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Advances in Radiotherapy &
Nuclear Medicine
REVIEW ARTICLE
Fibroblast activation protein-targeted
radioligand therapy in various types of cancer:
Background, clinical studies, and future
development
3
3
Yizhen Pang 1,2† , Liang Zhao 1,2† , Jianhao Chen , Weizhi Xu , Jiayu Cai ,
2
1,3
1,2
Haojun Chen *, and Qin Lin *
1 The School of Clinical Medicine, Fujian Medical University, Fuzhou, China
2 Department of Radiation Oncology, Xiamen Cancer Center, Xiamen Key Laboratory of Radiation Oncology,
the First Affiliated Hospital of Xiamen University, School of Medicine, Xiamen University, Xiamen, China
3 Department of Nuclear Medicine and Minnan PET Center, Xiamen Key Laboratory of Development
and Translation of Radiopharmaceuticals, The First Affiliated Hospital of Xiamen University, School
of Medicine, Xiamen University, Xiamen, China
Abstract
Cancer is the leading cause of mortality worldwide. The proliferation and viability of
† These authors contributed equally cancer cells are intricately related to the complex tumor microenvironment in which
to this work. they reside. Cancer-associated fibroblasts (CAFs) play a pivotal role in multiple stages
*Corresponding authors: of tumorigenesis, including tumor growth, invasion, metastasis, and resistance
Haojun Chen to treatment, through intricate crosstalk with tumor and immune cells. Targeted
(leochen0821@foxmail.com)
Qin Lin radionuclide therapy involves the systemic administration of small molecule drugs
(linqin05@163.com) labeled with β-emitting or α-emitting radioisotopes, allowing precise targeting
Citation: Pang Y, Zhao L, Chen J, of tumor sites and delivering radiation directly to the tumor. Prostate-specific
et al., 2023, Fibroblast activation membrane antigen-targeted radioligand therapy (RLT) and somatostatin receptor-
protein-targeted radioligand targeted peptide receptor radionuclide therapy (PRRT) have demonstrated favorable
therapy in various types of cancer:
Background, clinical studies, and safety profiles and significant antitumor efficacy, leading to their approval by the
future development. Adv Radiother Food and Drug Administration. Recently, the utilization of theranostic approaches
Nucl Med, 1(2): 1667 that target overexpressed fibroblast activation proteins (FAPs) within the CAFs of the
https://doi.org/10.36922/arnm.1667 tumor stroma has demonstrated encouraging preliminary outcomes. This review
Received: August 23, 2023 aims to provide a concise summary of current clinical research outcomes and the
Accepted: September 19, 2023 applications of RLT based on FAP inhibitors in the context of solid tumors.
Published Online: October 24,
2023 Keywords: Fibroblast activation proteins; Radioligand therapy; Immunotherapy;
Copyright: © 2023 Author(s). Synergistic effect
This is an Open-Access article
distributed under the terms of the
Creative Commons Attribution
License, permitting distribution,
and reproduction in any medium, 1. Introduction
provided the original work is
properly cited. Cancer is among the leading causes of mortality globally, with projections indicating
[1]
Publisher’s Note: AccScience that cancer-related deaths will surpass those caused by cardiovascular disease . Current
Publishing remains neutral with cancer treatment strategies typically involve a combination of chemotherapy, radiotherapy,
regard to jurisdictional claims in
published maps and institutional and surgical interventions tailored to individual patient needs. Remarkably, over the past
affiliations. two decades, there has been minimal appreciable improvement in the average cancer
Volume 1 Issue 2 (2023) 1 https://doi.org/10.36922/arnm.1667

