The discovery and increased understanding of tumor targets has led to the development and approval of 12 small molecule tyrosine kinase inhibitors (TKIs). Despite tremendous efforts in TKI development, treatment efficacies with these therapeutics are still too low and improvements require a personalized medicine approach. Positron emission tomography (PET) with radiolabeled TKIs (TKI-PET) is a tracking, quantification and imaging method, which provides a unique understanding of the behavior of these drugs in vivo and of the interaction with their target(s). In this article we provide an overview of tracer synthesis and development because each TKI requires a tailor made approach. Moreover, we describe current preclinical work and the first proof-of-principle clinical studies on the application of TKI-PET, illustrating the potential of this approach for improving therapy efficacy and personalized cancer treatment.
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