"Semaglutide candidate shows superiority over Rybelsus" & "Domestic Phase 1 clinical trials targeted for next year"

Daewon Pharmaceutical has unveiled research results demonstrating that its proprietary oral drug delivery technology significantly enhances the systemic absorption efficiency of semaglutide, a key ingredient used in diabetes and obesity treatments.

In human clinical studies comparing its formulation against Novo Nordisk’s oral semaglutide treatment "Rybelsus," Daewon Pharmaceutical’s candidate showed a systemic drug exposure level up to 3.14 times higher.

Daewon Pharmaceutical announced on the 23rd that it will present two abstracts on the preclinical and human pharmacokinetic (PK) research results of its oral semaglutide candidate "DW5324" at the American Association of Pharmaceutical Scientists (AAPS) PharmSci 360 annual meeting, held in New Orleans from October 25 to 28.

Semaglutide is a GLP-1 receptor agonist utilized in blockbuster treatments such as the diabetes drug "Ozempic," the obesity treatment "Wegovy," and the oral diabetes medication "Rybelsus."

However, due to the inherent characteristics of peptide-based drugs, they are easily degraded in the gastrointestinal (GI) tract and suffer from low absorption rates, making the development of oral formulations notoriously difficult.

To overcome these hurdles, Daewon Pharmaceutical developed a proprietary drug delivery platform leveraging a polymer-lipid complex. This technology protects the drug within the harsh environment of the digestive system, controls the release timing, and simultaneously improves mucosal permeability in the gastrointestinal tract.

In this latest research, Rybelsus 14mg was compared directly with a semaglutide formulation incorporating Daewon’s proprietary platform.

Across two human pharmacokinetic crossover studies involving 18 and 19 participants respectively, the area under the curve (AUC)—representing systemic drug exposure—for Daewon’s formulation was 1.90 to 3.14 times higher than that of Rybelsus. Furthermore, the maximum plasma concentration (Cmax) increased by up to 2.9 times.

Similar promising results were confirmed in preclinical studies. In a parallel artificial membrane permeability assay (PAMPA), drug permeability was up to 6 times higher than that of the control group, while animal testing in beagle dogs demonstrated up to a 6.41-fold increase in drug exposure following a single administration.

Notably, this novel formulation does not utilize "SNAC," the absorption enhancer applied in Rybelsus.

SNAC assists in the GI absorption of semaglutide, a technology for which Novo Nordisk holds key patents. Daewon successfully differentiated its approach from existing absorption-enhancing technologies by applying an independent polymer- and lipid-based delivery system.

Nevertheless, industry experts note that while this human study evaluates the degree of drug absorption into the body, it does not inherently mean that blood sugar control or weight loss efficacy will surpass existing products. Subsequent clinical trials remain necessary to confirm actual therapeutic efficacy and safety profiles.

Building on these findings, Daewon Pharmaceutical plans to further optimize the formulation and apply for an Investigational New Drug (IND) application for Phase 1 clinical trials in South Korea by 2027. The company is also actively pursuing discussions with global pharmaceutical firms regarding technology licensing for its oral drug delivery platform.

"This study demonstrates the potential of our oral drug delivery platform to overcome the low absorption rates of peptide drugs and the patent barriers of existing technologies," said Joo-il Kim, head of Daewon Pharmaceutical’s R&D division (Vice President). "Through formulation optimization, we will accelerate product development and global technology exports while expanding the application scope of our platform."

[ⓒ Global Economic Times. 무단전재-재배포 금지]