ArticleEuropean journal of nuclear medicine and molecular imaging2023
Head-to-head comparison of different classes of FAP radioligands designed to increase tumor residence time: monomer, dimer, albumin binders, and small molecules vs peptides.
Article in European journal of nuclear medicine and molecular imaging, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 48 papers.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
48 citing papers in PubMed, 79 citations in OpenAlex.
- Preclinical evaluation of homodimeric FAPI target modules for UniCAR-mediated targeting of FAP-expressing tumor and stromal cells.Oncoimmunology · 2026Article
- Optimizing FAPI homodimers for theranostic applications: The impact of the linker design in DOTAGA.GluEuropean journal of nuclear medicine and molecular imaging · 2026Article
- 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
- ALNCR.TNM as a Novel Prognostic Tool for Cancer Survival.Journal of cachexia, sarcopenia and muscle · 2026Article
- FAPI: a solution to all, what about NENs?EJNMMI reports · 2026Review
- PET Imaging of Cardiac Inflammation in Viral Myocarditis Using a DPP4-Targeted Probe.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2026Article
- Dual-tracer PET/CT and cocktail therapy with [European journal of nuclear medicine and molecular imaging · 2026Article
- FAPI Dimerization for Theranostic Applications: Molecular Design, Preclinical Validation, and Clinical Translation.Chemical & biomedical imaging · 2026Review
- 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
- FAP-targeting peptide-directed nanoprobes enable tumor microenvironment-activatable MR/NIRF imaging of breast cancer primary tumor and lung metastases.Materials today. Bio · 2026Article
- 177 Lu-FAP-2286 Therapy for Advanced Lung Adenocarcinoma With Multiple Metastases : A Promising Last-line Treatment Option.Clinical nuclear medicine · 2026Article
- Bridging the gaps in fibroblast activation protein targeted radionuclide therapy: a translational perspective.European journal of nuclear medicine and molecular imaging · 2026Review
- Design, Synthesis, and Evaluation of OncoFAP Derivatives with the Albumin Binder as Novel Antitumor Radiopharmaceuticals.Chemical & biomedical imaging · 2026Article
- On-Resin DIAMSAR-Conjugated CD38-Targeted Peptides and Their Inverso and Dimeric-Inverso Analogs for PET Imaging of Multiple Myeloma.Bioconjugate chemistry · 2026Article
- Comparison between [EJNMMI research · 2026Article
- Head-to-head comparison of FAP-targeting single-domain antibody 4AH29 vs. peptide FAP-2286.EJNMMI research · 2026Article
- Head-to-head comparison of [EJNMMI research · 2026Article
- Fibroblast activation protein-targeted radiopharmaceuticals: Recent trends in cancer diagnosis.Journal of clinical imaging science · 2026Review
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Authors and funding
6 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
purposeFibroblast activation protein-α (FAP)-targeting radioligands have recently demonstrated high diagnostic potential. However, their therapeutic value is impaired by the short tumor residence time. Several strategies have been tested to overcome this limitation, but a head-to-head comparison has never been done. With the aim to identify strengths and limitations of the suggested strategies, we compared the monomer FAPI-46 versus (a) its dimer (FAPI-46-F1D), (b) two albumin binders conjugates (FAPI-46-Ibu (ibuprofen) and FAPI-46-EB (Evans Blue)), and (c) cyclic peptide FAP-2286.
methods
resultsRadioligands showed IC
conclusionThe study indicated dimerization and cyclic peptide structures as promising strategies for prolonging tumor residence time, sparing healthy tissues. Albumin binding strategy outcome depended on the albumin binding moiety. The peptide showed advantages in terms of tumor-to-background ratios, besides tumor-to-kidneys, but its tumor uptake was FAP expression-dependent.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.