Astatine-211: Production and Availability

Overview

Journal Curr Radiopharm

Publisher Bentham Science Publishers

Specialties Nuclear Medicine
Pharmacology
Radiology

Date 2011 Dec 29

PMID 22201707

Citations 62

Authors

Michael R Zalutsky

Marek Pruszynski

Affiliations

Soon will be listed here.

Abstract

The 7.2-h half life radiohalogen (211)At offers many potential advantages for targeted α-particle therapy; however, its use for this purpose is constrained by its limited availability. Astatine-211 can be produced in reasonable yield from natural bismuth targets via the (209)Bi(α,2n)(211)At nuclear reaction utilizing straightforward methods. There is some debate as to the best incident α-particle energy for maximizing 211At production while minimizing production of (210)At, which is problematic because of its 138.4-day half life α-particle emitting daughter, (210)Po. The intrinsic cost for producing (211)At is reasonably modest and comparable to that of commercially available (123)I. The major impediment to (211)At availability is attributed to the need for a medium energy α-particle beam for its production. On the other hand, there are about 30 cyclotrons in the world that have the beam characteristics required for (211)At production.

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References

Harrison J, Leggett R, Lloyd D, Phipps A, Scott B . Polonium-210 as a poison. J Radiol Prot. 2007; 27(1):17-40. DOI: 10.1088/0952-4746/27/1/001. View

Larsen R, Wieland B, Zalutsky M . Evaluation of an internal cyclotron target for the production of 211At via the 209Bi (alpha,2n)211 at reaction. Appl Radiat Isot. 1996; 47(2):135-43. DOI: 10.1016/0969-8043(95)00285-5. View

Vaidyanathan G, Zalutsky M . Astatine Radiopharmaceuticals: Prospects and Problems. Curr Radiopharm. 2010; 1(3):177. PMC: 2818997. DOI: 10.2174/1874471010801030177. View

Andersson H, Cederkrantz E, Back T, Divgi C, Elgqvist J, Himmelman J . Intraperitoneal alpha-particle radioimmunotherapy of ovarian cancer patients: pharmacokinetics and dosimetry of (211)At-MX35 F(ab')2--a phase I study. J Nucl Med. 2009; 50(7):1153-60. DOI: 10.2967/jnumed.109.062604. View

Zalutsky M, Reardon D, Pozzi O, Vaidyanathan G, Bigner D . Targeted alpha-particle radiotherapy with 211At-labeled monoclonal antibodies. Nucl Med Biol. 2007; 34(7):779-85. PMC: 2083568. DOI: 10.1016/j.nucmedbio.2007.03.007. View

Vaidyanathan G, Affleck D, Schottelius M, Wester H, Friedman H, Zalutsky M . Synthesis and evaluation of glycosylated octreotate analogues labeled with radioiodine and 211At via a tin precursor. Bioconjug Chem. 2006; 17(1):195-203. DOI: 10.1021/bc0502560. View

. 1990 Recommendations of the International Commission on Radiological Protection. Ann ICRP. 1991; 21(1-3):1-201. View

Pozzi O, Zalutsky M . Radiopharmaceutical chemistry of targeted radiotherapeutics, Part 3: alpha-particle-induced radiolytic effects on the chemical behavior of (211)At. J Nucl Med. 2007; 48(7):1190-6. DOI: 10.2967/jnumed.106.038505. View

Groppi F, Bonardi M, Birattari C, Menapace E, Abbas K, Holzwarth U . Optimisation study of alpha-cyclotron production of At-211/Po-211g for high-LET metabolic radiotherapy purposes. Appl Radiat Isot. 2005; 63(5-6):621-31. DOI: 10.1016/j.apradiso.2005.05.041. View

10.

Zalutsky M, Reardon D, Akabani G, Coleman R, Friedman A, Friedman H . Clinical experience with alpha-particle emitting 211At: treatment of recurrent brain tumor patients with 211At-labeled chimeric antitenascin monoclonal antibody 81C6. J Nucl Med. 2007; 49(1):30-8. PMC: 2832604. DOI: 10.2967/jnumed.107.046938. View

11.

Hermanne A, Tarkanyi F, Takacs S, Szucs Z, Shubin Y, Dityuk A . Experimental study of the cross-sections of alpha-particle induced reactions on 209Bi. Appl Radiat Isot. 2005; 63(1):1-9. DOI: 10.1016/j.apradiso.2005.01.015. View

12.

Pozzi O, Zalutsky M . Radiopharmaceutical chemistry of targeted radiotherapeutics, part 1: effects of solvent on the degradation of radiohalogenation precursors by 211At alpha-particles. J Nucl Med. 2005; 46(4):700-6. View

13.

Roy K, Basu S, Ramaswami A, Nayak D, Lahiri S . Incorporation of thiosemicarbazide in Amberlite IRC-50 for separation of astatine from alpha-irradiated bismuth oxide. Appl Radiat Isot. 2004; 60(6):793-9. DOI: 10.1016/j.apradiso.2003.12.011. View

14.

Johnson E, Turkington T, Jaszczak R, Gilland D, Vaidyanathan G, Greer K . Quantitation of 211At in small volumes for evaluation of targeted radiotherapy in animal models. Nucl Med Biol. 1995; 22(1):45-54. DOI: 10.1016/0969-8051(94)00077-w. View

15.

Talanov V, Garmestani K, Regino C, Milenic D, Plascjak P, Waldmann T . Preparation and in vivo evaluation of a novel stabilized linker for 211At labeling of protein. Nucl Med Biol. 2006; 33(4):469-80. DOI: 10.1016/j.nucmedbio.2006.03.001. View

16.

Henriksen G, Messelt S, Olsen E, Larsen R . Optimisation of cyclotron production parameters for the 209Bi(alpha, 2n) 211At reaction related to biomedical use of 211At. Appl Radiat Isot. 2001; 54(5):839-44. DOI: 10.1016/s0969-8043(00)00346-8. View

17.

Haddad F, Ferrer L, Guertin A, Carlier T, Michel N, Barbet J . ARRONAX, a high-energy and high-intensity cyclotron for nuclear medicine. Eur J Nucl Med Mol Imaging. 2008; 35(7):1377-87. DOI: 10.1007/s00259-008-0802-5. View

18.

Barbet J, Chatal J, Gauche F, Martino J . Which radionuclides will nuclear oncology need tomorrow?. Eur J Nucl Med Mol Imaging. 2006; 33(6):627-30. DOI: 10.1007/s00259-006-0116-4. View

19.

Champion J, Alliot C, Renault E, Mokili B, Cherel M, Galland N . Astatine standard redox potentials and speciation in acidic medium. J Phys Chem A. 2009; 114(1):576-82. DOI: 10.1021/jp9077008. View

20.

Schwarz U, Plascjak P, Beitzel M, Gansow O, Eckelman W, Waldmann T . Preparation of 211At-labeled humanized anti-Tac using 211At produced in disposable internal and external bismuth targets. Nucl Med Biol. 1998; 25(2):89-93. DOI: 10.1016/s0969-8051(97)00165-0. View