PET Imaging for Tyrosine Kinase Inhibitor (TKI) Biodistribution in Mice

Abstract

Receptor tyrosine kinases play a critical role in cell growth, survival, and proliferation, and are considered potential molecular targets for the treatment of cancer. Although several tyrosine kinase inhibitors (TKIs), such as erlotinib and gefi tinib, have demonstrated clinical effi cacy via the inhibition of the epidermal growth factor receptor (EGFR), most TKIs are only effective in a small proportion of patients. Positron emission tomography (PET) imaging is a methodology of molecular imaging based on nuclear imaging. PET imaging in combination with radiolabeled TKIs improves accuracy of quantitative imaging strategies and the probability of successful drug development, and may facilitate the stratifi cation of patients. Here, we describe a protocol for PET imaging using radiolabeled TKI in preclinical trials.