Visualization of First-Pass Drug Metabolism of Terfenadine by MALDIImaging Mass Spectrometry

The aim of this article is to focus on the implementation and the application of matrix-assisted laser desorption/ ionization-imaging mass spectrometric system (MALDI-IMS) to determine the disposition or biotransformation pathway of terfenadine and its active metabolite, fexofenadine in mouse and rat whole-body tissue sections. Whole-body MALDI-IMS data showed that the poor oral bioavailability of terfenadine was largely due to high first-pass metabolism in the intestines and the liver before the compound reached systemic circulation.