Background: Radiopharmaceutical therapy is a cancer treatment modality by which radiation
is delivered directly to targeted tumor cells or to their microenvironment. This makes it possible to deliver
highly potent alpha-particle radiation. The short-range and highly potent nature of alpha-particles
require a dosimetry methodology that considers microscale distributions of the alpha-emitting agent.
The high energy deposition density along an alpha-particle track causes a spectrum of DNA lesions. The
majority of these are irreparable DNA double-stranded breaks. Accordingly the biologic effects of alpha-
particles are largely impervious to the adaptive and resistance mechanism that renders other therapeutics
Objectives: In this review, the radiobiology and dosimetry of alpha-particle emitting radionuclides as
related to their use in radiopharmaceutical therapy, are presented.
Conclusion: Alpha-particle emitter radiopharmaceutical therapy is distinguished from other treatment
modalities. Its safe clinical use requires an understanding of its unique dosimetry and radiobiology.
Keywords: Radiopharmaceutical therapy, alpha-particles, treatment planning, DNA damage, relative biological efficacy.
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