BEIJING China, May 16, 2025 — Gan & Lee Pharmaceuticals (hereafter referred to as “Gan & Lee”, stock code: 603087.SH) announced that the first patient has been dosed in a phase 1 clinical trial of GZR102 injection, a novel once-weekly fixed-ratio combination of basal insulin and glucagon-like peptide-1 receptor agonist (GLP-1 RA), in Chinese adult participants with overweight. This investigational therapy consists of once-weekly basal insulin (GZR4) and GLP-1 RA (bofanglutide, research code: GZR18) at a fixed ratio. Both GZR4 injection and bofanglutide injection have completed dose exploration in phase 2 clinical trials involving patients with type 2 diabetes mellitus (T2DM), demonstrating good glycemic control with favorable safety and tolerability profiles.

This randomized, double-blind, crossover phase 1 clinical study was designed to compare the safety, tolerability, pharmacokinetics (PK), and pharmacodynamics (PD) of a single dose of GZR102 injection with single doses of GZR4 injection and bofanglutide injection, respectively.

The pathophysiology of T2DM is complex. The combination of glucose-lowering agents with different mechanisms of action is beneficial for improving glycemic control and clinical outcomes in T2DM patients. The complementary mechanisms of GLP-1 RAs and basal insulin can effectively address multiple pathological defects in T2DM.At equivalent or even lower insulin doses, this combination therapy demonstrates superior glycemic efficacy compared to insulin monotherapy, while mitigating insulin-related adverse effects such as weight gain and hypoglycemia¹. Given these advantages, the combination of basal insulin and GLP-1 RA has become an increasing focus of research. The fixed-ratio combination formulations offer the benefit of reduced injection frequency to improved patient adherence, whereas free-dose combinations allow more flexible dose adjustments. Currently, only two fixed-ratio combinations of basal insulin and GLP-1 RA are available in China, both requiring once-daily administration.With ongoing advances in drug development, long-acting weekly formulations are now revolutionizing diabetes treatment paradigms. By significantly reducing injection frequency (86% fewer injections than daily regimens), once-weekly dosing can improve the treatment experience and provides important clinical value in enhancing long-term adherence².

Gan & Lee Pharmaceuticals' GZR102 injection is the first domestically developed once-weekly fixed-ratio combination of basal insulin and GLP-1 RA to enter clinical development (Class 1 New Drug) in China. Preclinical studies have demonstrated that GZR102 has a favorable safety, tolerability, and glucose-lowering efficacy. The initiation of this phase 1 trial in China marks the first-in-human clinical study for GZR102 injection. This innovative therapy offers a new treatment approach for combination therapy in diabetes management, with future clinical evidence expected to support its broader use and improve outcomes for people living with T2DM.

Reference:

1. 中国研究型医院学会糖尿病学专业委员会. 胰高糖素样肽‑1受体激动剂联合胰岛素治疗2型糖尿病专家共识（2025 版）[J]. 中华糖尿病杂志, 2025, 17(4): 421-430.DOI: 10.3760/cma. j.cn115791-20241213-00729.

2. Polonsky, W. H., Arora, R., Faurby, M., Fernandes, J., & Liebl, A. (2022). Higher Rates of Persistence and Adherence in Patients with Type 2 Diabetes Initiating Once-Weekly vs Daily Injectable Glucagon-Like Peptide-1 Receptor Agonists in US Clinical Practice (STAY Study). Diabetes therapy : research, treatment and education of diabetes and related disorders, 13(1), 175–187. https://doi.org/10.1007/s13300-021-01189-6

About GZR102 Injection
Gan & Lee Pharmaceuticals' proprietary GZR102 injection is a fixed-ratio once-weekly basal insulin/GLP-1RA combination, composed of the weekly insulin formulation GZR4 and the GLP-1RA bofanglutide (GZR18) in a fixed ratio. As a once-weekly subcutaneous formulation, GZR102 employs an innovative design to maximize the synergistic effects of both components. The insulin/GLP-1RA combination addresses multiple pathophysiological defects in T2DM, demonstrating enhanced glycemic control with reduced daily insulin requirements while mitigating adverse effects such as hypoglycemia and weight gain - positioning it as a potentially optimal therapeutic option that is effective, safe, and convenient for diabetes patients. GZR102 has now entered phase I clinical development globally.

About GZR4

Gan & Lee Pharmaceuticals' independently developed GZR4  injection is an ultra-long-acting weekly insulin preparation that is expected to provide more stable glucose-lowering effects and reduced intra- or inter-day blood glucose variability. GZR4 is anticipated to help patients with diabetes overcome injection barriers, enable earlier initiation of insulin therapy, optimize long-term diabetes management, and enhance patients' quality of life via once-weekly subcutaneous injection. Early clinical findings indicate that GZR4 demonstrates comparable reduction in HbA1c to insulin degludec in patients with inadequate glycemic control through oral antidiabetic medications. Currently, the global development of GZR4 has entered the Phase 3 clinical trial stage.

About Bofanglutide (GZR18)

Bofanglutide (R&D Code: GZR18) injection, developed by Gan & Lee Pharmaceuticals, is a bi-weekly GLP-1 receptor agonist (RA) indicated for glycemic control in adults with type 2 diabetes and body weight management in overweight/obese individuals. As the potential first bi-weekly GLP-1 RA in the world, early clinical trials have demonstrated its efficacy in weight reduction comparable to or superior to marketed counterparts, with a safety and tolerability profile consistent with the established class of GLP-1 RAs, and significant reductions in both blood glucose levels and body weight.

Forward-looking statements

Forward-looking statements are based on our expectations and assumptions as of the date of the statements. Actual results may differ materially from those expressed in these forward-looking statements due to a variety of factors, and we can give no assurance that such results will be achieved in the future. We undertake no obligation to update or revise any forward-looking statements, whether as a result of new information, future events, or otherwise.

About Gan & Lee

Gan & Lee Pharmaceuticals developed the first Chinese domestic insulin analog. Currently, Gan & Lee has six core insulin products, including five insulin analog varieties: long-acting glargine injection (Basalin^®), fast-acting lispro injection (Prandilin™), fast-acting aspart injection (Rapilin^®), mixed protamine zinc lispro injection (25R) (Prandilin™25), aspart 30 injection (Rapilin^®30), and one human insulin injection - mixed protamine human insulin injection (30R) (Similin^®30). The company has two approved medical devices in China, namely reusable insulin injection pen (GanleePen), and disposable pen needle (GanleeFine^®).

In China's 2024 National Insulin-Specific Centralized Procurement, Gan & Lee Pharmaceuticals ranked  first among all selected companies in terms of procurement demand for insulin analogs. The company is also making strides in international markets, with the disposable pen needle (GanleeFine^®) approved by the US Food and Drug Administration (FDA) in 2020 and received GMP inspection approval from the European Medicines Agency (EMA) in 2024. These achievements significantly boost Gan & Lee’s competitiveness in both international and domestic markets.

In the future, Gan & Lee will strive for comprehensive coverage in diabetes treatment. Moving forward with its mission to become a world-class pharmaceutical company, Gan & Lee will also actively develop new chemical entities and biological drugs, focusing on treatments for metabolic diseases, cardiovascular diseases, and other therapeutic areas.