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Feasibility and Therapeutic Potential of 177Lu–Fibroblast Activation Protein Inhibitor–46 for Patients With Relapsed or Refractory Cancers

Majid AssadiThe Persian Gulf Nuclear Medicine Research Center, Department of Molecular Imaging and Radionuclide Therapy, Bushehr Medical University Hospital, School of Medicine, Bushehr University of Medical SciencesSeyed Javad RekabpourDepartment of Oncology, Salman Farsi Hospital, BushehrEsmail JafariThe Persian Gulf Nuclear Medicine Research Center, Department of Molecular Imaging and Radionuclide Therapy, Bushehr Medical University Hospital, School of Medicine, Bushehr University of Medical SciencesGhasemali DivbandBabak NikkholghHamidreza AminiHassan KamaliDepartment of Chemistry, Kharazmi UniversitySakineh EbrahimiDivision of Oncology, Department of Internal Medicine, Loghman Hospital, Shahid Beheshti University of Medical Sciences, TehranNader ShakibazadDivision of Hematology/Oncology, Department of Pediatrics, Bushehr Medical University Hospital, School of Medicine, Bushehr University of Medical SciencesNarges JokarThe Persian Gulf Nuclear Medicine Research Center, Department of Molecular Imaging and Radionuclide Therapy, Bushehr Medical University Hospital, School of Medicine, Bushehr University of Medical SciencesIraj NabipourThe Persian Gulf Tropical Medicine Research Center, The Persian Gulf Biomedical Sciences Research Institute, Bushehr University of Medical Sciences, Bushehr, IranHojjat AhmadzadehfarDepartment of Nuclear Medicine, Klinikum Westfalen, Dortmund, Germany

2021en

ABI

Annotatsiya

INTRODUCTION: Fibroblast activation protein (FAP) is a member of the serine protease family and has a high expression in the stroma of approximately 90% of epithelial malignancies. The present investigation aimed to assess the feasibility, safety, and dosimetry data of 177Lu-FAPI-46 in diverse malignancies. PATIENTS AND METHODS: Patients with advanced cancers with nonoperable tumors, or tumors refractory to conventional therapies, were enrolled. Treatment included escalating doses of 177Lu-FAPI-46 (1.85-4.44 GBq) per cycle using a combination of clinical and statistical expertise design, and intervals of 4 to 6 weeks were considered between the cycles. Biodistribution and dosimetry were examined by whole-body scans. We applied the National Cancer Institute Common Terminology Criteria for Adverse Events version 4.03 to measure peptide-targeted radionuclide therapy (PTRT)-associated toxicity. RESULTS: A total of 21 patients (11 females and 10 males) with a median age of 50 years (range, 6-79 years) were investigated. Of 21 participants, 18 cases were selected for PTRT. Overall, 36 PTRT cycles were performed. The median number of PTRT cycles and the median injected amount of activity in each cycle were 2 and 3.7 GBq, respectively. The dosimetric analysis revealed median absorbed doses of 0.026, 0.136, 0.886, and 0.02 with ranges of 0.023-0.034, 0.001-0.2, 0.076-1.39, and 0.002-0.2 mGy/MBq for the whole body, liver, kidneys, and spleen, respectively. The therapy was well tolerated in almost all patients. CONCLUSIONS: The findings of this preliminary investigation might indicate the potential feasibility and safety of PTRT using 177Lu-FAPI-46 for different aggressive tumors. Moreover, the current study could be beneficial in determining the suitable amount of activity for a phase 2 study.

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DOI: 10.1097/rlu.0000000000003810

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