Visualization of first-pass drug metabolism of terfenadine by MALDI-imaging 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.
Chen
Jiwen
J
Schering-Plough Research Institute, 2015 Galloping Hill Road, K15-3700, Kenilworth, NJ 07033, USA.
Hsieh
Yunsheng
Y
Knemeyer
Ian
I
Crossman
Lee
L
Korfmacher
Walter A
WA
D000818:Animals; D001682:Biological Availability; D039563:Histamine H1 Antagonists, Non-Sedating / Q000493:pharmacokinetics*; D007413:Intestinal Mucosa / Q000378:metabolism; D008099:Liver / Q000378:metabolism; D008297:Male; D051379:Mice; D051381:Rats; D017207:Rats, Sprague-Dawley; D019032:Spectrometry, Mass, Matrix-Assisted Laser Desorption-Ionization / Q000379:methods*; D016593:Terfenadine / Q000031:analogs & derivatives* / Q000493:pharmacokinetics; D014018:Tissue Distribution
D039563:Histamine H1 Antagonists, Non-Sedating; D016593:Terfenadine; C093230:fexofenadine