2. Academic Validation
  3. Clinical summary of fibroblast activation protein inhibitor-based radiopharmaceuticals: cancer and beyond

Clinical summary of fibroblast activation protein inhibitor-based radiopharmaceuticals: cancer and beyond

  • Eur J Nucl Med Mol Imaging. 2022 Jul;49(8):2844-2868. doi: 10.1007/s00259-022-05706-y.
Mengting Li # 1 2,  Muhsin H Younis # 3,  Yongxue Zhang 1 2,  Weibo Cai 4,  Xiaoli Lan 5 6
Affiliations

Affiliations

  • 1 Department of Nuclear Medicine, Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan, China.
  • 2 Hubei Key Laboratory of Molecular Imaging, Wuhan, China.
  • 3 Departments of Radiology and Medical Physics, University of Wisconsin-Madison, Madison, WI, USA.
  • 4 Departments of Radiology and Medical Physics, University of Wisconsin-Madison, Madison, WI, USA. wcai@uwhealth.org.
  • 5 Department of Nuclear Medicine, Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan, China. xiaoli_lan@hust.edu.cn.
  • 6 Hubei Key Laboratory of Molecular Imaging, Wuhan, China. xiaoli_lan@hust.edu.cn.
  • # Contributed equally.
PMID: 35098327 DOI: 10.1007/s00259-022-05706-y
Abstract

Fibroblast activation protein (FAP) is a type II membrane-bound glycoprotein which is overexpressed in cancer-associated fibroblasts and activated fibroblasts at wound healing/inflammatory sites. Since the first clinical application of quinoline-based FAP ligands in 2018, FAP Inhibitor (FAPI)-based PET imaging and radiotherapy have been investigated for a wide variety of diseases, both cancerous and non-cancerous. As a consequence, promising strides have been made in particular to improve the understanding of FAPI-based PET imaging and the potential value of FAPI-based tumor radiotherapy. Herein, we present a comprehensive review of radiolabeled FAPI, including their clinical translation, in order to clarify the current and potential future role of this class of molecules in nuclear medicine. In particular, this review underlines the value of FAPI radiopharmaceuticals in the diagnosis or therapy of tumors or benign conditions. However, limitations in present studies have hampered a precise evaluation of FAPI radiopharmaceuticals. Despite this, it will likely be worthwhile to further explore the clinical value of FAPI in diagnosis and therapy through better-designed and larger-population clinical trials in the future.

Keywords

Cancer; FAP inhibitor (FAPI); Fibroblast activation protein (FAP); Fibrosis; Molecular imaging; Positron emission tomography (PET).

Figures
Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-128642
    98.94%, FAP抑制剂
    FAP
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