for hAMY1R over hCTR.

In a head-to-head diet-induced obese (DIO) rat study, compared with placebo (vehicle)-treated obese rats, oral daily administration of ASC39 resulted in statistically significant weight loss which was comparable to eloralintide (Table 1). Once-daily oral administration of 5 mg/kg ASC39 for 6 consecutive days produced significant placebo adjusted weight loss of 6.6%. Once-every-three-day subcutaneous (SQ) administration of 3 nmol/kg eloralintide for 6 consecutive days produced significant placebo adjusted weight loss of 5.6%, which is consistent with the literature data\[1\] .

Table 1. Once-daily oral administration of ASC39 for 6 consecutive days produced statistically significant body weight reduction, with an efficacy comparable to that of eloralintide.

Group

Dosing

Total body weight change

from baseline

Obese rats treated with vehicle

Vehicle,

PO, QD

0.6 %

Obese rats treated with eloralintide

3 nmol/kg,

SQ, Q3D

-5.0%

(*p*&lt;0.0001 vs

obese rats treated with vehicle)

Obese rats treated with ASC39

5 mg/kg,

PO, QD

-6.0%

(*p*&lt;0.0001 vs

obese rats treated with vehicle)

*Notes:*

a. SQ: subcutaneous; PO: oral administration; Q3D: once every 3 days; QD: once daily.

b. The body weight on Day 1 was set as the baseline.

c. Obese rats: diet-induced obese rats.

ASC39 demonstrated favorable pharmacokinetic profiles in rats and non-human primates (NHPs), supporting once-daily oral dosing in humans.

"Ascletis is committed to developing treatment options for patients living with obesity," said Jinzi Jason Wu, Ph.D., Founder, Chairman and CEO of Ascletis. "As such, we are excited to be advancing the first oral small molecule eloralintide-like selective amylin receptor agonist into the clinic later this year. We believe ASC39 may provide efficacy and safety similar to Eli Lilly’s eloralintide with the patient convenience and commercial scalability of a once-daily oral small molecule."

ASC39, a potent and amylin-selective oral small molecule amylin receptor agonist, is being developed as a monotherapy and in combination with ASC30, Ascletis’ oral small molecule, Phase III ready GLP-1, for the treatment of metabolic diseases including obesity. This new oral small molecule amylin is in addition to Ascletis’ current amylin peptide portfolio that includes ASC36, a once-monthly to once quarterly SQ amylin peptide for monotherapy and a fixed dosed combination of ASC36 and once-monthly ASC35, a GLP-1/GIP SQ peptide.

\[1\] Briere DA, Qu H, Lansu K, et al. Eloralintide (LY3841136), a novel amylin receptor agonist for the treatment of obesity: From discovery to clinical proof of concept. Mol Metab. 2025;102:102271. doi:10.1016/j.molmet.2025.102271

**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) and Ultra-Long-Acting Platform (ULAP) technologies as well as Peptide Oral Transport ENhancement Technology (POTENT), Ascletis has developed multiple drug candidates in-house, including both small molecules and peptides, such as its lead program, ASC30, a small molecule GLP-1R agonist designed to be administered once daily orally and once monthly to once quarterly subcutaneously as a treatment therapy and a maintenance therapy for chronic weight management; ASC36, an amylin receptor peptide agonist, ASC35, a once-monthly subcutaneously administered GLP-1R/GIPR dual peptide agonist and ASC37, a GLP-1R/GIPR/GCGR triple peptide agonist, and ASC39, a potent and amylin-selective oral small molecule amylin receptor agonist, for chronic weight management. Ascletis is listed on the Hong Kong Stock Exchange (1672.HK).

For more information, please visit [www.ascletis.com](https://www.ascletis.com/).

Contact:
Peter Vozzo
ICR Healthcare
443-231-0505 (U.S.)
<Peter.vozzo@icrhealthcare.com>

Ascletis Pharma Inc. PR and IR Teams
+86-181-0650-9129 (China)
<pr@ascletis.com><ir@ascletis.com>

[Source link ](http://www.prnasia.com/story/archive/4911869_AE11869_0?rand=89749)

```
This content was prepared by our news partner, Cision PR Newswire. The opinions and the content published on this page are the author’s own and do not necessarily reflect the views of Siam News Network
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