[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. [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). 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.

中文翻译：

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从靶标产生的 [11C]CO2 或 [11C]CH4 开始，对[11C]厄洛替尼的临床前和临床使用的全自动放射合成进行比较。

[11C]厄洛替尼已被提议作为 PET 示踪剂，以可视化癌症患者表皮生长因子受体 (EGFR) 的突变状态。对于临床应用来说，稳定、重复性好、高产的放射合成方法是先决条件。在这项工作中，提出了两种用于一系列临床前和临床研究的[11C]厄洛替尼生产方案，从[11C]CH4或[11C]CO2开始，在放射化学产率、摩尔活性和总体合成方面进行了比较时间。此外，还提出了一种省时的 RP-HPLC 质量控制方法，该方法所需时间不超过 1 分钟。使用这两种方法可靠地生产了[11C]厄洛替尼，从目标内产生的[11C]CO2和[11C]CH4开始，衰变校正的放射化学产率分别为13.4±6.2%和16.1±4.9%。产生[11C]CO2 的辐照时间较长，以便提供足够患者使用的最终产品量。总合成时间相当，主要归因于半制备型 HPLC 方案的调整。从 [11C]CH4 开始的方法的摩尔活性高出 1.8 倍（合成结束时为 157 ± 68 GBq/μmol 与 88 ± 57 GBq/μmol）。本研究比较了两种生产[11C]厄洛替尼的合成方案与目标产生的[11C]CO2 或[11C]CH4。两种方法都可靠地产生了足够高的产品量，可供临床前和临床使用。