Hamson EJ, Keane FM, Tholen S, Schilling O, Gorrell MD. Understanding fibroblast activation protein (FAP): substrates, activities, expression and targeting for cancer therapy. Proteomics Clin Appl. 2014;8:454–63. https://doi.org/10.1002/prca.201300095.
Article CAS PubMed Google Scholar
Altmann A, Haberkorn U, Siveke J. The latest developments in imaging of fibroblast activation protein. J Nucl Med. 2021;62:160–7. https://doi.org/10.2967/jnumed.120.244806.
Article CAS PubMed Google Scholar
Moon ES, Elvas F, Vliegen G, De Lombaerde S, Vangestel C, De Bruycker S, et al. Targeting fibroblast activation protein (FAP): next generation PET radiotracers using squaramide coupled bifunctional DOTA and DATA(5m) chelators. EJNMMI Radiopharm Chem. 2020;5:19. https://doi.org/10.1186/s41181-020-00102-z.
Article PubMed PubMed Central Google Scholar
Watabe T, Liu Y, Kaneda-Nakashima K, Shirakami Y, Lindner T, Ooe K, et al. Theranostics targeting fibroblast activation protein in the tumor stroma: (64)Cu- and (225)Ac-labeled FAPI-04 in pancreatic cancer xenograft mouse models. J Nucl Med. 2020;61:563–9. https://doi.org/10.2967/jnumed.119.233122.
Article CAS PubMed PubMed Central Google Scholar
Kosmala A, Serfling SE, Dreher N, Lindner T, Schirbel A, Lapa C, et al. Associations between normal organs and tumor burden in patients imaged with fibroblast activation protein inhibitor-directed positron emission tomography. Cancers (Basel). 2022;14. https://doi.org/10.3390/cancers14112609.
Privé BM, Boussihmad MA, Timmermans B, van Gemert WA, Peters SMB, Derks YHW, et al. Fibroblast activation protein-targeted radionuclide therapy: background, opportunities, and challenges of first (pre)clinical studies. Eur J Nucl Med Mol Imaging. 2023;50:1906–18. https://doi.org/10.1007/s00259-023-06144-0.
Article PubMed PubMed Central Google Scholar
Ferdinandus J, Costa PF, Kessler L, Weber M, Hirmas N, Kostbade K, et al. Initial clinical experience with (90)Y-FAPI-46 radioligand therapy for advanced-stage solid tumors: a case series of 9 patients. J Nucl Med. 2022;63:727–34. https://doi.org/10.2967/jnumed.121.262468.
Article PubMed PubMed Central Google Scholar
Moon ES, Ballal S, Yadav MP, Bal C, Van Rymenant Y, Stephan S, et al. Fibroblast Activation Protein (FAP) targeting homodimeric FAP inhibitor radiotheranostics: a step to improve tumor uptake and retention time. Am J Nucl Med Mol Imaging. 2021;11:476–91.
CAS PubMed PubMed Central Google Scholar
Millul J, Koepke L, Haridas GR, Sparrer KMJ, Mansi R, Fani M. 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. Eur J Nucl Med Mol Imaging. 2023. https://doi.org/10.1007/s00259-023-06272-7.
Article PubMed PubMed Central Google Scholar
Yadav MP, Ballal S, Martin M, Roesch F, Satapathy S, Moon ES, et al. Therapeutic potential of [177Lu]Lu-DOTAGA-FAPi dimers in metastatic breast cancer patients with limited treatment options: efficacy and safety assessment. Eur J Nucl Med Mol Imaging. 2023. https://doi.org/10.1007/s00259-023-06482-z.
Galbiati A, Zana A, Bocci M, Millul J, Elsayed A, Mock J, et al. A dimeric FAP-targeting small-molecule radioconjugate with high and prolonged tumor uptake. J Nucl Med. 2022;63:1852–8. https://doi.org/10.2967/jnumed.122.264036.
Article CAS PubMed PubMed Central Google Scholar
Zhao L, Niu B, Fang J, Pang Y, Li S, Xie C, et al. Synthesis, preclinical evaluation, and a pilot clinical PET imaging study of (68)Ga-labeled FAPI dimer. J Nucl Med. 2022;63:862–8. https://doi.org/10.2967/jnumed.121.263016.
Article CAS PubMed PubMed Central Google Scholar
Zhao L, Chen J, Pang Y, Fang J, Fu K, Meng L, et al. Development of fibroblast activation protein inhibitor-based dimeric radiotracers with improved tumor retention and antitumor efficacy. Mol Pharm. 2022;19:3640–51. https://doi.org/10.1021/acs.molpharmaceut.2c00424.
Article CAS PubMed Google Scholar
Loktev A, Lindner T, Burger EM, Altmann A, Giesel F, Kratochwil C, et al. Development of fibroblast activation protein-targeted radiotracers with improved tumor retention. J Nucl Med. 2019;60:1421–9. https://doi.org/10.2967/jnumed.118.224469.
