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Astatine-211-labeled radiotherapeutics: an emerging approach to targeted alpha-particle radiotherapy.

Publication ,  Journal Article
Zalutsky, MR; Vaidyanathan, G
Published in: Curr Pharm Des
September 2000

Targeted radiotherapy or endoradiotherapy is an appealing approach to cancer treatment because of the potential for delivering curative doses of radiation to tumor while sparing normal tissues. Radionuclides that decay by the emission of alpha-particles such as the heavy halogen astatine-211 (211At) offer the exciting prospect of combining cell-specific molecular targets with radiation having a range in tissue of only a few cell diameters. Herein, the radiobiological advantages of alpha-particle targeted radiotherapy will be reviewed, and the rationale for using 211At for this purpose will be described. The chemistry of astatine is similar to that of iodine; however, there are important differences which make the synthesis and evaluation of 211At-labeled compounds more challenging. Perhaps the most successful approach that has been developed involves the astatodemetallation of tin, silicon or mercury precursors. Astatine-211 labeled agents that have been investigated for targeted radiotherapy include [211At]astatide, 211At- labeled particulates, 211At-labeled naphthoquinone derivatives, 211At-labeled methylene blue, 211At-labeled DNA precursors, meta-[211At]astatobenzylguanidine, 211At-labeled biotin conjugates, 211At-labeled bisphosphonates, and 211At-labeled antibodies and antibody fragments. The status of these 211At-labeled compounds will be discussed in terms of their labeling chemistry, cytotoxicity in cell culture, as well as their tissue distribution and therapeutic efficacy in animal models of human cancers. Finally, an update on the status of the first clinical trial with an 211At-labeled targeted therapeutic, 211At-labeled chimeric anti-tenascin antibody 81C6, will be provided.

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Published In

Curr Pharm Des

DOI

ISSN

1381-6128

Publication Date

September 2000

Volume

6

Issue

14

Start / End Page

1433 / 1455

Location

United Arab Emirates

Related Subject Headings

  • Radioimmunotherapy
  • Neoplasms
  • Medicinal & Biomolecular Chemistry
  • Humans
  • DNA
  • Brachytherapy
  • Astatine
  • Antibodies, Monoclonal
  • Alpha Particles
  • 3214 Pharmacology and pharmaceutical sciences
 

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Zalutsky, M. R., & Vaidyanathan, G. (2000). Astatine-211-labeled radiotherapeutics: an emerging approach to targeted alpha-particle radiotherapy. Curr Pharm Des, 6(14), 1433–1455. https://doi.org/10.2174/1381612003399275
Zalutsky, M. R., and G. Vaidyanathan. “Astatine-211-labeled radiotherapeutics: an emerging approach to targeted alpha-particle radiotherapy.Curr Pharm Des 6, no. 14 (September 2000): 1433–55. https://doi.org/10.2174/1381612003399275.
Zalutsky MR, Vaidyanathan G. Astatine-211-labeled radiotherapeutics: an emerging approach to targeted alpha-particle radiotherapy. Curr Pharm Des. 2000 Sep;6(14):1433–55.
Zalutsky, M. R., and G. Vaidyanathan. “Astatine-211-labeled radiotherapeutics: an emerging approach to targeted alpha-particle radiotherapy.Curr Pharm Des, vol. 6, no. 14, Sept. 2000, pp. 1433–55. Pubmed, doi:10.2174/1381612003399275.
Zalutsky MR, Vaidyanathan G. Astatine-211-labeled radiotherapeutics: an emerging approach to targeted alpha-particle radiotherapy. Curr Pharm Des. 2000 Sep;6(14):1433–1455.
Journal cover image

Published In

Curr Pharm Des

DOI

ISSN

1381-6128

Publication Date

September 2000

Volume

6

Issue

14

Start / End Page

1433 / 1455

Location

United Arab Emirates

Related Subject Headings

  • Radioimmunotherapy
  • Neoplasms
  • Medicinal & Biomolecular Chemistry
  • Humans
  • DNA
  • Brachytherapy
  • Astatine
  • Antibodies, Monoclonal
  • Alpha Particles
  • 3214 Pharmacology and pharmaceutical sciences