Mass spectrometry imaging (MSI) has seen remarkable development in recent years. The possibility of getting quantitative or semiquantitative data, while maintaining the spatial component in the tissues has opened up unique study possibilities. Now with a spatial window of few tens of microns, we can characterize the events occurring in tissue subcompartments in physiological and pathological conditions. For example, in oncology—especially in preclinical models—we can quantitatively measure drug distribution within tumors, correlating it with pharmacological treatments intended to modify it. We can also study the local effects of the drug in the tissue, and their effects in relation to histology. This review focuses on the main results in the field of drug MSI in clinical pharmacology, looking at the literature on the distribution of drugs in human tissues, and also the first preclinical evidence of drug intratissue effects. The main instrumental techniques are discussed, looking at the different instrumentation, sample preparation protocols, and raw data management employed to obtain the sensitivity required for these studies. Finally, we review the applications that describe in situ metabolic events and pathways induced by the drug, in animal models, showing that MSI makes it possible to study effects that go beyond the simple concentration of the drug, maintaining the space dimension. © 2020 John Wiley & Sons Ltd. Mass Spec Rev

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微观层面的空间维度：组织中药物的质谱成像

近年来，质谱成像 (MSI) 取得了显着的发展。获得定量或半定量数据的可能性，同时保持组织中的空间成分，开辟了独特的研究可能性。现在有了几十微米的空间窗口，我们可以表征生理和病理条件下组织子隔室中发生的事件。例如，在肿瘤学中——尤其是在临床前模型中——我们可以定量测量肿瘤内的药物分布，将其与旨在改变它的药物治疗相关联。我们还可以研究药物在组织中的局部作用，以及它们对组织学的影响。本综述重点介绍了临床药理学中药物MSI领域的主要成果，查看有关药物在人体组织中分布的文献，以及药物组织内效应的第一个临床前证据。讨论了主要的仪器技术，着眼于为获得这些研究所需的灵敏度而采用的不同仪器、样品制备方案和原始数据管理。最后，我们回顾一下描述药物诱导的原位代谢事件和途径，在动物模型中，表明 MSI 可以研究超出药物简单浓度的影响，保持空间维度。© 2020 John Wiley & Sons Ltd. 质谱修订版