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Research ArticleThe State of The Art

Harnessing α-Emitting Radionuclides for Therapy: Radiolabeling Method Review

Hua Yang, Justin J. Wilson, Chris Orvig, Yawen Li, D. Scott Wilbur, Caterina F. Ramogida, Valery Radchenko and Paul Schaffer
Journal of Nuclear Medicine January 2022, 63 (1) 5-13; DOI: https://doi.org/10.2967/jnumed.121.262687
Hua Yang
1Life Sciences Division, TRIUMF, Vancouver, British Columbia, Canada;
2Department of Chemistry, Simon Fraser University, Burnaby, British Columbia, Canada;
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Justin J. Wilson
3Chemistry and Chemical Biology, Cornell University, Ithaca, New York;
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Chris Orvig
4Medicinal Inorganic Chemistry Group, Department of Chemistry, University of British Columbia, Vancouver, British Columbia, Canada;
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Yawen Li
5Department of Radiation Oncology, University of Washington, Seattle, Washington;
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D. Scott Wilbur
5Department of Radiation Oncology, University of Washington, Seattle, Washington;
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Caterina F. Ramogida
1Life Sciences Division, TRIUMF, Vancouver, British Columbia, Canada;
2Department of Chemistry, Simon Fraser University, Burnaby, British Columbia, Canada;
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Valery Radchenko
1Life Sciences Division, TRIUMF, Vancouver, British Columbia, Canada;
6Department of Chemistry, University of British Columbia, Vancouver, British Columbia, Canada; and
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Paul Schaffer
1Life Sciences Division, TRIUMF, Vancouver, British Columbia, Canada;
2Department of Chemistry, Simon Fraser University, Burnaby, British Columbia, Canada;
7Department of Radiology, University of British Columbia, Vancouver, British Columbia, Canada
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Article Figures & Data

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  • FIGURE 1.
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    FIGURE 1.

    Chelates for 149Tb. RT = room temperature.

  • FIGURE 2.
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    FIGURE 2.

    211At labeling methods. DMF = dimethylformamide; NaX = [125I]NaI or [211At]NaAt.

  • FIGURE 3.
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    FIGURE 3.

    212/213Bi chelators. N/A = not applicable; RT = room temperature.

  • FIGURE 4.
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    FIGURE 4.

    Chelators for 212Pb. N/A = not applicable; RT = room temperature.

  • FIGURE 5.
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    FIGURE 5.

    Chelators for 223Ra. RT = room temperature.

  • FIGURE 6.
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    FIGURE 6.

    Chelators for 225Ac. N/A = not applicable; RT = room temperature.

  • FIGURE 7.
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    FIGURE 7.

    Chelators for 226/227Th. N/A = not applicable; RT = room temperature.

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    TABLE 1.

    Isotopes for TAT

    IsotopeHalf-lifeCommon ionIonic radius (Å)Common coordination numberHard/softpKa (aqueous)
    149Tb4.1 hTb3+1.048–9Hard7.9
    211At7.2 hAt+, AtO+————
    212Bi60.6 minBi3+1.178Intermediate1.1
    213Bi45.6 minBi3+1.178Intermediate1.1
    212Pb (for 212Bi)10.6 hPb2+1.438Intermediate0.9
    223Ra11.4 dRa2+1.488–12Hard3.1
    225Ac9.9 dAc3+1.129–10Hard9.4
    226Th30.7 minTh4+1.05>8Hard3.2
    227Th18.7 dTh4+1.05>8Hard3.2
    230U20.8 d[UO2]2+—6Hard4.2
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Journal of Nuclear Medicine: 63 (1)
Journal of Nuclear Medicine
Vol. 63, Issue 1
January 1, 2022
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Harnessing α-Emitting Radionuclides for Therapy: Radiolabeling Method Review
Hua Yang, Justin J. Wilson, Chris Orvig, Yawen Li, D. Scott Wilbur, Caterina F. Ramogida, Valery Radchenko, Paul Schaffer
Journal of Nuclear Medicine Jan 2022, 63 (1) 5-13; DOI: 10.2967/jnumed.121.262687

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Harnessing α-Emitting Radionuclides for Therapy: Radiolabeling Method Review
Hua Yang, Justin J. Wilson, Chris Orvig, Yawen Li, D. Scott Wilbur, Caterina F. Ramogida, Valery Radchenko, Paul Schaffer
Journal of Nuclear Medicine Jan 2022, 63 (1) 5-13; DOI: 10.2967/jnumed.121.262687
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Keywords

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