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GPN01530 is a fibroblast activation protein (FAP)-targeted radiopharmaceutical drug conjugate (RDC) being developed by Grand Pharma in collaboration with Serilink Biotechnology. The drug consists of a small molecule ligand designed to bind with high affinity to FAP, a cell-surface serine protease that is highly expressed on cancer-associated fibroblasts (CAFs) within the tumor stroma of various solid tumors, while remaining largely absent in normal tissues. By targeting the tumor microenvironment, GPN01530 delivers a therapeutic radioactive payload directly to the site of the tumor, aiming to induce DNA damage and cell death in both FAP-expressing stromal cells and adjacent malignant cells via the bystander effect. The program has received FDA IND approval for Phase 1/2 clinical trials in patients with solid tumors. A companion diagnostic version, GPN01530-2, is also in development for patient selection and imaging.
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