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Keith Hoffmaster
Researcher at Novartis
Publications - 27
Citations - 4779
Keith Hoffmaster is an academic researcher from Novartis. The author has contributed to research in topics: Excretion & Drug development. The author has an hindex of 18, co-authored 27 publications receiving 4285 citations. Previous affiliations of Keith Hoffmaster include Pfizer & University of North Carolina at Chapel Hill.
Papers
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Journal ArticleDOI
Membrane transporters in drug development.
Kathleen M. Giacomini,Shiew-Mei Huang,Donald J. Tweedie,Leslie Z. Benet,Kim L. R. Brouwer,Xiaoyan Chu,Amber Dahlin,Raymond Evers,Volker Fischer,Kathleen M. Hillgren,Keith Hoffmaster,Toshihisa Ishikawa,Dietrich Keppler,Richard B. Kim,Caroline A. Lee,Mikko Niemi,Joseph W. Polli,Yuicchi Sugiyama,Peter W. Swaan,Joseph A. Ware,Stephen H. Wright,Sook Wah Yee,Maciej J. Zamek-Gliszczynski,Lei Zhang +23 more
TL;DR: Overall, it is advised that the timing of transporter investigations should be driven by efficacy, safety and clinical trial enrolment questions, as well as a need for further understanding of the absorption, distribution, metabolism and excretion properties of the drug molecule, and information required for drug labelling.
Journal ArticleDOI
Integration of hepatic drug transporters and phase II metabolizing enzymes: mechanisms of hepatic excretion of sulfate, glucuronide, and glutathione metabolites
Maciej J. Zamek-Gliszczynski,Keith Hoffmaster,Ken Ichi Nezasa,Melanie N. Tallman,Kim L. R. Brouwer +4 more
TL;DR: This review summarizes sulfation, glucuronidation, and glutathione conjugation reactions, as well as recent progress in elucidating the hepatic transport mechanisms responsible for the excretion of these conjugates from the liver, and focuses on alterations of metabolism and transport by chemical modulators, and disease states.
Journal ArticleDOI
In Vitro Methods to Support Transporter Evaluation in Drug Discovery and Development
Kim L. R. Brouwer,Dietrich Keppler,Keith Hoffmaster,Daniel A.J. Bow,Yaofeng Cheng,Yurong Lai,J E Palm,Bruno Stieger,Raymond Evers +8 more
TL;DR: In vitro tools to address key questions in drug development, including vesicle‐ and cell‐based systems, are discussed and how these methods can be used to assess the liability of compounds for transporter‐based drug–drug interactions in vivo is explored.
Journal ArticleDOI
Liver tissue engineering in the evaluation of drug safety
Ajit Dash,Walker Inman,Keith Hoffmaster,Samantha Sevidal,Joan M. Kelly,R. Scott Obach,Linda G. Griffith,Steven R. Tannenbaum +7 more
TL;DR: An experimental model is described that captures complex liver physiology through incorporation of heterotypic cell–cell interactions, 3D architecture and perfused flow and is demonstrated how heterotypes can be manipulated to recreate an inflammatory environment and apply the model to test compounds that potentially exhibit idiosyncratic drug toxicity.
Journal ArticleDOI
SHP2 inhibition restores sensitivity in ALK-rearranged non-small-cell lung cancer resistant to ALK inhibitors
Leila Dardaei,Hui Qin Wang,Manrose Singh,Paul Fordjour,Katherine X Shaw,Satoshi Yoda,Grainne Kerr,Kristine Yu,Jinsheng Liang,Yichen Cao,Yan Chen,Michael S. Lawrence,Michael S. Lawrence,Adam Langenbucher,Justin F. Gainor,Luc Friboulet,Ibiayi Dagogo-Jack,David T. Myers,Emma Labrot,David A. Ruddy,Melissa Parks,Dana Lee,Richard H. DiCecca,Susan Moody,Huaixiang Hao,Morvarid Mohseni,Matthew J. LaMarche,Juliet Williams,Keith Hoffmaster,Giordano Caponigro,Alice T. Shaw,Aaron N. Hata,Cyril H. Benes,Fang Li,Jeffrey A. Engelman +34 more
TL;DR: Treatment with SHP099, the recently discovered small-molecule inhibitor of SHP2, in combination with the ALK tyrosine kinase inhibitor (TKI) ceritinib halted the growth of resistant PDCs through preventing compensatory RAS and ERk1 and ERK2 (ERK1/2) reactivation.