Similar Effects to GLP-1 Injections… Average 10.5% Reduction at Highest Dosage
Domestic Companies like Ildong Pharmaceutical and D&D Pharmatech Also Developing Oral GLP-1
[Seoul=Newsis] Reporter Song Yeon-joo: Eli Lilly, a U.S. pharmaceutical company, has once again boosted market expectations by meeting evaluation criteria in clinical trials for an oral obesity treatment.
According to the pharmaceutical industry on the 27th, Eli Lilly announced on the 26th (local time) that its oral GLP-1 (glucagon-like peptide-1) agent “Opeglypron” achieved successful topline results in its third phase 3 clinical trial.
In the study “ATTAIN-2,” Opeglypron demonstrated efficacy and safety trends consistent with GLP-1 medications used as injections, meeting primary and major secondary evaluation criteria.
Opeglypron is a low-molecular-weight oral GLP-1 agent that transforms GLP-1 medications like Wegovy and Mounjaro from injectable to oral form, taken once daily.
In this study, Lilly evaluated Opeglypron among adults with obesity or overweight and type 2 diabetes. Results showed that all three doses of Opeglypron (6mg, 12mg, 36mg) met primary and key secondary evaluation metrics, demonstrating weight loss, reduction in glycated hemoglobin (A1C), and improvement in cardiovascular metabolic risk factors by the 72nd week of administration.
At the highest dosage of 36mg, an average weight reduction of 10.5% was observed, proving its efficacy over a 2.2% reduction with placebo, thereby meeting the primary endpoint.
Secondary analysis showed that the drug reduced A1C by 1.3% to 1.8% across all dosages. Additionally, 75% of participants on the highest dose of Opeglypron achieved an A1C of 6.5% or less, below the diabetes criterion defined by the American Diabetes Association.
The most common side effects were gastrointestinal-related, generally mild to moderate, including nausea, vomiting, diarrhea, constipation, and indigestion. Treatment discontinuation rates due to side effects were 6.1% (6mg), 10.6% (12mg), and 10.6% (36mg) for Opeglypron, compared to 4.6% for placebo.
Kenneth Custer, Senior Vice President at Lilly, said, “These results suggest that once-daily Opeglypron can provide meaningful weight loss and A1C reduction similar to GLP-1 injections,” adding, “We are moving urgently toward regulatory filing based on the positive data.”
If oral GLP-1 is successfully developed, it is expected to offer convenience benefits to those who have been reluctant to use self-injections.
Domestic companies are also developing oral GLP-1 obesity treatments. Ildong Pharmaceutical is conducting phase 1 clinical trials of ‘ID110521156’ through its new drug development subsidiary UNOBIA. The oral drug, based on low-molecular compounds, offers higher manufacturing efficiency than peptide-based injectable medications, facilitating mass production. The phase 1 results presented at the American Diabetes Association (ADA) in June showed reductions in blood glucose and weight, with fewer gastrointestinal side effects compared to existing GLP-1 medications across effective dosage ranges.
D&D Pharmatech’s oral GLP-1 treatment “DD02S” was licensed out to U.S.-based Metacera in 2023, and the first North American phase 1/2 patient dosing was completed last November. The focus is on increasing oral absorption through the “Oral-Lynk” peptide oral administration platform technology.
Several global pharmaceutical companies are also developing oral GLP-1. Novo Nordisk’s oral semaglutide version showed about 15% weight reduction in clinical trials. Viking Therapeutics in the U.S. is in phase 2 for its oral obesity treatment “VK2735,” a dual-acting agent targeting both GLP-1 and GIP (Glucose-Dependent Insulinotropic Polypeptide). AstraZeneca is developing the GLP-1 pill “ECC5004” (AZD5004) with China’s Echo Gene. Roche is in phase 1 for “CT-996.”