GRANDPHARMA's independently developed heavyweight global innovative radiolabeled conjugate drug GPN01530-2 has received Fast Track designation from the FDA

According to the news from Zhitong Finance APP, GRANDPHARMA (00512) announced that its self-developed globally innovative radiolabeled drug conjugate ("RDC") GPN01530-2 for diagnosing solid tumors has recently received Fast Track Designation ("FTD") from the U.S. Food and Drug Administration ("FDA"). The FDA established the Fast Track mechanism to accelerate and facilitate the review process for new drugs that are intended to treat serious or life-threatening diseases for which there are currently no effective treatment options and that demonstrate the potential to meet the unmet medical needs of these diseases. Candidates granted Fast Track Designation may qualify for more frequent communication with the FDA, priority review (if they meet relevant criteria), and rolling review of new drug applications, thereby speeding up the development and market launch of related drugs. Previously, GPN01530-2 had received FDA approval to conduct Phase I/II clinical studies for diagnosing solid tumors. The successful acquisition of FTD qualification marks an important milestone in the global R&D and registration layout of the group's nuclear medicine anti-tumor diagnosis and treatment sector, fully validating the group's comprehensive strength in building cutting-edge nuclear medicine technology platforms, international clinical development, and registration applications. The group will rely on the "dual application" international registration path between China and the U.S. to continuously promote the global R&D and registration work of GPN01530-2, and based on this, further deepen the global development strategy of this sector, actively promoting more self-developed innovative nuclear medicine products for international clinical research and registration applications, and continuously enhancing the group's core competitiveness and international influence in the field of nuclear medicine anti-tumor diagnosis and treatment.

GPN01530-2 is a small molecule RDC drug that targets fibroblast activation protein ("FAP"). FAP is one of the important markers of cancer-associated fibroblasts ("CAFs"), involved in processes such as extracellular matrix remodeling, tumor cell proliferation regulation, and tumor immune suppression, promoting tumor growth and invasion, making it a novel specific target for tumor diagnosis and treatment. Studies have shown that FAP is not expressed or is expressed at low levels in normal tissues but is highly expressed in 90% of epithelial tumor tissues and various tumor microenvironment CAFs. The specific targeting of FAP by GPN01530-2 provides new possibilities for the diagnosis of various malignant tumors. Currently, the commonly used PET/CT imaging agent in clinical practice is fluorine-18-fluorodeoxyglucose ("18F-FDG"), which assesses and evaluates diseases based on the level of glucose metabolism in lesions, but its sensitivity is relatively low (40%-68%), limiting its value in early tumor diagnosis. In contrast, imaging agents targeting FAP have broad application prospects for solid tumors and high sensitivity, making them one of the popular targets in radiopharmaceutical research. The GPN01530-2 developed by the group optimizes the structure of the FAP ligand, enhancing its uptake in tumor tissues while reducing its uptake in normal tissues. Preclinical research results indicate that this product exhibits rapid tumor targeting, higher tumor uptake, and superior pharmacokinetic properties compared to other FAP ligands In addition, the ongoing IIT human studies have shown that this product has good safety, rapid background clearance, strong and lasting lesion uptake, and demonstrates superior clinical image contrast and positive lesion detection rates compared to 18F-FDG. Based on existing preclinical and clinical research results, this product significantly enhances the diagnostic efficacy of FAP-targeted RDC drugs and is expected to provide a new tumor diagnostic solution for a large number of solid tumor patients.

The early research of the GPN01530-2 project was fully independently realized based on the group's radiopharmaceutical labeling platform and animal molecular imaging platform in the Chengdu nuclear medicine base, completing the labeling process development and animal imaging research in a one-stop manner. It also achieved the production and inspection release of the registration batch relying on a production line that complies with Good Manufacturing Practice (GMP). This project is also the first self-developed product to enter the FDA clinical stage since the Chengdu nuclear medicine base began operations, showcasing the excellent preclinical development and international registration capabilities of the technology platform.

Cancer is one of the leading causes of death worldwide. According to GLOBOCAN data, there were approximately 20 million new cancer cases and about 9.7 million deaths globally in 2022, with predictions that new cancer cases will approach 24 million and deaths will approach 12 million by 2030. In the foreseeable future, cancer will remain a significant public health issue threatening human health. It is widely believed that precise diagnosis and treatment are crucial for cancer prognosis; therefore, radiopharmaceuticals with integrated diagnostic and therapeutic potential have become a hot research area. Statistics show that the global radiopharmaceutical market size has increased from USD 5 billion in 2018 to USD 9.7 billion in 2024, with a compound annual growth rate (CAGR) of 11.7%. It is estimated to rise to USD 57.3 billion by 2035, with a CAGR of 17.5% from 2024 to 2035. During the same period in the Chinese market, the scale has grown from RMB 3.6 billion in 2018 to RMB 7.4 billion in 2024, with a CAGR of 13.0%. By 2035, it is expected to reach RMB 75.8 billion, with a CAGR of 23.5% from 2024 to 2035. The continuous advancement of imaging technology and radioligand therapy, along with the aging population, will sustain the rapid growth momentum of the radiopharmaceutical market. If the development of GPN01530-2 proceeds smoothly, this product is expected to become a significant breakthrough in solving the diagnostic challenges of solid tumors, reshaping the diagnostic landscape of solid tumors with significant product advantages, seizing a leading global market position, and bringing new hope to patients worldwide.

