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Drug Metab Dispos. 2021 Dec;49(12):1109-1117. doi: 10.1124/dmd.121.000595. Epub 2021 Oct 08.

Pharmacokinetics and ADME Characterization of Intravenous and Oral [.

Drug metabolism and disposition: the biological fate of chemicals

Maciej J Zamek-Gliszczynski, David Kenworthy, David A Bershas, Mitesh Sanghvi, Adrian I Pereira, Jennypher Mudunuru, Lee Crossman, Jill L Pirhalla, Karl M Thorpe, Jeremy M T J Dennison, Megan M McLaughlin, Matthew Allinder, Brandon Swift, Robin L O'Connor-Semmes, Graeme C Young

Affiliations

  1. Drug Metabolism and Disposition (M.J.Z.-G., D.A.B., J.M., J.L.P.), Medicine Development (M.M.M.), and Development Biostatistics (M.A.), GlaxoSmithKline, Collegeville, Pennsylvania; Drug Metabolism and Disposition (D.K., G.C.Y.), and Bioanalysis, Immunogenicity and Biomarkers (A.I.P.), GlaxoSmithKline, Ware, United Kingdom; Pharmaron ABS Inc., Germantown, Maryland (M.S.); Covance, Harrogate, United Kingdom (L.C.); Global Clinical Development, GlaxoSmithKline, Brentford, United Kingdom (K.M.T.); Hammersmith Medicines Research, London, United Kingdom (J.M.T.J.D.); Clinical Pharmacology, Modeling and Simulation, GlaxoSmithKline, RTP, North Carolina (B.S.); and Clinical Pharmacology, Modeling and Simulation, Parexel, Durham, North Carolina (R.L.O.-S.) [email protected].
  2. Drug Metabolism and Disposition (M.J.Z.-G., D.A.B., J.M., J.L.P.), Medicine Development (M.M.M.), and Development Biostatistics (M.A.), GlaxoSmithKline, Collegeville, Pennsylvania; Drug Metabolism and Disposition (D.K., G.C.Y.), and Bioanalysis, Immunogenicity and Biomarkers (A.I.P.), GlaxoSmithKline, Ware, United Kingdom; Pharmaron ABS Inc., Germantown, Maryland (M.S.); Covance, Harrogate, United Kingdom (L.C.); Global Clinical Development, GlaxoSmithKline, Brentford, United Kingdom (K.M.T.); Hammersmith Medicines Research, London, United Kingdom (J.M.T.J.D.); Clinical Pharmacology, Modeling and Simulation, GlaxoSmithKline, RTP, North Carolina (B.S.); and Clinical Pharmacology, Modeling and Simulation, Parexel, Durham, North Carolina (R.L.O.-S.).

PMID: 34625435 DOI: 10.1124/dmd.121.000595

Abstract

Linerixibat, an oral small-molecule ileal bile acid transporter inhibitor under development for cholestatic pruritus in primary biliary cholangitis, was designed for minimal absorption from the intestine (site of pharmacological action). This study characterized the pharmacokinetics, absorption, metabolism, and excretion of [

Copyright © 2021 by The Author(s).

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