Ascletis Develops a Revolutionary Fixed-Dose Combination for Obesity Treatment
Ascletis Develops a Revolutionary Fixed-Dose Combination for Obesity Treatment
Introduction
Ascletis Pharma Inc. has made significant strides in the clinical development of an innovative obesity treatment regimen. The company recently announced the selection of a fixed-dose combination of ASC48, a first-in-class oral small molecule GIPR agonist, and ASC30, an oral small molecule GLP-1R agonist. This combination, known as ASC30_48 FDC, aims to offer a once-daily oral solution for managing obesity, targeting both GIPR and GLP-1R pathways.
What is ASC48?
ASC48 is noteworthy for its potential as a leading-edge GIPR agonist. In scientific assays, it demonstrated an EC50 of just 1 pM in the hGIPR cAMP activation test, surpassing the potency of tirzepatide, which has an EC50 of 3 pM. Furthermore, ASC48 shows selective activity for GIPR without impacting GLP-1R or GCGR, making it a unique player in the obesity treatment landscape. The drug exhibits excellent oral bioavailability and a long half-life in rodent and non-human primate models, suggesting that it can be effectively administered once daily in human patients.
The ASC30_48 FDC Combination
The ASC30_48 FDC represents a significant advancement as a combined treatment option. Clinical trials indicated that this fixed-dose combination resulted in approximately 52% greater relative body weight reduction compared to the ASC30 monotherapy, making it an exciting development for obesity management. In head-to-head studies with non-human primates (NHPs), ASC30_48 FDC showed a remarkable improvement in body weight loss, further validating its potential efficacy.
| Group | Dosing | Total Body Weight Change | Greater Relative Body Weight Reduction |
|---|---|---|---|
| --- | ------ | ----- | --------- |
| ASC30 | 2 mg/kg PO, QD | -6.9% | NA |
| ASC48 | 5 mg/kg PO, QD | -1.7% | NA |
| ASC30_48 FDC | 2 mg/kg ASC30 and 5 mg/kg ASC48 PO, QD | -10.5% | 52% (vs ASC30) / 518% (vs ASC48) |
FDA Submission and Future Outlook
Ascletis plans to file an Investigational New Drug Application (IND) with the U.S. Food and Drug Administration (FDA) by the end of 2026 for the oral ASC30_48 FDC tablets. This submission marks an important milestone in the regulatory process and brings the company a step closer to making this innovative therapy available to those struggling with obesity.
Dr. Jinzi Jason Wu, Founder and CEO of Ascletis, expressed optimism about the upcoming clinical trials, noting the potential of the ASC48 and ASC30 combination to address the existing gaps in obesity treatment. He stated, "We believe there is an unmet medical need for an oral drug that when given in combination with GLP-1R therapy can achieve the same weight loss and tolerability as tirzepatide weekly injections."
About Ascletis Pharma Inc.
Ascletis Pharma is a fully integrated biotechnology company dedicated to developing and commercializing novel therapeutics for metabolic diseases. Leveraging its proprietary technologies, including Artificial Intelligence-assisted Structure-Based Drug Discovery (AISBDD) and Ultra-Long-Acting Platform (ULAP), Ascletis is pioneering solutions in this critical area of healthcare. Their extensive pipeline features multiple candidates, including small molecules and peptide-based therapies designed to treat obesity effectively.
For those interested in learning more about Ascletis and their initiatives, they are available at www.ascletis.com.
Conclusion
Ascletis Pharma's commitment to innovation in obesity management, embodied in the ASC30_48 FDC, represents a significant advancement in the field. As the company moves forward with its FDA submission and further clinical trials, the potential for improved therapeutic solutions for obesity is on the horizon, providing hope for those affected by this condition.
Topics Health）
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