DOI: 10.1186/s41181-018-0044-1Pages: 1-9

Comparison of fully-automated radiosyntheses of [11C]erlotinib for preclinical and clinical use starting from in target produced [11C]CO2 or [11C]CH4

1. Medical University of Vienna, Department of Biomedical Imaging and Image-guided Therapy, Division of Nuclear Medicine

2. University of Vienna, Department of Pharmaceutical Technology and Biopharmaceutics

3. Biomedical Systems, Center for Health & Bioresources, AIT Austrian Institute of Technology GmbH

4. University of Vienna, Department of Nutritional Sciences

5. Ludwig Boltzmann Institute Applied Diagnostics

6. Medical University of Vienna, Department of Clinical Pharmacology

7. CBmed

8. University of Vienna, Department of Inorganic Chemistry

Correspondence to:
Wolfgang Wadsak
Email: wolfgang.wadsak@meduniwien.ac.at

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Abstract

Background

[11C]erlotinib has been proposed as a PET tracer to visualize the mutational status of the epidermal growth factor receptor (EGFR) in cancer patients. For clinical use, a stable, reproducible and high-yielding radiosynthesis method is a prerequisite. In this work, two production schemes for [11C]erlotinib applied in a set of preclinical and clinical studies, starting from either [11C]CH4 or [11C]CO2, are presented and compared in terms of radiochemical yields, molar activities and overall synthesis time. In addition, a time-efficient RP-HPLC method for quality control is presented, which requires not more than 1 min.

Results

[11C]erlotinib was reliably produced applying both methods with decay-corrected radiochemical yields of 13.4 ± 6.2% and 16.1 ± 4.9% starting from in-target produced [11C]CO2 and [11C]CH4, respectively. Irradiation time for the production of [11C]CO2 was higher in order to afford final product amounts sufficient for patient application. Overall synthesis time was comparable, mostly attributable to adaptions in the semi-preparative HPLC protocol. Molar activities were 1.8-fold higher for the method starting from [11C]CH4 (157 ± 68 versus 88 ± 57 GBq/μmol at the end of synthesis).

Conclusions

This study compared two synthetic protocols for the production of [11C]erlotinib with in-target produced [11C]CO2 or [11C]CH4. Both methods reliably yielded sufficiently high product amounts for preclinical and clinical use.

This article is freely available, click here to access the full text/PDF

  • Accepted: May 1, 2018
  • Online: May 30, 2018

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