In recent years the analysis in mass spectrometry (MS) [corrected] imaging has been expanded to detect a wide variety of low molecular weight compounds (LMWC), including exogenous and endogenous compounds. The high sensitivity and selectivity of MS imaging combined with visualization of molecular spatial distribution in tissues, makes it a valuable [corrected] platform in targeted drug and untargeted metabolomic analysis [corrected] in biological and clinical research. Here, we review the current and potential applications of MALDI MS imaging in these areas. The aim of advancing MALDI MS imaging in the field of LMWC is to support clinical applications by understanding drug and drug-metabolite distribution, investigating toxicity and discovering [corrected] new biomarkers.