Protein-based Radiopharmaceuticals that target fibroblast activation protein alpha: a review of current progress

Abdelrahman Homedan; Darpan N. Pandya; Nicholas J. Schnicker; Thaddeus J. Wadas

doi:10.1186/s41181-025-00356-5

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Protein-based Radiopharmaceuticals that target fibroblast activation protein alpha: a review of current progress

Journal article

Open access

Peer reviewed

Protein-based Radiopharmaceuticals that target fibroblast activation protein alpha: a review of current progress

Abdelrahman Homedan, Darpan N. Pandya, Nicholas J. Schnicker and Thaddeus J. Wadas

EJNMMI radiopharmacy and chemistry, Vol.10(1), 32

06/21/2025

DOI: 10.1186/s41181-025-00356-5

PMCID: PMC12182545

PMID: 40542914

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Abstract

Background Fibroblast activation protein alpha (FAP) is a serine protease that is expressed at basal levels in benign tissues but is overexpressed in a variety of pathologies, including cancer. Consequently, significant research efforts have been expended to develop diagnostic radiopharmaceuticals and effective radiotherapies that target this protein. The aim of this review is to summarize the current progress on the development of protein-based radiopharmaceuticals that target FAP. Main body A literature survey spanning nearly 40 years was conducted to assess the historical development and current progress in protein-based radiopharmaceuticals that target FAP. To date, more than 20 publications have been introduced that describe these agents in preclinical and clinical settings. This review summarizes the development and evaluation of radiopharmaceuticals involving antibodies, antibody fragments, and single domain antibodies. Conclusion The results of this literature review demonstrate that while significant research efforts have been expended on peptide-based radiopharmaceuticals and small molecule FAP inhibitors, the development of protein-based radiopharmaceuticals that target FAP remains an active research area that has yet to reach its full potential.

Nuclear Chemistry

Nuclear Medicine

Pharmacotherapy

Radiology

Fibroblast Activation Protein Inhibitor (FAPI): novel tracers and approaches for optimized imaging and therapy

Imaging

Medicine

Medicine & Public Health

Molecular Medicine

Review

Details

Title: Subtitle: Protein-based Radiopharmaceuticals that target fibroblast activation protein alpha: a review of current progress
Creators: Abdelrahman Homedan - University of Iowa
Darpan N. Pandya - University of Iowa
Nicholas J. Schnicker - University of Iowa
Thaddeus J. Wadas - University of Iowa
Resource Type: Journal article
Publication Details: EJNMMI radiopharmacy and chemistry, Vol.10(1), 32
Publisher: Springer International Publishing
DOI: 10.1186/s41181-025-00356-5
PMID: 40542914
PMCID: PMC12182545
ISSN: 2365-421X
eISSN: 2365-421X
Grant note: R21-CA219899; R21-CA227709 / National Institute of Health W81XWH-19-1-0046 / CDMRP
Language: English
Date published: 06/21/2025
Academic Unit: Radiology; Molecular Physiology and Biophysics; Radiation Oncology; Medicine Administration
Record Identifier: 9984832087602771

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