Innovent Submits IND Application for IBI3042, the World’s First Once-Weekly Oral Small Molecule GLP-1 Receptor Agonist

On July 21, 2026, public information from the Center for Drug Evaluation (CDE) of the National Medical Products Administration indicated that the clinical trial application for IBI3042, a Class 1 innovative chemical drug submitted by Innovent Biologics, Inc., has been officially accepted. As the first oral small-molecule weekly GLP-1 formulation globally to enter the clinical application stage, the advancement of this product marks a differentiated breakthrough in long-acting oral dosage forms within China’s metabolic disease treatment pipeline, and introduces new industry variables to the competitive landscape of the domestic GLP-1 sector.

IBI3042, accepted for registration as a Class 1 new chemical drug, includes four clinical trial application records, all with an acceptance date of July 21, 2026. The applicant is Innovent Biologics, Inc.

This product was independently developed by the company and is the first long-acting oral GLP-1 candidate drug in its metabolic disease pipeline to be submitted for clinical trial approval.

IBI3042 is a novel oral small-molecule GLP-1 receptor agonist, with the core development objective of achieving once-weekly oral dosing. The intended indications cover type 2 diabetes and obesity. Unlike currently marketed and most investigational daily oral GLP-1 formulations, this product features“Long-Acting + Oral”as the core differentiating feature, with the original intent of development being to improve long-term medication adherence in patients with chronic metabolic diseases.

According to the preclinical study results presented by Innovent at the 2026 American Diabetes Association (ADA) Scientific Sessions, in hGLP-1R gene knock-in mouse models, a single dose of IBI3042 at 0.4 mg/kg sustained glucose-lowering effects for at least 7 days, demonstrating significant long-acting characteristics and a duration of action superior to that of the once-daily oral small-molecule GLP-1 drug Orforglipron.

In the diet-induced obesity (DIO) humanized mouse model, the weight loss efficacy of IBI3042 administered at 1.0 mg/kg twice weekly was comparable to that of Lilly’s Orforglipron administered at 1.5 mg/kg once daily; the 3.0 mg/kg twice-weekly dosing regimen of IBI3042 demonstrated superior weight loss outcomes. Concurrent control data showed that Orforglipron administered at 3.0 mg/kg twice weekly did not exhibit significant weight loss effects.

In the obese cynomolgus monkey model, the weight loss efficacy of IBI3042 administered once weekly at 7 mg/kg was comparable to that of Orforglipron administered once daily at 1.0 mg/kg. The groups receiving IBI3042 twice weekly at doses of 1.5 mg/kg and 4.5 mg/kg demonstrated clear dose-dependent weight loss characteristics, with the maximum weight loss observed in the 4.5 mg/kg regimen surpassing that of the once-daily dosing control group.

In the current global GLP-1 drug market, oral formulations have become a core R&D focus due to their convenience of administration. Both Novo Nordisk and Eli Lilly, the two leading companies, have launched commercialized oral GLP-1 products. Notably, Eli Lilly’s small-molecule GLP-1 receptor agonist, Orforglipron, has been approved for marketing in the United States.

To further strengthen its pipeline competitiveness, Eli Lilly acquired Insilico Medicine’s oral small-molecule GLP-1 receptor agonist for $2.75 billion in March 2026, doubling down on the development of long-acting, potent oral products, as industry competition has graduallyUpgrading from “Oral Accessibility” to “Long-Acting Optimization.”

The landscape of oral weight-loss drugs in China continues to expand, with all products currently in late-stage development being daily-dose formulations. Among these, WenTai Pharmaceuticals has submitted a marketing application for its oral weight-loss drug, while Hengrui Medicine has completed Phase III clinical trials for its oral agent targeting two indications: weight loss and glycemic control. Prior to this submission, there were no domestically developed weekly-dose oral weight-loss drugs in clinical stages in China; Innovent’s IBI3042 fills this gap in clinical-stage research.

Obesity and type 2 diabetes are both chronic conditions requiring long-term intervention, with medication adherence being one of the core factors influencing the effectiveness of long-term management. If the subsequent clinical validation of IBI3042 proceeds smoothly, its once-weekly oral dosing regimen could significantly reduce dosing frequency: compared to weekly injectable formulations, it eliminates the barriers and concerns associated with injection administration; compared to daily oral formulations, it reduces the cognitive burden of remembering daily doses. This offers patients a more convenient treatment option and presents differentiated application advantages in the long-term management of chronic metabolic diseases.

The clinical application for IBI3042 further strengthens Innovent’s product portfolio in the cardiometabolic field. Currently, its metabolic pipeline has established a multi-tiered layout: mazdutide has been approved for market launch; the once-daily oral small-molecule GLP-1 receptor agonist IBI3032 has completed Phase I clinical trials; and the company has also advanced several other candidates, including IBI3012 (a monthly GGG antibody–peptide conjugate), IBI3030 (a monthly PCSK9-GGG formulation), IBI3040 (an amylin analog), and IBI3046 (an INHBE siRNA). These assets cover diverse dosing frequencies and therapeutic targets, thereby constructing a comprehensive pipeline for the treatment of metabolic diseases.

From an industry perspective, IBI3042, as the first oral small-molecule weekly GLP-1 formulation globally to enter the clinical trial application stage, provides a new R&D pathway for domestic pharmaceutical companies to achieve differentiated competition in the GLP-1 sector, and also propels the development of oral GLP-1 drugs in China into a new phase characterized by long-acting formulations.。