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P‐glycoprotein (P‐gp) exhibits a broad substrate specificity and affects pharmacokinetics, especially intestinal absorption. However, prediction, in vivo, of P‐gp‐mediated drug–drug interaction (DDI) and non‐linear absorption at the preclinical stage, is… Click to show full abstract
P‐glycoprotein (P‐gp) exhibits a broad substrate specificity and affects pharmacokinetics, especially intestinal absorption. However, prediction, in vivo, of P‐gp‐mediated drug–drug interaction (DDI) and non‐linear absorption at the preclinical stage, is challenging. Here we evaluate the use of human MDR1 mouse artificial chromosome (hMDR1‐MAC) mice carrying human P‐gp and lacking their own murine P‐gp to quantitatively predict human P‐gp‐mediated DDI and non‐linear absorption.
Journal Title: British Journal of Pharmacology
Year Published: 2021
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