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Current Topics in Medicinal Chemistry


ISSN (Print): 1568-0266
ISSN (Online): 1873-4294

Alpha-Emitters for Immuno-Therapy: A Review of Recent Developments from Chemistry to Clinics

Author(s): Sandrine Huclier-Markai, Cyrille Alliot, Nicolas Varmenot, Cathy S. Cutler and Jacques Barbet

Volume 12, Issue 23, 2012

Page: [2642 - 2654] Pages: 13

DOI: 10.2174/1568026611212230002


Alpha-particles are of considerable growing interest for Targeted Alpha Therapy (TAT). TAT gains more attention as new targets, chemical labeling techniques and α-particle emitters are developed but translation of TAT into the clinic has been slow, in part because of the limited availability and the short physical half-lives of some of the available α- particle emitters. This article is an up-to-date overview of the literature concerning α-emitters used for TAT of cancer. It briefly describes the nuclear characteristics, the production parameters (targets, extraction and purification), the complexation properties of these radionuclides to chelates and biological vectors and finally draws-upon the preclinical and clinical studies that have been performed over the past two decades. Radiobiology and dosimetry aspects are also presented in this paper.

Keywords: 212Pb, 212Bi, 213Bi, 211At, 223Ra, 225Ac

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