Antibody-targeted radiation cancer therapy

Milenic, Diane E.; Brady, Erik D.; Brechbiel, Martin W.

doi:10.1038/nrd1413

Cited by 380Radiopharmaceutical Chemistry and ApplicationsMonoclonal and Polyclonal Antibodies ResearchEffects of Radiation Exposure

Antibody-targeted radiation cancer therapy

Milenic, Diane E., Brady, Erik D., Brechbiel, Martin W.·2004·Nature Reviews Drug Discovery

DOI 10.1038/nrd1413

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HER2-targeted radioimmunotherapy using radionuclides conjugated to trastuzumab delivers localized radiation directly to tumor cells, enhancing treatment efficacy and reducing systemic side effects.
“Conjugating radionuclides to trastuzumab, a monoclonal antibody specific to HER2 receptors, has demonstrated the potential to deliver localized radiation directly to tumor cells, enhancing treatment efficacy and reducing systemic side effects [96].”
From Radiopharmaceuticals: navigating the frontier of precision medicine and therapeutic innovation (2024) · cites this paper as [96]
The introduction identifies trastuzumab as an anti-HER2 antibody and describes linking antibodies to radioisotopes to target tumour cells, with the promise of greater efficacy and less toxicity (page unavailable). But the “The protein” section discusses anti-HER2 antibodies with external-beam radiation and trastuzumab with chemotherapy—not radionuclides conjugated to trastuzumab. The copy therefore does not establish those claimed benefits for a trastuzumab–radionuclide conjugate. (LLM, conf=0.88)
Experimental — accuracy not yet measured
The cross-fire effect is critical for the improvement of tumor dose homogeneity and for ensuring a sufficient dose for each cell.
“Using β particle emitters, the cross-fire effect is critical for the improvement of tumor dose homogeneity and for ensuring a sufficient dose for each cell [32].”
From Lutathera®: The First FDA- and EMA-Approved Radiopharmaceutical for Peptide Receptor Radionuclide Therapy (2019) · cites this paper as [32]
In “The radionuclide” (page unavailable), the paper says β-emitter crossfire provides therapeutic benefit and can bypass tumour-antigen heterogeneity, making uniform targeting of a lesion possible when the emission range exceeds its radius. This supports improved coverage, but the paper does not say crossfire ensures a sufficient dose for each cell; it also notes limitations for single-cell and disseminated disease. (LLM, conf=0.84)
Experimental — accuracy not yet measured

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Authors: Milenic, D. E., Brady, E. D., & Brechbiel, M. W.
Affiliations: National Institutes of Health (US)
ORCID: Brechbiel, Martin W.
Venue: Nature Reviews Drug Discovery
Publisher: Springer Science and Business Media LLC
Published: 2004-06
Volume: 3
Issue: 6
Pages: 488-499
ISSN: 1474-1776 (ISSN-L)
1474-1784
DOI: 10.1038/nrd1413
OpenAlex: W2034924732
Cited by: 380
References: 93
Citations by year: 2026: 8 · 2025: 10 · 2024: 11 · 2023: 14 · 2022: 18 · 2021: 19 · 2020: 14 · 2019: 20 · 2018: 13 · 2017: 14 · 2016: 14 · 2015: 15 · 2014: 18 · 2013: 27 · 2012: 18
FWCI: 3.77
Type: journal article
Language: en
Open access: closed
Licence: www.springer.com/tdm (tdm)
Locations: Nature Reviews Drug Discovery (publishedVersion)
PubMed (publishedVersion)
Topics: Health Sciences › Medicine › Radiology, Nuclear Medicine and Imaging › Radiopharmaceutical Chemistry and Applications
Health Sciences › Medicine › Radiology, Nuclear Medicine and Imaging › Monoclonal and Polyclonal Antibodies Research
Health Sciences › Medicine › Radiology, Nuclear Medicine and Imaging › Effects of Radiation Exposure
Keywords: radiolabeled monoclonal antibodies, antibody-drug conjugates, radionuclide conjugation, immune effector mechanisms, rituximab, B-cell non-Hodgkin lymphoma, clinical trials, targeted cancer therapy
MeSH terms: Animals, Antibodies, Monoclonal, Antibodies, Neoplasm, Clinical Trials as Topic, Humans, Neoplasms, Drug Delivery Systems

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