Fibroblast Activation Protein Inhibitor Theranostics: Preclinical Considerations

Kazuko Kaneda-Nakashima; Yoshifumi Shirakami; Yuichiro Kadonaga; Tadashi Watabe

doi:10.1016/j.cpet.2023.02.005

Fibroblast Activation Protein Inhibitor Theranostics: Preclinical Considerations

PET Clin. 2023 Jul;18(3):397-408. doi: 10.1016/j.cpet.2023.02.005. Epub 2023 Mar 28.

Authors

Kazuko Kaneda-Nakashima¹, Yoshifumi Shirakami², Yuichiro Kadonaga³, Tadashi Watabe⁴

Affiliations

¹ Division of Radiation Science, Institute for Radiation Sciences, Osaka University, 2-4 Yamadaoka, Suita, Osaka 565-0871, Japan; MS-CORE, Forefront Research Center, Graduate School of Science, Osaka University, 1-1 Machikaneyama, Toyonaka, Osaka 560-0043, Japan. Electronic address: kkaneda@irs.osaka-u.ac.jp.
² Division of Radiation Science, Institute for Radiation Sciences, Osaka University, 2-4 Yamadaoka, Suita, Osaka 565-0871, Japan; MS-CORE, Forefront Research Center, Graduate School of Science, Osaka University, 1-1 Machikaneyama, Toyonaka, Osaka 560-0043, Japan.
³ MS-CORE, Forefront Research Center, Graduate School of Science, Osaka University, 1-1 Machikaneyama, Toyonaka, Osaka 560-0043, Japan; Department of Nuclear Medicine and Tracer Kinetics, Graduate School of Medicine, Osaka University, 2-2 Yamadaoka, Suita, Osaka 565-0871, Japan.
⁴ Division of Radiation Science, Institute for Radiation Sciences, Osaka University, 2-4 Yamadaoka, Suita, Osaka 565-0871, Japan; Department of Nuclear Medicine and Tracer Kinetics, Graduate School of Medicine, Osaka University, 2-2 Yamadaoka, Suita, Osaka 565-0871, Japan.

PMID: 36997365
DOI: 10.1016/j.cpet.2023.02.005

Abstract

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.

Keywords: Actinium-225; Antitumor effect; Astatine-211; FAP inhibitors; Lutetium-177; Targeted radiotherapy; Theranostics; Tumor-bearing model.

Publication types

Review

MeSH terms

Fibroblasts / metabolism
Fibroblasts / pathology
Humans
Membrane Proteins* / metabolism
Neoplasms* / diagnostic imaging
Neoplasms* / drug therapy
Neoplasms* / metabolism
Precision Medicine
Serine Endopeptidases / metabolism

Substances

Membrane Proteins
Serine Endopeptidases