On September 17, Geli Pharmaceutical-B(01672.HK) announced that the board of directors announced that its recent ASC30 two-phase I clinical trial conducted in the United States has completed the initial patient dosing. ASC30 is the first and only small molecule GLP-1 receptor (GLP-1R) agonist for the treatment of obesity, which can be administered either as a monthly subcutaneous injection or a daily oral dose. The ASC30 tablet and ASC30 injection were approved for new drug clinical trials (IND) by the Food and Drug Administration (FDA) in July 2024 and September 2024, respectively. The company expects to obtain the top-line data of the above two US phase I clinical trials in the first quarter of 2025.

ASC30 is a small molecule GLP-1R biased agonist (GLP-1 Rbiased small molecule agonist) independently developed by Geli, without β-arrestin recruitment. ASC30 has unique and differentiated properties, making it possible to administer it in the form of a monthly subcutaneous injection and a daily oral tablet. Through head-to-head comparison, ASC30 demonstrated 2 to 3 times higher in vitro efficacy towards GLP-1R compared to orforglipron. In non-human primate (NHPs) intravenous glucose tolerance test (IVGTT), ASC30 (dose: 1.5 mg/kg) stimulated more insulin secretion compared to orforglipron (dose: 6 mg/kg), with statistically significant differences.

In the animal model, the half-life of ASC30 injection is as long as 25 days, which supports monthly injection in the human body. In NHPs, a single subcutaneous injection of ASC30 effectively reduces weight continuously for one month compared to a certain antibody peptide conjugate drug that is injected weekly for a total of 6 times. Compared to weekly injection peptide GLP-1 drugs and monthly injection antibody peptide conjugate candidate drugs, monthly subcutaneous injection of ASC30 has the potential for strong competitive advantages (lower injection frequency and/or lower cost).

The once-daily tablet of ASC30 has superior pharmacokinetic (PK) characteristics and a more potent stimulating effect on GLP-1R, making it a potential best-in-class GLP-1R small molecule agonist. In the animal model, the half-life of ASC30 tablet is as long as 36 hours, supporting daily oral administration. In NHPs, daily oral administration of ASC30 significantly reduces weight. Utilizing Geli's proprietary technology, the steady-state relative bioavailability of ASC30 tablet reached 99% in the animal model.

In the obesity and diabetes market, both monthly injections and daily oral medications are attractive to patients for long-term weight management, lifestyle, and convenience. Patients may choose to switch from injections to oral administration, or from oral administration to injections, based on long-term weight management methods, lifestyle, and convenience. As a small molecule, ASC30 can provide both monthly injection and daily oral dose options. In addition, the ASC30 oral tablet and injection have similar or identical safety profiles, making it easy for patients to switch between the two regimens.