Literature DB >> 34269729

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

Majid Assadi1, Seyed Javad Rekabpour, Esmail Jafari, GhasemAli Divband, Babak Nikkholgh, Hamidreza Amini, Hassan Kamali, Sakineh Ebrahimi, Nader Shakibazad, Narges Jokar, Iraj Nabipour, Hojjat Ahmadzadehfar.   

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 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.
Copyright © 2021 Wolters Kluwer Health, Inc. All rights reserved.

Entities:  

Year:  2021        PMID: 34269729     DOI: 10.1097/RLU.0000000000003810

Source DB:  PubMed          Journal:  Clin Nucl Med        ISSN: 0363-9762            Impact factor:   7.794


  8 in total

1.  Synthesis, Preclinical Evaluation, and a Pilot Clinical PET Imaging Study of 68Ga-Labeled FAPI Dimer.

Authors:  Liang Zhao; Bo Niu; Jianyang Fang; Yizhen Pang; Siyang Li; Chengrong Xie; Long Sun; Xianzhong Zhang; Zhide Guo; Qin Lin; Haojun Chen
Journal:  J Nucl Med       Date:  2021-09-23       Impact factor: 11.082

2.  PET with a 68Ga-Labeled FAPI Dimer: Moving Toward Theranostics.

Authors:  Muhsin H Younis; Xiaoli Lan; Weibo Cai
Journal:  J Nucl Med       Date:  2021-11-05       Impact factor: 11.082

3.  FAP-targeted radionuclide therapy with [177Lu]Lu-FAPI-46 in metastatic nasopharyngeal carcinoma.

Authors:  Kaili Fu; Yizhen Pang; Liang Zhao; Limei Lin; Hua Wu; Long Sun; Qin Lin; Haojun Chen
Journal:  Eur J Nucl Med Mol Imaging       Date:  2021-12-08       Impact factor: 9.236

4.  Enhancing fibroblast activation protein (FAP)-targeted radionuclide therapy with albumin binding, and beyond.

Authors:  Muhsin H Younis; Sara Malih; Xiaoli Lan; Mohammad Javad Rasaee; Weibo Cai
Journal:  Eur J Nucl Med Mol Imaging       Date:  2022-05       Impact factor: 10.057

Review 5.  Fibroblast activation protein-based theranostics in cancer research: A state-of-the-art review.

Authors:  Liang Zhao; Jianhao Chen; Yizhen Pang; Kaili Fu; Qihang Shang; Hua Wu; Long Sun; Qin Lin; Haojun Chen
Journal:  Theranostics       Date:  2022-01-09       Impact factor: 11.556

6.  Interobserver Agreement Rates on Fibroblast Activation Protein Inhibitor-Directed Molecular Imaging and Therapy.

Authors:  Sebastian E Serfling; Philipp E Hartrampf; Yingjun Zhi; Takahiro Higuchi; Steven P Rowe; Lena Bundschuh; Markus Essler; Andreas K Buck; Ralph Alexander Bundschuh; Rudolf A Werner
Journal:  Clin Nucl Med       Date:  2022-04-19       Impact factor: 10.782

7.  From Automated Synthesis to In Vivo Application in Multiple Types of Cancer-Clinical Results with [68Ga]Ga-DATA5m.SA.FAPi.

Authors:  Lukas Greifenstein; Carsten S Kramer; Euy Sung Moon; Frank Rösch; Andre Klega; Christian Landvogt; Corinna Müller; Richard P Baum
Journal:  Pharmaceuticals (Basel)       Date:  2022-08-14

Review 8.  Imaging Cancer-Associated Fibroblasts (CAFs) with FAPi PET.

Authors:  Laura Gilardi; Lighea Simona Airò Farulla; Emre Demirci; Ilaria Clerici; Emanuela Omodeo Salè; Francesco Ceci
Journal:  Biomedicines       Date:  2022-02-23
  8 in total

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