The group has achieved a comprehensive layout in the nuclear medicine anti-tumor diagnosis and treatment sector, covering multiple links such as R&D, production, distribution, and sales, with over 1,000 employees globally. Based on R&D centers in Boston and Chengdu, production bases in Boston, Frankfurt, Singapore, and Chengdu, and a sales network covering more than 50 countries and regions, the group has realized a global nuclear medicine industry chain layout.

The group has established an internationally first-class tumor interventional R&D platform and an RDC drug R&D platform. Focusing on the integrated treatment concept of tumor diagnosis and treatment, 16 innovative products have been reserved in the R&D registration stage, covering five radioactive nuclides including 68Ga, 177Lu, 131I, 90Y, and 89Zr Covering 7 types of cancers including liver cancer, prostate cancer, and brain cancer; the early research and development phase focuses on RDC drugs, with a product reserve of over 10 varieties. In terms of product types, it includes two categories of radiopharmaceuticals for diagnosis and treatment, providing patients with multiple treatment options for various indications, as well as integrated diagnosis and treatment solutions that are globally leading in anti-tumor therapies.

The global research and development of innovative products in this sector is progressing smoothly. In China, Yigantai® Yttrium [90Y] microsphere injection was successfully launched in January 2022 for the treatment of colorectal cancer liver metastasis, and in May 2025, it received approval from the China National Medical Products Administration to conduct a Phase II registration clinical trial for the treatment of unresectable HCC; globally, the innovative temperature-sensitive embolic agent GPN00289 completed the enrollment of all patients in its registration clinical study by October 2025. In terms of overseas registration, SIR-Spheres® Yttrium [90Y] microsphere injection was officially approved for a new indication in the United States in July 2025 for the treatment of unresectable HCC, marking it as the first and only selective internal radiation therapy product approved by the FDA for both unresectable HCC and colorectal cancer liver metastasis; in August 2025, it received CE mark certification in Europe for additional liver cancer indications, further promoting comprehensive coverage of this product in the treatment of unresectable liver cancer, achieving strategic expansion of market space; additionally, the group is collaborating with domestic and foreign experts to develop other indications for Yttrium [90Y] microsphere injection and will adopt an "international dual filing" registration path to accelerate the global market expansion of this product.

Currently, the group has six innovative RDCs approved to conduct registration clinical research in the nuclear medicine anti-tumor diagnosis and treatment sector, one of which has entered the NDA stage, and three have entered Phase III clinical stages, including the diagnostic product TLX591 CDx for prostate cancer, the treatment product TLX591 for prostate cancer, the diagnostic product TLX250-CDx for clear cell renal cell carcinoma, and the treatment product ITM-11 for gastroenteropancreatic neuroendocrine tumors (GEP-NETs). The group's globally innovative diagnostic radiopharmaceutical GPN02006, based on radioactive nuclide antibody conjugate technology targeting glypican-3 (GPC-3), has achieved a milestone breakthrough in investigator-initiated clinical research (IIT clinical research) conducted in China, and it won a verbal presentation at the 2025 Annual Meeting of the Society of Nuclear Medicine and Molecular Imaging (SNMMI); this product has great potential and is expected to become the world's first diagnostic RDC product targeting the GPC-3 site for hepatocellular carcinoma (HCC).

The group's radioactive drug research and production base located in Wenjiang District, Chengdu, Sichuan Province, China, was completed and accepted in April 2025, received a Class A "Radiation Safety License" issued by the Ministry of Ecology and Environment in May, and officially commenced operations at the end of June. This base is the world's first closed-loop platform for the entire nuclear medicine industry chain, covering the entire chain from "isotope preparation - nuclear drug R&D - clinical production - commercialization," forming a full lifecycle management capability from early research and development to clinical transformation to market sales, with internationally leading R&D efficiency; it has solved the "bottleneck" problem of nuclear medicine, achieving 100% independent production to break the reliance on imports, with 14 high-standard GMP production lines meeting the needs for multi-variety and large-scale preparation Establish a full-process intelligent management system, with nuclear power-grade safety and unmanned intelligent manufacturing, achieving "zero leakage" of radiation, "zero discharge" of pollution, and "zero excess" of occupational exposure, reaching the standards of top global nuclear facilities; establish a world-class R&D production quality and operation system, making it one of the most comprehensive in terms of nuclear material types and highest in automation levels in the international arena. This R&D and production base will further solidify the foundation of the group's nuclear medicine industry, accelerate the implementation of global innovative R&D pipelines, promote the high-quality development of the group's nuclear medicine industry, cultivate high-value flagship products, and lay a solid foundation for the localization of the group's radiopharmaceuticals. In the future, the group will continue to strengthen the R&D and construction of the nuclear medicine oncology diagnosis and treatment sector, enrich and improve the product pipeline and industrial layout, forming a cluster of nuclear medicine oncology diagnosis and treatment products centered around Yttrium-90 microsphere injection (易甘泰®钇 [90Y] 微球注射液), continuously solidifying the group's position as a leading enterprise in the global nuclear medicine oncology diagnosis and treatment field.

The group has always placed great importance on the R&D of innovative products and advanced technologies, focusing on patient needs, driven by technological innovation, increasing investment in global innovative products and advanced technologies to address unmet clinical needs, enriching and improving the product pipeline and industrial layout, adopting a strategy of "global operational layout and dual circulation business development," forming a new pattern of domestic and international dual circulation development that promotes and interacts with each other, fully leveraging the group's industrial advantages and R&D strength, rapidly bringing technological innovation products to market, and providing global patients with more advanced and diverse treatment options