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

作者：Huclier Markai Sandrine^*; Alliot Cyrille; Varmenot Nicolas; Cutler Cathy S; Barbet Jacques

来源：Current Topics in Medicinal Chemistry, 2012, 12(23): 2642-2654.

• Pb-212
• Bi-212
• Bi-213
• At-211
• Ra-223
• Ac-225

Alpha-particles are of considerable growing interest for Targeted Alpha Therapy (TAT). TAT gains more attention as new targets, chemical labeling techniques and alpha-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 alpha-particle emitters. This article is an up-to-date overview of the literature concerning alpha-emitters used for 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.

• 出版日期2012-12