Article CAS PubMed PubMed Central Google Scholar
Zhong X, Guo J, Han X, Wu W, Yang R, Zhang J, et al. Synthesis and preclinical evaluation of a novel FAPI-04 dimer for cancer theranostics. Mol Pharm. 2023;20:2402–14. https://doi.org/10.1021/acs.molpharmaceut.2c00965.
Article CAS PubMed Google Scholar
Li H, Ye S, Li L, Zhong J, Yan Q, Zhong Y, et al. (18)F- or (177)Lu-labeled bivalent ligand of fibroblast activation protein with high tumor uptake and retention. Eur J Nucl Med Mol Imaging. 2022;49:2705–15. https://doi.org/10.1007/s00259-022-05757-1.
Article CAS PubMed Google Scholar
Zhao L, Chen J, Pang Y, Fu K, Shang Q, Wu H, et al. Fibroblast activation protein-based theranostics in cancer research: a state-of-the-art review. Theranostics. 2022;12:1557–69. https://doi.org/10.7150/thno.69475.
Article CAS PubMed PubMed Central Google Scholar
Giesel FL, Kratochwil C, Lindner T, Marschalek MM, Loktev A, Lehnert W, et al. (68)Ga-FAPI PET/CT: biodistribution and preliminary dosimetry estimate of 2 DOTA-containing FAP-targeting agents in patients with various cancers. J Nucl Med. 2019;60:386–92. https://doi.org/10.2967/jnumed.118.215913.
Article CAS PubMed PubMed Central Google Scholar
Ballal S, Yadav MP, Moon ES, Kramer VS, Roesch F, Kumari S, et al. Biodistribution, pharmacokinetics, dosimetry of [(68)Ga]Ga-DOTA.SA.FAPi, and the head-to-head comparison with [(18)F]F-FDG PET/CT in patients with various cancers. Eur J Nucl Med Mol Imaging. 2021;48:1915–31. https://doi.org/10.1007/s00259-020-05132-y.
Loktev A, Lindner T, Mier W, Debus J, Altmann A, Jager D, et al. A tumor-imaging method targeting cancer-associated fibroblasts. J Nucl Med. 2018;59:1423–9. https://doi.org/10.2967/jnumed.118.210435.
Article CAS PubMed PubMed Central Google Scholar
Assadi M, Rekabpour SJ, Jafari E, Divband G, Nikkholgh B, Amini H, et al. Feasibility and therapeutic potential of 177Lu-fibroblast activation protein inhibitor-46 for patients with relapsed or refractory cancers: a preliminary study. Clin Nucl Med. 2021;46:e523–30. https://doi.org/10.1097/RLU.0000000000003810.
Li ZB, Chen K, Chen X. (68)Ga-labeled multimeric RGD peptides for microPET imaging of integrin alpha(v)beta (3) expression. Eur J Nucl Med Mol Imaging. 2008;35:1100–8. https://doi.org/10.1007/s00259-007-0692-y.
Article CAS PubMed Google Scholar
Zang J, Wen X, Lin R, Zeng X, Wang C, Shi M, et al. Synthesis, preclinical evaluation and radiation dosimetry of a dual targeting PET tracer [(68)Ga]Ga-FAPI-RGD. Theranostics. 2022;12:7180–90. https://doi.org/10.7150/thno.79144.
Article CAS PubMed PubMed Central Google Scholar
Pang Y, Zhao L, Fang J, Chen J, Meng L, Sun L, et al. Development of FAPI tetramers to improve tumor uptake and efficacy of FAPI radioligand therapy. J Nucl Med. 2023:jnumed.123.265599. https://doi.org/10.2967/jnumed.123.265599.
Lang L, Li W, Guo N, Ma Y, Zhu L, Kiesewetter DO, et al. Comparison study of [18F]FAl-NOTA-PRGD2, [18F]FPPRGD2, and [68Ga]Ga-NOTA-PRGD2 for PET imaging of U87MG tumors in mice. Bioconjug Chem. 2011;22:2415–22. https://doi.org/10.1021/bc200197h.
Article CAS PubMed PubMed Central Google Scholar
Zhang RH, Guo HY, Deng H, Li J, Quan ZS. Piperazine skeleton in the structural modification of natural products: a review. J Enzyme Inhib Med Chem. 2021;36:1165–97. https://doi.org/10.1080/14756366.2021.1931861.
Article CAS PubMed PubMed Central Google Scholar
Meyer C, Dahlbom M, Lindner T, Vauclin S, Mona C, Slavik R, et al. Radiation dosimetry and biodistribution of (68)Ga-FAPI-46 PET imaging in cancer patients. J Nucl Med. 2020;61:1171–7. https://doi.org/10.2967/jnumed.119.236786.
留言 (0)