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Updated: May 27, 2026

Whole-body Mass Spectrometry Imaging by Infrared Matrix-assisted Laser Desorption Electrospray Ionization (IR-MALDESI)
Published on: March 24, 2016
MALDI imaging mass spectrometry: bridging biology and chemistry in drug development
Stephen Castellino1, M Reid Groseclose, David Wagner
1Department of Drug Metabolism & Pharmacokinetics, Platform Science & Technology, GlaxoSmithKline, RTP, NC 27709, USA. steve.x.castellino@gsk.com
Abstract:
Our understanding of drug tissue distribution impacts a number of areas in drug development, including: pharmacology, pharmacokinetics, safety, drug-drug interactions, transport and metabolism. Despite their extensive use, autoradiography and tissue homogenate LC-MS analysis have limitations in providing a comprehensive assessment of tissue distributions. In the case of autoradiography, it is the inability to distinguish between parent drug and drug metabolites. In LC-MS analysis of tissue homogenate, all tissue localization information is lost. The emerging technique of MALDI imaging mass spectrometry has the capability to distinguish between parent and metabolites while maintaining spatial distribution in tissues. In this article, we will review the MALDI imaging MS methodology as applied to drug development and provide examples highlighting the impact of this important technique in drug development.
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