Analysis of the pharmacokinetic/pharmacodynamic relationship of a small molecule CXCR3 antagonist NBI-74330 using a murine CXCR3 internalization assay

摘要

Background and purpose:Pharmacokinetic/pharmacodynamic (PK/PD) models are necessary to relate the degree of drug exposure in vivo to target blockade and pharmacological efficacy. This manuscript describes a murine agonist-induced CXCR3 receptor internalization assay and demonstrates its utility for PK/PD analyses.