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The Current Status of Radionuclide Tumor Targeting Diagnosis and Therapy Based on FAP-2286: From Preclinical Studies

Huajun Liu1,2,3,4, Zhen Yang5, Junzheng Wang1,2,3,4

  • 1Department of Nuclear Medicine, Affiliated Hospital of Southwest Medical University, Luzhou, Sichuan, China.

Molecular Diagnosis & Therapy
|January 25, 2026
PubMed

Insights

FAP-2286, a novel peptide-based radiopharmaceutical targeting fibroblast activation protein (FAP), shows promise for cancer diagnosis and therapy. Its prolonged tumor retention and safety profile support its role as a theranostic agent.

Area of Science:

  • Oncology
  • Molecular Imaging
  • Radiopharmaceutical Therapy

Background:

  • Fibroblast activation protein (FAP) is a key target in oncology.
  • FAP inhibitor (FAPI)-based small molecules show potential for tumor diagnosis and treatment.
  • Developing targeted therapeutic agents for FAP is a major research focus.

Purpose of the Study:

  • To review the development and potential of FAP-2286 as a theranostic agent.
  • To highlight the diagnostic value and therapeutic applications of FAP-2286.
  • To discuss the current status of FAP-targeted radionuclide therapy.

Main Methods:

  • FAP-2286 is a peptide-based radiopharmaceutical derived from FAPI.
  • It combines a FAP-specific binding peptide with a DOTA chelator.
  • Structural optimization enhances tumor retention compared to small-molecule FAPI tracers.

Main Results:

  • FAP-2286 preserves high affinity and favorable imaging characteristics.
  • It demonstrates markedly prolonged tumor retention.
  • Preclinical and early clinical studies show encouraging results, including a favorable safety profile.

Conclusions:

  • FAP-2286 exhibits potential as a theranostic agent for FAP-expressing tumors.
  • Its prolonged in vivo retention supports both diagnostic and therapeutic applications.
  • Further research is needed to advance FAP-based theranostics.

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