Diagnostic and Therapeutic Application of Fibroblast Activation Protein Inhibitors in Oncologic and Nononcologic Diseases

Cancer J. 2024 May-Jun;30(3):210-217. doi: 10.1097/PPO.0000000000000719.

Abstract

Fibroblast activation protein inhibitor positron emission tomography (PET) has gained interest for its ability to demonstrate uptake in a diverse range of tumors. Its molecular target, fibroblast activation protein, is expressed in cancer-associated fibroblasts, a major cell type in tumor microenvironment that surrounds various types of cancers. Although existing literature on FAPI PET is largely from single-center studies and case reports, initial findings show promise for some cancer types demonstrating improved imaging when compared with the widely used 18F-fludeoxyglucose PET for oncologic imaging. As we expand our knowledge of the utility of FAPI PET, accurate understanding of noncancerous uptake seen on FAPI PET is crucial for accurate evaluation. In this review, we summarize potential diagnostic and therapeutic applications of radiolabeled FAP inhibitors in oncological and nononcological disease processes.

Publication types

  • Review

MeSH terms

  • Animals
  • Cancer-Associated Fibroblasts / drug effects
  • Cancer-Associated Fibroblasts / metabolism
  • Endopeptidases
  • Gelatinases / antagonists & inhibitors
  • Gelatinases / metabolism
  • Humans
  • Membrane Proteins / antagonists & inhibitors
  • Membrane Proteins / metabolism
  • Neoplasms* / diagnosis
  • Neoplasms* / drug therapy
  • Neoplasms* / metabolism
  • Positron-Emission Tomography / methods
  • Radiopharmaceuticals
  • Serine Endopeptidases / metabolism
  • Tumor Microenvironment / drug effects

Substances

  • fibroblast activation protein alpha