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OncoFAP is an ultra-high-affinity small organic ligand that targets fibroblast activation protein (FAP), a cell surface antigen overexpressed in more than 90% of epithelial cancers, including breast, colorectal, ovarian, lung, skin, prostate, and pancreatic cancers as well as some soft tissue and bone sarcomas. OncoFAP serves as a modular platform for the development of various therapeutic and diagnostic agents by conjugation to different payloads such as cytotoxic drugs (e.g., monomethyl auristatine E), radiolabels (e.g., lutetium-177 or gallium-68), or immune modulators (e.g., TLR agonists). The mechanism of action involves highly selective binding to FAP in the tumor stroma; when used in drug conjugates like OncoFAP-GlyPro-MMAE, proteases in the tumor microenvironment cleave the linker to release active cytotoxic agents directly at the tumor site. This approach enables potent anti-tumor activity with minimal off-target toxicity. OncoFAP-based products are being developed for imaging and treatment of solid tumors and are currently undergoing preclinical studies and early-phase clinical trials[1][2][3][4][5][6].
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