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Background  [ 11 C]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 [ 11 C]erlotinib applied in a set of preclinical and clinical studies, starting from either [ 11 C]CH 4  or [ 11 C]CO 2 , 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  [ 11 C]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 [ 11 C]CO 2  and [ 11 C]CH 4 , respectively. Irradiation time for the production of [ 11 C]CO 2  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 [ 11 C]CH 4  (157 ± 68 versus 88 ± 57 GBq/μmol at the end of synthesis).    Conclusions  This study compared two synthetic protocols for the production of [ 11 C]erlotinib with in-target produced [ 11 C]CO 2  or [ 11 C]CH 4 . Both methods reliably yielded sufficiently high product amounts for preclinical and clinical use.

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