Yipinhong’s APH04935 wins FDA clinical clearance, as two Chinese-developed oral small-molecule GLP-1 drugs reach the marketing application stage in China.
Guangzhou Yipinhong Pharmaceutical (300723.SZ), a wholly owned subsidiary of ApicHope Pharmaceutical Group, has authorization from the U.S. Food and Drug Administration (FDA) to start clinical trials of APH04935, an innovative drug developed in-house.
According to Yipinhong, APH04935 is a highly potent, highly selective small-molecule glucagon-like peptide-1 receptor (GLP-1R) agonist. The company aims to develop it as a once-daily oral treatment for weight control and long-term weight management.
The drug received clinical trial authorization from China’s National Medical Products Administration (NMPA) in August.
Oral small-molecule weight-loss drugs are not new. Earlier examples included rimonabant, orlistat and lorcaserin, but these drugs faced questions over efficacy and side effects.
The discovery of GLP-1 as a therapeutic target, followed by the global success of semaglutide and tirzepatide, has renewed interest in oral small-molecule treatments. The most advanced candidates currently in development are largely focused on GLP-1.
Two domestic filings are already in
On April 1, Eli Lilly announced that orforglipron had received FDA approval for treating obesity or overweight in adults. It is the world’s first approved oral, nonpeptide small-molecule GLP-1 receptor agonist, marking a milestone for the drug class. The drug had already been submitted for approval in China in January.
Chinese developers have moved quickly to catch up, with the first domestically developed candidate reaching the market-application stage just six months after the first global product’s application was submitted in China.
On July 20, China’s Center for Drug Evaluation (CDE) website showed that an application for VCT-220, an oral small-molecule GLP-1 drug developed by Suzhou Wentai Pharmaceutical, which operates globally as Vincentage Pharma, had been accepted for review. Its presumed indication is weight loss.
VCT-220 was the first domestically developed small-molecule GLP-1 receptor agonist to reach the marketing application stage.
Just over a month later, on Sept. 1, the CDE disclosed that it had accepted HRS-7535, an oral small-molecule GLP-1 receptor agonist developed by Hengrui Pharmaceuticals (600276.SH) (1276.HK), for review. The presumed indication was type 2 diabetes. Two days later, a separate application for its use in weight loss was also accepted.
These are currently the only three oral small-molecule GLP-1 drugs at the marketing application stage in China: one imported product and two domestically developed candidates.
Seven leading Chinese-developed candidates
Several other Chinese-developed drugs have also made substantial progress, with some approaching regulatory submission.
Huadong Medicine (000963.SZ) has reported positive topline results from a Chinese Phase III clinical trial of HDM1002 tablets for weight management in people with overweight or obesity. The company has completed pre-NDA discussions and is preparing to formally submit a marketing application in China.
Chengdu Di’ao Pharmaceutical Group has advanced its independently developed oral small-molecule GLP-1 drug, DA-302168S tablets, into Phase III clinical development.
Structure Therapeutics (NASDAQ: GPCR), which operates in the U.S. and China, has reported Phase II clinical results for aleniglipron, also known as GSBR-1290.
Chengyi Biotech, known internationally as Eccogene, entered into an exclusive licensing agreement with AstraZeneca for its investigational oral GLP-1 receptor agonist, initially designated ECC5004 and subsequently known as elecoglipron. The drug is now advancing through a global Phase III clinical program under AstraZeneca’s leadership.
MindRank AI has signed a commercialization agreement with 3SBio (1530.HK) for MDR-001, an AI-designed oral small-molecule GLP-1 receptor agonist. Developed using MindRank’s proprietary drug discovery platform, the drug is undergoing a pivotal Phase III trial in China for adults with overweight or obesity. The agreement covers mainland China, Hong Kong and Macau, with a potential total transaction value of up to 1.75 billion yuan.
Other candidates are also progressing. Hansoh Pharmaceutical’s (3692.HK) oral GLP-1 receptor agonist HS-10501/HS-10501-2, Qilu Pharmaceutical‘s RGT-274 capsules and Salubris Pharmaceuticals‘ (002294.SZ) SAL-0112 have all reached Phase II clinical development.
GLP-1 remains the main focus
China’s small-molecule obesity drug pipeline is heavily concentrated on GLP-1 receptor agonists. The success of semaglutide and tirzepatide in treating obesity has sharply increased interest in the drug class.
Small-molecule drugs also offer potential advantages in manufacturing, storage and transportation, making them an increasingly important focus of pharmaceutical research and development.
Source:
Yaotongshe Newswire
