Transmembrane receptor tyrosine kinase signalling triggers cell proliferation, apoptosis suppression and neovasculature recruitment. Transmembrane receptor tyrosine kinases are overexpressed in many malignancies, which have become the molecular targets for an increasing number of anticancer drugs. For example, monoclonal antibodies and small-molecule tyrosine kinase inhibitors have been clinically proved to boost the therapeutic effect and increase the survival of patients. However, the targeted drugs are clinically limited by specific target and high price, and the early monitoring of therapeutic effects of targeted drugs is important for the design of clinical regimen and reduction of adverse effects and medical expense. The imaging of receptor tyrosine kinase targeted drugs by radionuclide has been clinically employed in the monitoring of therapeutic effects of targeted drugs, and the research progress of this application is reviewed in this paper.