Biodistribution of Zr-89-trastuzumab and PET Imaging of HER2-Positive Lesions in Patients With Metastatic Breast Cancer

Dijkers, E. C., Oude Munnink, T. H., Kosterink, J. G., Brouwers, A. H., Jager, P. L., De Jong, J. R., Van Dongen, G. A., Schröder, C. P., Lub-De Hooge, M. N. & De Vries, E. G., May-2010, In : Clinical Pharmacology & Therapeutics. 87, 5, p. 586-592 7 p.

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  • Biodistribution of 89Zr‐trastuzumab and PET Imaging of HER2‐Positive Lesions in Patients With Metastatic Breast Cancer

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We performed a feasibility study to determine the optimal dosage and time of administration of the monoclonal antibody zirconium-89 (Zr-89)-trastuzumab to enable positron emission tomography (PET) imaging of human epidermal growth factor receptor 2 (HER2)-positive lesions. Fourteen patients with HER2-positive metastatic breast cancer received 37 MBq of Zr-89-trastuzumab at one of three doses (10 or 50 mg for those who were trastuzumab-naive and 10 mg for those who were already on trastuzumab treatment). The patients underwent at least two PET scans between days 2 and 5. The results of the study showed that the best time for assessment of Zr-89-trastuzumab uptake by tumors was 4-5 days after the injection. For optimal PET-scan results, trastuzumab-naive patients required a 50 mg dose of Zr-89-trastuzumab, and patients already on trastuzumab treatment required a 10 mg dose. The accumulation of Zr-89-trastuzumab in lesions allowed PET imaging of most of the known lesions and some that had been undetected earlier. The relative uptake values (RUVs) (mean +/- SEM) were 12.8 +/- 5.8, 4.1 +/- 1.6, and 3.5 +/- 4.2 in liver, bone, and brain lesions, respectively, and 5.9 +/- 2.4, 2.8 +/- 0.7, 4.0 +/- 0.7, and 0.20 +/- 0.1 in normal liver, spleen, kidneys, and brain tissue, respectively. PET scanning after administration of Zr-89-trastuzumab at appropriate doses allows visualization and quantification of uptake in HER2-positive lesions in patients with metastatic breast cancer.

Original languageEnglish
Pages (from-to)586-592
Number of pages7
JournalClinical Pharmacology & Therapeutics
Issue number5
Publication statusPublished - May-2010


  • epidermal growth factor receptor 2, radiopharmaceutical agent, trastuzumab, trastuzumab zr 89, unclassified drug, absence of side effects, adult, aged, article, brain damage, brain metastasis, brain tissue, breast cancer, clinical article, controlled study, dose response, drug blood level, drug bone level, drug brain level, drug distribution, drug dose comparison, drug liver level, drug uptake, feasibility study, female, human, human tissue, kidney, lung metastasis, metastasis, nuclear magnetic resonance imaging, optimal drug dose, positron emission tomography, priority journal, prospective study, spine metastasis, spleen

ID: 5073885