ArticleEuropean journal of nuclear medicine and molecular imaging2025
Improved FAPI-radiopharmaceutical pharmacokinetics from the perspectives of a dose escalation study.
Article in European journal of nuclear medicine and molecular imaging, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.
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Who cites it
12 citing papers in PubMed.
- Optimizing FAPI homodimers for theranostic applications: The impact of the linker design in DOTAGA.GluEuropean journal of nuclear medicine and molecular imaging · 2026Article
- Near-infrared light-controlled catalytic hairpin assembly fluorescent biosensor for the sensitive and specific detection of fibroblast activation protein.Nanoscale advances · 2026Article
- FAP-Inhibitor Homodimers with Engineered Linker-Spacer Units: Toward Optimized Radiopharmaceuticals.ACS omega · 2026Article
- The Evolution of FAP-Targeted CAR T-Cell Therapy in Solid Tumors: From Immunotherapy to Immunotheranostic Applications.International journal of molecular sciences · 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
- Design, Synthesis, and Evaluation of OncoFAP Derivatives with the Albumin Binder as Novel Antitumor Radiopharmaceuticals.Chemical & biomedical imaging · 2026Article
- Preclinical evaluation of DOTAGA.Glu.(FAPI)European journal of nuclear medicine and molecular imaging · 2026Article
- Head-to-head comparison of [EJNMMI research · 2026Article
- Radiolabelled FAPI Radiotracers in Oncology: A Comprehensive Review of Current Diagnostic and Emerging Therapeutic Applications.Pharmaceuticals (Basel, Switzerland) · 2026Review
- Stem-Cell Niches in Health and Disease: Microenvironmental Determinants of Regeneration and Pathology.Cells · 2025Review
- Based on small molecules: development and application of fibroblast activation protein inhibitors radiopharmaceutical in tumor precision therapy.Frontiers in pharmacology · 2025Review
Corrections and comments
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Authors and funding
11 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
purposeThis study explores the use of fibroblast activation protein inhibitors (FAPI) targeting radiopharmaceuticals as a new approach for pan-cancer treatment, focusing on key factors affecting their effectiveness. We hypothesized that adjusting the administered radiotracer dose one could enhance the tumor-to-background ratios.
methodsIn a dose-escalation study with PC3 xenografts, all radiotracers were administered at doses between 10 and 1500 pmol, followed by biodistribution and PET/CT imaging. Their selectivity towards FAP, PREP, and DDP4, along with their stability in vivo, was assessed by biodistribution and metabolite analysis, respectively. Organ FAP expression was quantified using qPCR, and circulating FAP (sFAP) levels were measured in mouse and human blood samples via ELISA. Proof-of-principle human studies were also conducted.
resultsIncreasing the dose from 10 to 600 pmol significantly reduced blood uptake and enhanced tumor uptake, optimizing their in vivo performance. All radiotracers showed peak efficacy at 350-600 pmol, with altered pharmacokinetics beyond 600 pmol. Biodistribution studies validated the in vivo selectivity of all radiotracers towards FAP, even in the presence of PREP and DPP4 inhibitors, while they demonstrated remarkable stability in vivo. FAP expression was confirmed in various organs, with sFAP quantified in both healthy mice and humans. Human studies with [
conclusionThe study highlights the crucial need for precise FAPI-radiotracer dosing, optimizing PET imaging, reducing radiation exposure, and enhancing treatment by accounting for FAP biology and sFAP's influence on pharmacokinetics.
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