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Investigation of metabolism and disposition of GSK1322322, a peptidase deformylase inhibitor, in healthy humans using the entero-test for biliary sampling.

Drug Metab Dispos

August 2014

Department of Drug Metabolism and Pharmacokinetics, GlaxoSmithKline, King of Prussia, Pennsylvania (D.M.F., M.L., E.P., C.B., P.D.G., B.W., L.C., Y.D.) and Ware, United Kingdom (C.F.); Department of Clinical Pharmacology Modeling and Simulation, GlaxoSmithKline, King of Prussia, Pennsylvania (J.Z.); Department of Projects Clinical Pharmacology and Sciences, GlaxoSmithKline, Research Triangle Park, North Carolina (L.J., P.S., O.N., P.P.) and Collegeville, Pennsylvania (E.D.)

GSK1322322 (N-((R)-2-(cyclopentylmethyl)-3-(2-(5-fluoro-6-((S)-hexahydropyrazino[2,1-c][1,4]oxazin-8(1H)-yl)-2-methylpyrimidin-4-yl)hydrazinyl)-3-oxopropyl)-N-hydroxy-formamide) is an antibiotic in development by GlaxoSmithKline. In this study, we investigated the metabolism and disposition of [(14)C]GSK1322322 in healthy humans and demonstrated the utility of the Entero-Test in a human radiolabel study. We successfully collected bile from five men using this easy-to-use device after single i.

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