Abstract

Understanding the biodistribution, metabolism and accumulation of drugs in the body is a fundamental of pharmaceutical research and development. Mass Spectrometry imaging (MSI) has been proven to be a powerful tool to image the unlabelled spatial distribution of exogenous drugs and endogenous metabolites from the surface of tissue sections or small clinical biopsies, aiding the delivery of safe and effective medicines to the market and ultimately benefiting patients. Here we review the current advancements in MSI sample preparation, qualitative and quantitative MSI methodology and drug discovery and development applications. MSI is shown to be supporting R&D from early target identification through to the clinic. In conclusion, we discuss future directions of the technology and the hurdles that need addressing to strengthen its status in multimodal imaging.

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