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Synthesis and Preliminary Evaluation of the <sup>211</sup>At-Labeled PARP Inhibitor [<sup>211</sup>At]Talazoparib as a Targeted Alpha-Particle Emitting Therapeutic.

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Related Experiment Video

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Structural Studies of Macromolecules in Solution using Small Angle X-Ray Scattering
07:19

Structural Studies of Macromolecules in Solution using Small Angle X-Ray Scattering

Published on: November 5, 2018

Astatine-211: production and availability.

Michael R Zalutsky1, Marek Pruszynski

  • 1Department of Radiology, Duke University Medical Center, Durham, NC 27710 USA. zalut001@mc.duke.edu

Current Radiopharmaceuticals
|December 29, 2011
PubMed
Summary

Astatine-211 (211At) shows promise for targeted alpha therapy due to its short half-life. Its limited availability stems from production challenges, despite modest costs and existing cyclotron infrastructure.

Area of Science:

  • Nuclear Medicine
  • Radiochemistry
  • Medical Physics

Background:

  • Astatine-211 (211At) is a radiohalogen with a 7.2-hour half-life, making it suitable for targeted alpha-particle therapy.
  • Current limitations in 211At availability hinder its widespread application in therapy.
  • Production of 211At is feasible via the (209)Bi(α,2n)(211)At nuclear reaction using natural bismuth targets.

Purpose of the Study:

  • To evaluate the potential advantages and constraints of using Astatine-211 for targeted alpha-particle therapy.
  • To address the debate surrounding optimal alpha-particle energy for maximizing 211At production while minimizing problematic 210At co-production.
  • To assess the cost-effectiveness and availability challenges of 211At.

Main Methods:

  • Production of 211At through the nuclear reaction of bismuth-209 with alpha particles.

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  • Analysis of factors influencing 211At yield and the minimization of 210At byproduct.
  • Comparison of 211At production costs with existing radioisotopes like Iodine-123.

    • Main Results:

    • The intrinsic cost of producing 211At is comparable to commercially available Iodine-123.
    • The primary obstacle to 211At availability is the requirement for a medium-energy alpha-particle beam.
    • Approximately 30 cyclotrons globally possess the necessary beam characteristics for 211At production.

    Conclusions:

    • Astatine-211 offers significant potential for targeted alpha-particle therapy.
    • Despite production challenges, the necessary infrastructure (cyclotrons) exists globally.
    • Addressing production optimization and beam requirements is key to increasing 211At availability.