Dong-A ST's New Diabetes Drug Shows Blood Sugar Reduction Effect in US Phase 1b Clinical Trial

Plan to Present at the American Diabetes Association Conference This June

[Asia Economy Reporter Kim Ji-hee] Dong-A ST announced on the 8th that it confirmed the blood glucose-lowering effect in the US Phase 1b clinical trial of ‘DA-1241,’ a first-in-class new drug under development as a treatment for type 2 diabetes. The clinical results are scheduled to be presented at the American Diabetes Association meeting in June, and the abstract submission has been completed.

DA-1241 is a first-in-class new drug with a GPR119 agonist mechanism. GPR119 is a receptor present in pancreatic beta cells that, when activated, increases insulin secretion depending on the amount of glucose or lipid metabolites. DA-1241 activates this receptor to improve postprandial blood glucose without the risk of hypoglycemia.

GPR119 is also found in the small intestine and liver. When activated, it increases the secretion of GLP-1, which is involved in lipid metabolism in the small intestine, thereby inhibiting the blood transport of fat, and suppresses fatty acid biosynthesis in the liver. DA-1241 is expected to improve dyslipidemia by activating GPR119 in the small intestine and liver.

The US Phase 1b clinical trial was conducted as a repeated administration and dose-escalation study in healthy subjects and patients with type 2 diabetes. Diabetic patients took metformin along with placebo, sitagliptin, or DA-1241 at doses of 25, 50, or 100 mg once daily for 8 weeks. The clinical trial, conducted as a controlled, double-blind, randomized study, confirmed significant clinical efficacy.

In the measurement of the area under the curve of blood glucose increase to evaluate the postprandial blood glucose reduction effect due to GPR119 activation, DA-1241 100 mg (-13.8%) showed a blood glucose improvement effect similar to sitagliptin 100 mg (-9.0%) compared to before administration. The blood glucose improvement effect was also superior compared to placebo (+10.5%).

Indicators of blood glucose variability through fasting blood glucose and continuous glucose monitoring showed levels similar to sitagliptin. Notably, DA-1241 was shown to increase GLP-1 secretion upon administration, confirming the activation of the GPR119 receptor by DA-1241 in the body. Sitagliptin, on the other hand, showed a decrease in GLP-1 secretion over time after administration.

No clinically significant adverse effects were observed, and DA-1241 100 mg (-2.2%, -1.57 kg) showed a relatively higher weight reduction effect compared to placebo (-0.3%) and sitagliptin (-0.3%).

A Dong-A ST official stated, “Many pharmaceutical companies have previously developed GPR119 agonist class therapeutics focusing on their excellent blood glucose-lowering and dyslipidemia improvement effects, but failed to prove clinical efficacy. Dong-A ST has completed the US Phase 1b clinical trial by deriving candidate substances with efficacy through various derivative studies, and we will make every effort to ensure the successful development of DA-1241 in the upcoming Phase 2 clinical trial.”

This content was produced with the assistance of AI translation services.