Fibroblast Activation Protein Inhibitor Theranostics: Preclinical Considerations.

Fibroblast activation protein (FAP) was first reported in 1986. However, FAP is not expressed in normal fibroblasts, normal or malignant epithelial cells, or the stroma of benign epithelial tumors. FAP is a cell membrane-bound serine peptidase overexpressed on the surface of cancer-associated fibroblasts and, as such, is a novel target for molecular imaging of several tumors. FAP inhibitors (FAPI) are potential theranostic molecular probes for various cancers. A tumor model expressing FAP was used to verify or confirm the usefulness of FAPI experimentally.