Current Radiopharmaceuticals

Sean L. Kitson
Current Radiopharmaceuticals
Radiochemistry
Almac Sciences
Almac House
20 Seagoe Industrial Estate
Craigavon, BT63 5QD
Northern Ireland

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Targeted Alpha-Particle Therapy with 227Th-Labeled Antibodies

Author(s): Jostein Dahle, Roy H. Larsen.

Abstract:

A novel technology for preparing low dose rate alpha-radioimmunoconjugates has recently been developed based on the actinide radionuclide 227Th (T1/2=18.7 days). Thorium-227 has interesting properties that can be exploited in radioimmunotherapy: (1) it can be conjugated in stable fashion to antibodies using bifunctional DOTA; (2) it can be produced in virtually unlimited amounts with current technology; (3) it has a half-life suitable for central production and long distance shipment; (4) the alpha-particle released during decay has an average energy of 5.9 MeV, which is well suited for inactivation of tumor cells; (5) the in vivo fate of its radioactive daughter product in terms of distribution and toxicity is well known in animals as well as in humans. This review presents in vitro and in vivo preclinical results obtained using 227Th conjugated to the monoclonal antibodies rituximab and trastuzumab.

Keywords: Alpha-particle radiation, radioimmunotherapy, thorium-227, rituximab, trastuzumab

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Article Details

VOLUME: 1
ISSUE: 3
Year: 2008
Page: [209 - 214]
Pages: 6
DOI: 10.2174/1874471010801030209
Price: $58