Grand Pharma’s FAP-Targeted Innovative Radionuclide-Drug Conjugate (RDC) GPN01530-2 Granted FDA Fast Track Designation

Recently, GPN01530-2, an innovative FAP-targeted radiopharmaceutical developed by Grand Pharmaceutical Group Limited (00512.HK), was granted Fast Track Designation (FTD) by the U.S. Food and Drug Administration (FDA), becoming the world’s first FAP-targeted diagnostic RDC for solid tumors to receive FDA Fast Track Designation. The designation is primarily granted to investigational drugs intended to treat serious conditions and with the potential to address unmet medical needs, with the aim of accelerating the review process for high-value drug candidates.

GPN01530-2 is a small-molecule radionuclide-drug conjugate (RDC) targeting fibroblast activation protein (FAP). FAP is not expressed or is expressed at low levels in normal tissues, but is highly expressed in 90% of epithelial tumor tissues and in cancer-associated fibroblasts (CAFs) within various tumor microenvironments. As a novel specific target for diagnosis and treatment of cancer, FAP has broad potential applications across multiple solid tumors, including lung cancer, colorectal cancer, and pancreatic cancer. By optimizing the structure of its FAP ligand, GPN01530-2 enhances uptake in tumor tissues while reducing uptake in normal tissues. Compared with other FAP-targeted products as well as 18F fluorodeoxyglucose (18F-FDG), the mainstream PET/CT imaging agent currently used in clinical practice, GPN01530-2 has demonstrated significant advantages and strong potential to become a best-in-class (BIC) product. Based on existing study findings, GPN01530-2 has demonstrated rapid tumor targeting, higher tumor uptake, and more favorable pharmacokinetic properties compared with other FAP ligands. In addition, completed investigator-initiated trial (IIT) studies in humans have shown that GPN01530-2 provides rapid background clearance and strong, sustained lesion uptake, while demonstrating superior clinical image contrast and a higher accuracy rate for detecting positive lesions compared with 18F-FDG. GPN01530-2 had previously received FDA approval to initiate Phase I/II clinical studies in the United States for the diagnosis of solid tumors. The granting of Fast Track Designation is expected to accelerate subsequent development and commercialization of this product. As the world’s first and currently only FAP-targeted diagnostic radiopharmaceutical for solid tumors to receive FTD, GPN01530-2 has received recognition from authoritative regulatory authorities for its significant clinical value and BIC development potential. This also marks a breakthrough for China’s innovative radiopharmaceuticals in the field of FAP-targeted radiopharmaceuticals, demonstrating China’s global leadership, standard synchronization, and priority access to the benefits of innovation in this cutting-edge field.

Grand Pharma will also leverage its international registration pathway involving “dual filings in China and the United States” to continue advancing the global development and registration of GPN01530-2. Building on this foundation, the Company will further deepen its global developmental strategy for its anti-tumor radiopharmaceutical sector, actively promote international clinical studies and submissions for more innovative proprietary radiopharmaceutical products, and continuously enhance its core competitiveness and international influence in the field of nuclear medicine anti-tumor diagnosis and treatment. 

About Grand Pharma

Grand Pharmaceutical Group Limited (abbr. Grand Pharma), headquartered in Wuhan, is an international pharmaceutical company focused on technological innovation, integrating radiopharmaceutical-based diagnosis and treatment of cancer, precision cardiovascular and cerebrovascular interventional diagnosis and treatment, pharmaceutical technologies, and biotechnology. Grand Pharma’s businesses cover radiopharmaceutical-based diagnosis and treatment of cancer, precision cardiovascular and cerebrovascular interventional diagnosis and treatment, respiratory and critical care, ophthalmology and otolaryngology, cardiovascular and cerebrovascular emergency care, active pharmaceutical ingredients (APIs), and high-quality amino acids. Grand Pharma continues to advance its “Go Global” global innovation strategy, building a portfolio of innovative pharmaceutical and medical device products from the United States, Australia, Germany and Belgium. The Company has established in-depth partnerships with leading pharmaceutical companies, universities, and research institutions worldwide and has developed rich and diversified product pipelines across a series of cutting-edge medical treatment fields.