Beijing, China / Bridgewater, New Jersey, U.S., April 22, 2025 — Gan & Lee Pharmaceuticals (hereafter referred to as “Gan & Lee”, stock code: 603087.SH) announced that GZR102 injection, a Class 1 innovative drug independently developed by its wholly owned subsidiary, Gan & Lee Pharmaceutical Shandong Co., Ltd., has received implied approval from the National Medical Products Administration (NMPA) to initiate clinical trials for the treatment of type 2 diabetes mellitus (T2DM). GZR102 is a once-weekly fixed-ratio combination (FRC) of once-weekly basal insulin (GZR4 injection) and ultra-long-acting glucagon-like peptide-1 receptor agonist (GLP-1 RA), Bofanglutide (GZR18) injection. Both GZR4 and Bofanglutide have demonstrated strong glucose-lowering efficacy with favorable safety and tolerability profiles in completed phase 2 clinical trials for the treatment of T2DM. Currently, global development of these two monotherapies has progressed into phase 3 clinical stages.

GZR4 injection is the first domestically developed, once-weekly basal insulin analog in China. By structurally modifying the human insulin molecule, GZR4 binds strongly yet reversibly to albumin after subcutaneous injection, forming a circulating depot that enables stable and sustained insulin release, achieving effective glucose lowering throughout the week.

Bofanglutide injection is a bi-weekly GLP-1 RA indicated for the glycemic control in adults with T2DM and for body weight management in overweight or obese individuals. It is currently undergoing phase 3 clinical trials in China and phase 2 trials in the United States for obesity/overweight indication. Notably, bofanglutide is the world’s first single-target GLP-1 RA being evaluated in a head-to-head clinical study against tirzepatide to assess weight loss efficacy.

T2DM is a complex metabolic disease characterized primarily by insulin resistance and a progressive decline in β-cell function. While traditional insulin monotherapy is effective in lowering blood glucose, it often carries risks such as hypoglycemia and weight gain. Studies have shown that combining basal insulin with a GLP-1 RA can address multiple pathophysiological defects of T2DM in a complementary manner, reducing the risks associated with insulin monotherapy while enhancing glycemic control. In FRC of basal insulin and GLP-1 RA, the basal insulin component enhances glucose uptake in skeletal muscle, suppresses hepatic glycogenolysis and gluconeogenesis, thereby reducing hepatic glucose output and effectively lowering fasting plasma glucose¹. The GLP-1 RA component lowers postprandial glucose by stimulating glucose-dependent insulin secretion from pancreatic β-cells, while simultaneously inhibiting glucagon secretion from α-cells. It also slows gastric emptying, and enhances satiety via central nervous system pathways, ultimately contributing to improved glycemic control and weight management². Compared with currently marketed daily FRC formulations, GZR102’s once-weekly formulation reduces injection frequency by more than 80% annually. At present, no once-weekly FRC of basal insulin and GLP-1RA has been approved globally. As the only domestically developed once-weekly FRC in China, GZR102 has the potential to significantly improve patient adherence and enhance comprehensive treatment outcomes.

Reference:

1. Niswender KD. Basel insulin: beyond glycemia [J]. Postgrad Med, 2011, 123(4):27-37.

2. Meier JJ. GLP-1 receptor agonist for individualize treatment of type 2 diabetes mellitus [J].Nat Rev Endocrinol, 2012, 8(12):728-742

3. 中华医学会糖尿病学分会 . 中国糖尿病防治指南（2024 版）[J]. 中华糖尿病杂志, 2025, 17(1):16-139. DOI: 10.3760/cma.j.cn115791-20241203-00705.

4. American Diabetes Association Professional Practice Committee; 9. Pharmacologic Approaches to Glycemic Treatment: Standards of Care in Diabetes—2025. Diabetes Care 1 January 2025; 48 (Supplement_1): S181–S206.

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.

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.