Imaging mass spectrometry in drug discovery and development

This themed issue was compiled to give pharmaceutical researchers, be it analytical, biological or chemical, a brief but current review on mass spectrometry imaging (MSI) technology, methods and applications as used in pharmaceutical research and development, including current challenges and future developments. The strength of MSI lies in its ability to preserve the spatial location of molecular entities in tissues while maintaining the molecular specificity of mass spectrometry. As such, this technology has a unique place in pharmaceutical research and development to provide spatial distribution of unlabeled compounds and their metabolites as well as potential biomarkers of efficacy and toxicity. This unique ability lends to its utility across all aspects of research and development, from target occupancy and drug metabolism and pharmacokinetics, to pharmacodynamics and toxicity. These distinctive aspects and applications of MSI for pharmaceutical research and development have been reviewed in the following articles.