| Summary: | Systemic anticancer treatments fail in a substantial number of patients. This may be caused by inadequate uptake and penetration of drugs in malignant tumors. Consequently, improvement of drug delivery to solid tumors may enhance its efficacy. Before evaluating strategies to enhance drug uptake in tumors, better understanding of drug delivery to human tumors is needed. Positron emission tomography (PET) is an imaging technique that can be used to monitor drug pharmacokinetics non-invasively in patients, based on radiolabeling these drugs with short-lived positron emitters. In this mini review, principles and potential applications of PET using radiolabeled anticancer drugs will be discussed with respect to personalized treatment planning in oncology. In particular, it will be discussed how these radiolabeled anticancer drugs could help to develop strategies for improved drug delivery to solid tumors. The development and clinical implementation of PET using radiolabeled anticancer drugs will be illustrated by validation studies of carbon-11 labeled docetaxel ([11C]docetaxel) in lung cancer patients.
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