Development

Gan & Lee advances once-weekly oral GLP-1 peptide into Phase I

Edited by Robert McTiernan··2 min read
Gan & Lee advances once-weekly oral GLP-1 peptide into Phase I

China-based Gan & Lee Pharmaceuticals Co., Ltd. has dosed the first participant in a Phase I study of GZC8072, an oral peptide glucagon-like peptide-1 receptor agonist (GLP-1 RA) engineered for once-weekly administration. The candidate targets type 2 diabetes mellitus (T2DM) and weight management in people with obesity or overweight, and its entry into clinical testing adds to a field of oral GLP-1 agents.

The study CTR20263271 is a multicenter, randomized, double-blind, placebo-controlled Phase I trial enrolling 112 participants. A single ascending dose (SAD) portion will evaluate safety and tolerability in healthy adults; a multiple ascending dose (MAD) portion will enroll participants with overweight or obesity. Primary endpoints cover safety and tolerability; pharmacokinetic and pharmacodynamic data will also be collected.

GZC8072 is built on two proprietary platforms Gan & Lee calls NovaPeptide, intended to extend peptide half-life and support manufacturing, and SupOraTide, designed to improve oral bioavailability. The company said the combination yields enhanced intrinsic GLP-1 receptor activity, a prolonged pharmacokinetic half-life, and sufficient oral absorption to support weekly dosing. GZC8072 sits alongside bofanglutide (GZR18), a biweekly injectable GLP-1 RA currently in Phase III trials in China and Phase II in the US, and Insulin Ludefen (GZR4), an ultra-long-acting weekly basal insulin analog.

GLP-1 is an incretin hormone secreted from intestinal L-cells that stimulates glucose-dependent insulin secretion, suppresses glucagon, delays gastric emptying, and acts centrally to reduce appetite. Its plasma half-life of roughly one to two minutes, owing to rapid cleavage by dipeptidyl peptidase-4 (DPP-4), makes native GLP-1 clinically unusable without structural modification. Approved peptide GLP-1 RAs extend half-life through fatty acid conjugation enabling albumin binding — the basis for semaglutide's approximately 160-hour half-life — or through other stabilisation strategies. GZC8072 applies a distinct proprietary approach to achieve weekly oral dosing, though preclinical pharmacokinetic data have not been publicly disclosed.

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Oral semaglutide (Rybelsus), approved for T2DM, relies on the absorption enhancer sodium N-[8-(2-hydroxybenzoyl) aminocaprylate (SNAC) and requires fasting administration with limited water. The US FDA approved oral semaglutide tablets under the Wegovy brand for obesity management on December 22, 2025. Eli Lilly and Company's orforglipron (Foundayo), a non-peptide small-molecule GLP-1 RA, received FDA approval in April 2025.

Notably, Innovent Biologics’ IBI3042, an oral non-peptide small-molecule GLP-1 receptor agonist also designed for once-weekly dosing that entered Phase I development in September 2026. IBI3042 also entered first-in-human testing earlier this month. GZC8072 therefore enters an emerging race to establish whether weekly oral GLP-1 dosing can be achieved, although its peptide-based approach distinguishes it from Innovent’s small-molecule strategy.

Weekly oral dosing could differentiate GZC8072 from currently approved daily oral GLP-1 therapies, while retaining a peptide-based pharmacology distinct from small-molecule agonists such as orforglipron. Real-world adherence to injectable GLP-1 RAs at six months has been reported at 58–69%, supporting the rationale for more convenient oral formulations. Whether GZC8072's proprietary delivery platforms achieve bioavailability sufficient to produce clinically meaningful receptor engagement will be the central question Phase I pharmacokinetic data must answer.

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