Keith Hoffmaster

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.

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.

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.

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.

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.