FAPα inhibitor

FAPα inhibitors (FAPIs) are a class of small-molecule compounds designed to target and inhibit Fibroblast Activation Protein alpha (FAPα), a type II transmembrane serine protease. FAPα is highly overexpressed in cancer-associated fibroblasts (CAFs) within the tumor microenvironment of over 90% of epithelial cancers, while remaining largely absent in healthy adult tissues. This selective expression makes FAPα an attractive target for both diagnostic imaging and targeted therapy. FAPIs are frequently utilized as targeting ligands in radiopharmaceuticals, where they are conjugated to isotopes like Gallium-68 for PET imaging or Lutetium-177 for radionuclide therapy. Beyond oncology, FAPα inhibitors are being investigated for inflammatory and fibrotic conditions, such as rheumatoid arthritis and myocardial infarction, where activated fibroblasts play a key role in disease progression.

Other names

FAP inhibitorFibroblast activation protein alpha inhibitorFAPI