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Related Experiment Video

Updated: Jun 27, 2026

Automated Preparation of [68Ga]Ga-3BP-3940 on a Synthesis Module for PET Imaging of the Tumor Microenvironment
10:33

Automated Preparation of [68Ga]Ga-3BP-3940 on a Synthesis Module for PET Imaging of the Tumor Microenvironment

Published on: April 25, 2025

FAPI Dimerization for Theranostic Applications: Molecular Design, Preclinical Validation, and Clinical Translation.

Peng Jiang1, Kejing Shao1, Bao Zhu1

  • 1Department of Nuclear Medicine, the Affiliated Wuxi People's Hospital of Nanjing Medical University, Wuxi People's Hospital, Wuxi Medical Center, Nanjing Medical University, Wuxi, Jiangsu 214023, P. R. China.

Chemical & Biomedical Imaging
|June 26, 2026
PubMed
Summary

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Multimerized fibroblast activation protein inhibitors (FAPI) show improved tumor retention and therapeutic potential for cancer theranostics. These advanced FAPI multimers also hold promise for treating fibrotic and inflammatory diseases.

Area of Science:

  • Oncology
  • Radiopharmaceuticals
  • Molecular Imaging

Background:

  • Fibroblast activation protein (FAP) is overexpressed in cancer-associated fibroblasts, making it a key target for cancer theranostics.
  • Monomeric FAP inhibitors (FAPIs) have rapid clearance, limiting their therapeutic efficacy despite good diagnostic performance.
  • Multimerization of FAPIs enhances binding avidity and tumor retention, improving theranostic outcomes.

Purpose of the Study:

  • To review recent advances in FAPI-based multimers for theranostic applications.
  • To analyze molecular design, synthesis, and evaluation of FAPI multimers.
  • To discuss clinical applications and emerging uses in non-oncology diseases.

Main Methods:

  • Comprehensive literature review of FAPI multimer research.
Keywords:
FAPI dimerFibroblast activation proteinHeterodimerMolecular imagingRadioligand therapyTheranostics

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Last Updated: Jun 27, 2026

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  • Analysis of molecular design strategies, including linker chemistry and chelator selection.
  • Evaluation of preclinical and clinical data for homodimeric and heterodimeric FAPI constructs.

    • Main Results:

    • FAPI multimers, including homodimers and heterodimers, demonstrate enhanced tumor uptake and retention compared to monomers.
    • Dual-targeting heterodimers (e.g., FAPI-RGD, PSFA-01) show promise for improved specificity.
    • Early clinical trials indicate enhanced diagnostic sensitivity and therapeutic potential across various cancers.
    • FAPI multimers show potential in treating fibrotic and inflammatory diseases like rheumatoid arthritis and interstitial lung disease.

    Conclusions:

    • FAPI multimers represent a significant advancement in theranostic radiopharmaceuticals, improving upon monomeric FAPIs.
    • Optimized linker chemistry and chelator selection are crucial for enhancing pharmacokinetic profiles.
    • FAPI multimers show broad applicability in oncology and emerging potential in non-oncology indications.
    • Ongoing innovations aim to address challenges like renal uptake and cost for wider clinical adoption.