Goli Pharmaceutical-B (01672) launches phase I study in the US on the treatment of obesity with oral insulin agonist peptide ASC36

Zhitong Finance App News, Goli Pharmaceutical-B (01672) issued an announcement. After recently receiving approval from the US Food and Drug Administration (FDA) for clinical trials (IND) of new drugs, it has initiated a US phase I study on ASC36 oral tablets (oral insulin receptor agonist polypeptides) for the treatment of obesity.

This phase I study aimed to evaluate the safety, tolerability, pharmacokinetics, and pharmacokinetics of ASC36 after single dose and multiple incremental doses of oral administration in 86 obese (body mass index (BMI) ≥30.0 kg/m²) or overweight (BMI ≥27.0 kg/m²) subjects.

“In 2026, we launched four Phase I studies on the peptide pipeline. ASC36 oral tablets are the fourth and newest. This is an important milestone in the Geli peptide pipeline and further validates our proprietary POTENT oral peptide delivery technology.” Dr. Wu Jinzi, founder of Geli, Chairman of the Board and CEO, said, “ASC36 has shown encouraging weight loss results, good oral bioavailability, and a long half-life in preclinical studies. We believe an effective oral insulin receptor agonist has the potential to provide convenient and differentiated treatment options for obese people. Combining our oral small molecule and long-acting injectable programs, ASC36 further strengthens our diversified product pipeline to meet the changing treatment needs of patients with obesity and other metabolic diseases.”

ASC36 is a pancreatin receptor agonist polypeptide developed independently using Goli's proprietary Artificial Intelligence- Assisted Structure-Based Drug Discovery (AISBDD) technology. ASC36 oral tablets were developed and optimized by Culley using its proprietary Oral Peptide Transport Enhancement Technology (POTENT), which enables oral peptide delivery.

In non-human primates, 10 mg ASC36 oral tablets were administered once a day in each animal. After 7 days, absolute oral bioavailability (absolute oral bioavailability) [1] in the steady state was 8%, and the elimination half-life (elimination half-life) reached 116 hours; 25 mg ASC36 oral tablets were administered once a day in each animal. After 7 days of administration, the absolute oral bioavailability in the steady state was 6%, and the elimination half-life reached 167 hours. The long elimination half-life (116 hours to 167 hours) of ASC36 oral tablets supports once-daily and lower frequency oral administration regimens.

ASC36 oral tablets and subcutaneous injections showed significant weight loss effects in non-human primates and rat models of diet-induced obesity (DIO), respectively. In non-human primates, the average body weight decreased by up to 13.2% compared to baseline after 7 days of administration of ASC36 oral tablets once a day. ASC36 tablets also significantly reduced food intake. In a head-to-head DIO rat model, after 7 days of treatment, compared with eloralintide and petrelintide injections, ASC36 subcutaneous injections achieved a relative increase of about 32% and 91% in weight loss, respectively.

Based on potentially better oral bioavailability and efficacy, the dosage of ASC36 oral tablets is expected to be lower compared to a GLP-1R agonist polypeptide recently approved by the FDA. ASC36 polypeptide, which has a superior weight loss effect per mg, may also make it cheaper in large-scale production (advantages in manufacturing).