Alpha-emitters for immuno-therapy: a review of recent developments from chemistry to clinics

Curr Top Med Chem. 2012;12(23):2642-54. doi: 10.2174/1568026611212230002.

Abstract

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.

Publication types

  • Review

MeSH terms

  • Alpha Particles / therapeutic use*
  • Antibodies / chemistry
  • Antibodies / immunology
  • Chelating Agents / chemistry
  • Clinical Trials as Topic
  • Half-Life
  • Humans
  • Molecular Targeted Therapy
  • Neoplasms / diagnosis
  • Neoplasms / immunology
  • Neoplasms / radiotherapy*
  • Radioimmunotherapy*
  • Radioisotopes / isolation & purification
  • Radioisotopes / therapeutic use*
  • Radiometry
  • Radiopharmaceuticals / isolation & purification
  • Radiopharmaceuticals / therapeutic use*

Substances

  • Antibodies
  • Chelating Agents
  • Radioisotopes
  • Radiopharmaceuticals