Abstract
This review summarizes recent progress and developments as well as the most important pitfalls in targeted alpha-particle therapy, covering single alpha-particle emitters as well as in vivo alpha-particle generators. It discusses the production of radionuclides like 211At, 223Ra, 225Ac/213Bi, labelling and delivery employing various targeting vectors (small molecules, chelators for alpha-emitting nuclides and their biomolecular targets as well as nanocarriers), general radiopharmaceutical issues, preclinical studies, and clinical trials including the possibilities of therapy prognosis and follow-up imaging. Special attention is given to the nuclear recoil effect and its impacts on the possible use of alpha emitters for cancer treatment, proper dose estimation, and labelling chemistry. The most recent and important achievements in the development of alpha emitters carrying vectors for preclinical and clinical use are highlighted along with an outlook for future developments.
Highlights
Targeted alpha-particle therapy (TAT) is the most rapidly developing field in nuclear medicine and radiopharmacy
To mitigate the consequences of the nuclear recoil effect in the body, we propose three methods based on the corresponding theorems: Theorem 1
Different approaches have been explored to inhibit the accumulation of both parent and daughter radionuclides in critical organs or acceleration of their clearance: co-injection of lysine with 213 Bi-labelled conjugate can reduce kidney uptake of 213 Bi [64], bismuth citrate pre-treatment blocks renal retention of 213 Bi [65], and oral administration of BaSO4 known as a coprecipitating agent of radium reduces the 223 Ra accumulation in the large intestine [66]
Summary
Targeted alpha-particle therapy (TAT) is the most rapidly developing field in nuclear medicine and radiopharmacy. Called in vivo generators [2] that provide, typically, four α decays, depending on the selected radionuclide system, suffer from the nuclear recoil effect, causing at least partial release of daughter radioactive nuclei from the targeting molecule or a delivery vehicle. In such cases, an unwanted radioactive burden is spread over the body and its elimination is limited [3]. Several different approaches were developed regarding the carriers for TAT Small molecules, those labelled with single α emitters, brought the advantage of fast kinetics even though their in vivo stability was not always good. In order to estimate the potential risks and benefits of TAT, we survey important features of different stages of radiopharmaceutical preparation and the directions of required investigation and development
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