Radionuclide imaging of drug delivery for patient selection in targeted therapy

During the last decade, numerous antibodies and tyrosine kinase inhibitors have been developed for cancer treatment. However, only a limited number of these agents have been shown to significantly improve survival of patients. Therefore, it is of crucial importance to identify the subset of patients who benefit from targeted therapy. Biomarkers can play an important role in selecting the right drug for the right patient.

In this review, the potential role of molecular imaging of drug delivery for patient selection in targeted therapy will be discussed. The advantages and limitations of molecular imaging will be compared to those of conventional biomarkers. Moreover, we will address the factors that affect imaging of drug delivery, such as target expression, type of drug, in vivo accessibility of the receptor (e.g., vascular density, vascular permeability, interstitial pressure), enhanced permeability and retention (EPR) effect, receptor internalization, tracer protein dose and timing of imaging.

Molecular imaging of drug delivery clearly has potential for patient selection for targeted therapy. The main advantage of this technique is that not only can antigen expression be measured noninvasively but also target accessibility is taken into account. However, up to now, most of these studies have been performed in preclinical models. Therefore, future research should focus on bringing promising tracers to the clinic, preferable in an early stage of drug development in order to test their potential role as a biomarker.