Alpha-Emitters and Targeted Alpha Therapy in Oncology: from Basic Science to Clinical Investigations

Makvandi, Mehran; Dupis, Edouard; Engle, Jonathan W.; Nortier, F. Meiring; Fassbender, Michael E.; Simon, Sam; Birnbaum, Eva R.; Atcher, Robert W.; John, Kevin D.; Rixe, Olivier; Norenberg, Jeffrey P.

doi:10.1007/s11523-018-0550-9

Title: Alpha-Emitters and Targeted Alpha Therapy in Oncology: from Basic Science to Clinical Investigations

Journal Article · 08 February 2018 · Targeted Oncology

DOI: https://doi.org/10.1007/s11523-018-0550-9 · OSTI ID:1459839

Makvandi, Mehran ^[1]; Dupis, Edouard ^[2]; Engle, Jonathan W. ^[3]; Nortier, F. Meiring ^[3]; Fassbender, Michael E. ^[3]; Simon, Sam ^[1]; Birnbaum, Eva R. ^[3]; Atcher, Robert W. ^[4]; John, Kevin D. ^[3]; Rixe, Olivier ^[2]; Norenberg, Jeffrey P. ^[1]

Univ. of New Mexico, Albuquerque, NM (United States). Radiopharmaceutical Sciences Program. College of Pharmacy. Health Sciences Center
Univ. of New Mexico Comprehensive Cancer Center, Albuquerque, NM (United States). Experimental Therapeutics Unit
Los Alamos National Lab. (LANL), Los Alamos, NM (United States)
Univ. of New Mexico, Albuquerque, NM (United States). Radiopharmaceutical Sciences Program. College of Pharmacy. Health Sciences Center; Los Alamos National Lab. (LANL), Los Alamos, NM (United States)

Alpha-emitters are radionuclides that decay through the emission of high linear energy transfer α-particles and possess favorable pharmacologic profiles for cancer treatment. When coupled with monoclonal antibodies, peptides, small molecules, or nanoparticles, the excellent cytotoxic capability of α-particle emissions has generated a strong interest in exploring targeted α-therapy in the pre-clinical setting and more recently in clinical trials in oncology. Multiple obstacles have been overcome by researchers and clinicians to accelerate the development of targeted α-therapies, especially with the recent improvement in isotope production and purification, but also with the development of innovative strategies for optimized targeting. Numerous studies have demonstrated the in vitro and in vivo efficacy of the targeted α-therapy. Radium-223 (²²³Ra) dichloride (Xofigo®) is the first α-emitter to have received FDA approval for the treatment of prostate cancer with metastatic bone lesions. There is a significant increase in the number of clinical trials in oncology using several radionuclides such as Actinium-225 (²²⁵Ac), Bismuth-213 (²¹³Bi), Lead-212 (²¹²Pb), Astatine (²¹¹At) or Radium-223 (²²³Ra) assessing their safety and preliminary activity. Finally, this review will cover their therapeutic application as well as summarize the investigations that provide the foundation for further clinical development.

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Research Organization:: Los Alamos National Laboratory (LANL), Los Alamos, NM (United States); Univ. of New Mexico, Albuquerque, NM (United States)

Sponsoring Organization:: USDOE

Grant/Contract Number:: AC52-06NA25396

OSTI ID:: 1459839

Report Number(s):: LA-UR-16-27976

Journal Information:: Targeted Oncology, Vol. 13, Issue 2; ISSN 1776-2596

Publisher:: SpringerCopyright Statement

Country of Publication:: United States

Language:: English

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Cited by: 84 works

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