Medicinal Chemistry

Atta-ur-Rahman  
Honorary Life Fellow
Kings College
University of Cambridge
Cambridge
UK
Email: mc@benthamscience.org

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86Y Based PET Radiopharmaceuticals: Radiochemistry and Biological Applications

Author(s): Tapan K. Nayak and Martin W. Brechbiel

Affiliation: 10 Center Drive MSC 1002, Room B3B69, NCI-Bethesda, Bethesda, MD 20892, USA.

Keywords: PET imaging, radiochemistry, 90Y, 86Y, bioconjugate chemistry, peptides, antibodies, positron emitter, Radiopharmaceuticals, targeted radionuclide therapy

Abstract:

Development of targeted radionuclide therapy with 90Y labeled antibodies and peptides has gained momentum in the past decade due to the successes of 90Y-ibritumomab tiuxetan and 90Y-DOTA-Phe1-Tyr3-octreotide in treatment of cancer. 90Y is a pure β--emitter and cannot be imaged for patient-specific dosimetry which is essential for pre-therapeutic treatment planning and accurate absorbed dose estimation in individual patients to mitigate radiation related risks. This review article describes the utility of 86Y, a positron emitter (33%) with a 14.7-h half-life that can be imaged by positron emission tomography and used as an isotopically matched surrogate radionuclide for 90Y radiation doses estimations. This review discusses various aspects involved in the development of 86Y labeled radiopharmaceuticals with the specific emphasis on the radiochemistry and biological applications with antibodies and peptides.

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Article Details

VOLUME: 7
ISSUE: 5
Page: [380 - 388]
Pages: 9
DOI: 10.2174/157340611796799249