Fibroblast activation protein-based theranostics in cancer research: A state-of-the-art review

Theranostics. 2022 Jan 9;12(4):1557-1569. doi: 10.7150/thno.69475. eCollection 2022.

Abstract

In recent years, quinoline-based fibroblast activation protein (FAP) inhibitors (FAPI) have shown promising results in the diagnosis of cancer and several other diseases, making them the hotspot of much productive research. This review summarizes the literature for the state-of-the-art FAPI-PET imaging for cancer diagnosis compared with fluorodeoxyglucose (FDG)-PET. We also summarize the use of FAPI-PET for therapeutic regimen improvement and fibroblast activation protein (FAP)-targeted molecule modification strategies, as well as preliminary clinical studies regarding FAP-targeted radionuclide therapy. Our qualitative summary of the literature to date can inform future research directions, medical guidelines, and optimal clinical decision-making.

Keywords: PET/CT; cancer management; cancer-associated fibroblasts (CAF); fibroblast activation protein (FAP); targeted radionuclide therapy.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Endopeptidases
  • Fibroblasts / metabolism
  • Membrane Proteins / metabolism
  • Neoplasms* / diagnostic imaging
  • Neoplasms* / therapy
  • Positron Emission Tomography Computed Tomography / methods
  • Positron-Emission Tomography
  • Precision Medicine*

Substances

  • Membrane Proteins
  • Endopeptidases