FAP-2286

FAP-2286 is a low-molecular-weight cyclic peptide that selectively targets fibroblast activation protein (FAP), a serine protease highly expressed on cancer-associated fibroblasts (CAFs) in the tumor microenvironment but with limited expression in normal tissues. The molecule is conjugated to a tetraazacyclododecane tetraacetic acid (DOTA) chelator, enabling it to carry radionuclides such as lutetium-177 for therapeutic applications or gallium-68 for imaging. As a radiopharmaceutical, FAP-2286 delivers targeted radiation therapy or enables PET imaging of FAP-expressing tumors. Its mechanism of action involves binding and inhibiting FAP, thereby disrupting tumor growth, angiogenesis, and metastasis by targeting CAFs. Preclinical studies have shown potent antitumor activity and high selectivity for FAP over related proteases. Developed initially by 3B-Pharma and later licensed globally (excluding Europe) to Clovis Oncology, clinical development is ongoing for advanced solid tumors[1][2][4][5][6][8].