Feasibility and Therapeutic Potential of 177Lu–Fibroblast Activation Protein Inhibitor–46 for Patients With Relapsed or Refractory Cancers: A Preliminary Study. (November 2021)

• Record Type: Journal Article
• Authors: Assadi, Majid; Rekabpour, Seyed Javad; Jafari, Esmail; Divband, GhasemAli; Nikkholgh, Babak; Amini, Hamidreza; Kamali, Hassan; Ebrahimi, Sakineh; Shakibazad, Nader; Jokar, Narges; Nabipour, Iraj; Ahmadzadehfar, Hojjat
• Is Part Of: Clinical nuclear medicine. Volume 46:Number 11(2021)
• Publication Date: 2021-11
• Subjects: peptide-targeted radionuclide therapy -- 177Lu-FAPI-46 -- theranostics -- fibroblast activation protein; Nuclear medicine -- Periodicals; Radioisotope scanning -- Periodicals; Nuclear Medicine -- Periodicals; 616.07575
• DOI: 10.1097/RLU.0000000000003810
• Languages: English
• ISSNs: 0363-9762

Abstract

Abstract : 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 177 Lu-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 177 Lu-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 177 Lu-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.