Alpha particles more promising than toxins?

Barbet, Jacques; Chérel, Michel; Chatal, Jean‐François

doi:10.1007/s00259-010-1421-5

Cited by 5 publications

(3 citation statements)

References 9 publications

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“…New concepts, approaches, and techniques will be described as well. As yet, numerous review articles related to the development of TAT have been published and are readily available [6][7][8][9][10][11][12][13][14][15][16][17][18][19][20][21], and this discussion will again be principally limited to providing an update those reviews.…”

Section: Introductionmentioning

confidence: 99%

An overview of targeted alpha therapy

2011

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The effectiveness of targeted α-therapy (TAT) can be explained by the properties of α-particles. Alpha particles are helium nuclei and are ~8,000 times larger than β(-)-particles (electrons). When emitted from radionuclides that decay via an α-decay pathway, they release enormous amounts of energy over a very short distance. Typically, the range of α-particles in tissue is 50-100 μm and they have high linear energy transfer (LET) with a mean energy deposition of 100 keV/μm, providing a more specific tumor cell killing ability without damage to the surrounding normal tissues than β(-)-emitters. Due to these properties, the majority of pre-clinical and clinical trials have demonstrated that α-emitters such as (225)Ac, (211)At, (212)Bi, (213)Bi, (212)Pb, (223)Ra, and (227)Th are ideal for the treatment of smaller tumor burdens, micrometastatic disease, and disseminated disease. Even though these α-emitters have favorable properties, the development of TAT has been limited by high costs, unresolved chemistry, and limited availability of the radionuclides. To overcome these limitations, more potent isotopes, additional sources, and more efficient isotope production methods should be addressed. Furthermore, better chelation and labeling methods with the improvements of isotope delivery, targeting vehicles, molecular targets, and identification of appropriate clinical applications are still required.

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Section: Introductionmentioning

confidence: 99%

An overview of targeted alpha therapy

2011

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“…These treatments are generally not curative. More efficient radiopharmaceuticals and more toxic radionuclides, such as alpha-emitters, as well as combination therapy or multiple injection protocols, seldom studied yet in the field of targeted radionuclide therapy, should be developed with the objective of killing the last tumor cell, which is most probably a cancer stem cell ( 25 ). Efficacy of alpha-therapy has been recently shown in a pre-clinical model of multiple myeloma using anti-syndecan 1 MAbs labeled with the alpha-emitter 213 Bi ( 26 ).…”

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confidence: 99%

“…Radionuclide such as 131 I, 177 Lu, or 67 Cu with shorter-range beta − emissions should be more favorable in the minimal residual disease setting. Alpha particle emitters offer the theoretical possibility to kill isolated tumor cells and microscopic clusters of tumor cells because of the short tracks of alpha particles ( 25 ). For alpha-emitters, 213 Bi is available through a 225 Ac/ 213 Bi generator.…”

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confidence: 99%