PLX-1

PLX-1 is a high-affinity small-molecule radiopharmaceutical ligand designed to target Fibroblast Activation Protein (FAP). FAP is a cell-surface glycoprotein that is significantly overexpressed in cancer-associated fibroblasts (CAFs) within the stroma of many solid tumors, while showing minimal expression in healthy adult tissues. Developed by PharmaLogic, PLX-1 is primarily utilized as a diagnostic tool when radiolabeled with fluorine-18 ([18F]) for Positron Emission Tomography (PET) imaging. This allows for sensitive detection, staging, and monitoring of various cancers, including those of the pancreas, breast, and colon, by visualizing the tumor microenvironment. Beyond its diagnostic utility, the PLX-1 scaffold is being evaluated for its potential in radioligand therapy (RLT), where it could serve as a targeting vehicle for delivering cytotoxic radioisotopes directly to FAP-positive tumor sites.

Other names

FAP-targeting ligand PLX-1