Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
Review
. 2015 Jun 10;8(2):321-36.
doi: 10.3390/ph8020321.

A Critical Review of Alpha Radionuclide Therapy-How to Deal with Recoiling Daughters?

Affiliations
Review

A Critical Review of Alpha Radionuclide Therapy-How to Deal with Recoiling Daughters?

Robin M de Kruijff et al. Pharmaceuticals (Basel). .

Abstract

This review presents an overview of the successes and challenges currently faced in alpha radionuclide therapy. Alpha particles have an advantage in killing tumour cells as compared to beta or gamma radiation due to their short penetration depth and high linear energy transfer (LET). Touching briefly on the clinical successes of radionuclides emitting only one alpha particle, the main focus of this article lies on those alpha-emitting radionuclides with multiple alpha-emitting daughters in their decay chain. While having the advantage of longer half-lives, the recoiled daughters of radionuclides like 224Ra (radium), 223Ra, and 225Ac (actinium) can do significant damage to healthy tissue when not retained at the tumour site. Three different approaches to deal with this problem are discussed: encapsulation in a nano-carrier, fast uptake of the alpha emitting radionuclides in tumour cells, and local administration. Each approach has been shown to have its advantages and disadvantages, but when larger activities need to be used clinically, nano-carriers appear to be the most promising solution for reducing toxic effects, provided there is no accumulation in healthy tissue.

Keywords: alpha-emitters; radionuclide therapy; recoils.

PubMed Disclaimer

Figures

Figure 1
Figure 1
Schematic representation of a recoiling daughter radionuclide detaching from a targeting agent as a consequence of alpha decay.

References

    1. Meredith R.F., Torgue J., Azure M.T., Shen S., Saddekni S., Banaga E., Carlise R., Bunch P., Yoder D., Alvarez R. Pharmacokinetics and imaging of 212Pb-TCMC-trastuzumab after intraperitoneal administration in ovarian cancer patients. Cancer Biother. Radiopharm. 2014;29:12–17. doi: 10.1089/cbr.2013.1531. - DOI - PMC - PubMed
    1. Allen B.J., Singla A.A., Rizvi S.M.A., Graham P., Bruchertseifer F., Apostolidis C., Morgenstern A. Analysis of patient survival in a Phase I trial of systemic targeted α-therapy for metastatic melanoma. Immunotherapy. 2011;3:1041–1050. doi: 10.2217/imt.11.97. - DOI - PubMed
    1. Raja C., Graham P., Rizvi S., Song E., Goldsmith H., Thompson J., Bosserhoff A., Morgenstern A., Apostolidis C., Kearsley J., et al. Interim analysis of toxicity and response in phase 1 trial of systemic targeted alpha therapy for metastatic melanoma. Cancer Biol. Ther. 2007;6:846–852. doi: 10.4161/cbt.6.6.4089. - DOI - PubMed
    1. Mcdevitt M.R., Finn R.D., Ma D., Larson S.M., Scheinberg D.A. Preparation of alpha-Emitting 213Bi-Labeled Antibody Constructs for Clinical Use. J. Nucl. Med. 1999;40:1722–1727. - PubMed
    1. Jurcic J.G., Larson S.M., Sgouros G., Mcdevitt M.R., Finn R.D., Divgi C.R., Ballangrud Å.M., Hamacher K.A., Ma D., Humm J.L., et al. Targeted alpha particle immunotherapy for myeloid leukemia. Blood. 2002;100:1233–1240. - PubMed