Title: Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme.
Journal: Drug metabolism and disposition: the biological fate of chemicals 20120701
Title: Antagonism of chemokine receptor CXCR3 inhibits osteosarcoma metastasis to lungs.
Journal: International journal of cancer 20091201
Title: Optimization of a series of quinazolinone-derived antagonists of CXCR3.
Journal: Bioorganic & medicinal chemistry letters 20090901
Title: An inhibitory metabolite leads to dose- and time-dependent pharmacokinetics of (R)-N-{1-[3-(4-ethoxy-phenyl)-4-oxo-3,4-dihydro-pyrido[2,3-d]pyrimidin-2-yl]-ethyl}-N-pyridin-3-yl-methyl-2-(4-trifluoromethoxy-phenyl)-acetamide (AMG 487) in human subjects after multiple dosing.
Journal: Drug metabolism and disposition: the biological fate of chemicals 20090301
Title: CXCR3 ANTAGONISTS. WIPO Patent Application WO/2002/083143
