ArticleEuropean journal of nuclear medicine and molecular imaging2022
Preclinical evaluation of FAP-2286 for fibroblast activation protein targeted radionuclide imaging and therapy.
Article in European journal of nuclear medicine and molecular imaging, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 152 papers.
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152 citing papers in PubMed, 238 citations in OpenAlex.
- Feasibility and therapeutic potential of [European journal of nuclear medicine and molecular imaging · 2024Trial
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- Context-dependent efficacy of fibroblast activation protein-targeted radionuclide therapy (FAP-TRT): the dual role of CAFs.European journal of nuclear medicine and molecular imaging · 2026Article
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- The value of fibroblast activation protein inhibitor-based radionuclide theranostics in sarcoma: a systematic review.Annals of nuclear medicine · 2026Review
- FAP-Inhibitor Homodimers with Engineered Linker-Spacer Units: Toward Optimized Radiopharmaceuticals.ACS omega · 2026Article
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- Tetrazine-Enabled Peptide Macrocyclization and Bioorthogonal Cell Penetration Profiling.JACS Au · 2026Article
- The FAP-FDG Integration Score (FFIS): Development and prognostic validation of a dual-tracer PET phenotype for solid tumors.European journal of nuclear medicine and molecular imaging · 2026Article
- Clinical and research applications of fibroblast activation protein-α inhibitor tracers: a review.The British journal of radiology · 2026Review
- Dual-tracer PET/CT and cocktail therapy with [European journal of nuclear medicine and molecular imaging · 2026Article
- Automated and manual synthesis of [EJNMMI radiopharmacy and chemistry · 2026Article
- Homomultimeric FAP Inhibitor-Based Radioligands for Cancer Theranostics: Design Principles, Structure-Function Relationships, and Preclinical Performance.Molecules (Basel, Switzerland) · 2026Review
- Head-to-Head Comparison of Monomeric, Homodimeric, and Heterodimeric Fibroblast Activation Protein-Targeting Radioligands Based on Small Molecule Inhibitor and Cyclic Peptide.ACS pharmacology & translational science · 2026Article
- Development of LRRC15-binding disulfide-constrained peptides for PET imaging of cancer-associated fibroblasts.Nature communications · 2026Article
- Head to head comparison of [EJNMMI research · 2026Article
- Radionuclide‑drug conjugates in lung cancer: advances in precision therapy and clinical translation.Molecular cancer · 2026Review
- 177 Lu-FAP-2286 Therapy for Advanced Lung Adenocarcinoma With Multiple Metastases : A Promising Last-line Treatment Option.Clinical nuclear medicine · 2026Article
- A FAP-Targeted SMDC Platform Enables Synergistic Radionuclide-Chemotherapy with PET-Guided Evaluation.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2026Article
- Observational
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Authors and funding
21 authors at 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
purposeFibroblast activation protein (FAP) is a membrane-bound protease that has limited expression in normal adult tissues but is highly expressed in the tumor microenvironment of many solid cancers. FAP-2286 is a FAP-binding peptide coupled to a radionuclide chelator that is currently being investigated in patients as an imaging and therapeutic agent. The potency, selectivity, and efficacy of FAP-2286 were evaluated in preclinical studies.
methodsFAP expression analysis was performed by immunohistochemistry and autoradiography on primary human cancer specimens. FAP-2286 was assessed in biochemical and cellular assays and in in vivo imaging and efficacy studies, and was further evaluated against FAPI-46, a small molecule-based FAP-targeting agent.
resultsImmunohistochemistry confirmed elevated levels of FAP expression in multiple tumor types including pancreatic, breast, and sarcoma, which correlated with FAP binding by FAP-2286 autoradiography. FAP-2286 and its metal complexes demonstrated high affinity to FAP recombinant protein and cell surface FAP expressed on fibroblasts. Biodistribution studies in mice showed rapid and persistent uptake of
conclusionIn preclinical models, radiolabeled FAP-2286 demonstrated high tumor uptake and retention, as well as potent efficacy in FAP-positive tumors. These results support clinical development of
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