Liver imaging

  • Radiology. 2019;290:125-133. Quantitative assessment of liver function by using Gadoxetic acid-enhanced MRI: hepatocyte uptake ratio. Yoon JH, Lee JM, Kang HJ, Ahn SJ, Yang H, Kim E, Okuaki T, Han JK. PubMed
  • Clin Pharmacol Ther. 2018;in press. Impact of acute alcohol exposure on P-Glycoprotein function at the Blood Brain Barrier assessed Using 11C-Metoclopramide PET imaging. Auvity S, Tournier N. PubMed
  • J Nucl Med. 2019, in press. Impact of P-glycoprotein function on the brain kinetics of the weak substrate 11C-Metoclopramide assessed with PET imaging in humans. Tournier N, Bauer M, Pichler V, Nics L, Klebermass EM, Bamminger K, Matzneller P, Weber M, Karch R, Caille F, Auvity S, Marie S, Jaeger W, Wadsak W, Hacker M, Zeitlinger M, Langer O. PubMed
  • Diabetes. 2019;68:271-280. Dynamic contrast-enhanced MRI of OATP dysfunction in diabetes. Shuboni-Mulligan DD, Parys M, Blanco-Fernandez B, Mallett CL, Schnegelberger R, Takada M, Chakravarty S, Hagenbuch B, Shapiro EM. PubMed
  • Drug Metab Dispos. 2019; in press. Hepatocyte concentrations of imaging compounds associated with transporter inhibition: evidence in perfused rat livers. Bonnaventure P, Cusin F, Pastor C. PubMed

Hepatic clearance

  • Drug Metab Dispos. 2019;47:58-66. Meeting the challenge of predicting hepatic clearance of compounds slowly metabolized by Cytochrome P450 using a novel hepatocyte model, HepatoPac. Chan TS, Yu H, Moore A, Khetani SR, Tweedie D. PubMed
  • Drug Metab Dispos. 2019;47:94-103. Extrapolation of in vivo hepatic clearance from in vitro uptake clearance by suspended human hepatocytes for anionic drugs with high ginding to human albumin: improvement of in vitro-to-in vivo extrapolation by considering the "albumin-mediated" hepatic uptake mechanism on the basis of the "facilitated-dissociation model". Kim SJ, Lee KR, Miyauchi S, Sugiyama Y. PubMed
  • Eur J Pharm Sci. 2018;125:181-192. Strategies to improve the prediction accuracy of hepatic intrinsic clearance of three antidiabetic drugs: Application of the extended clearance concept and consideration of the effect of albumin on CYP2C metabolism and OATP1B-mediated hepatic uptake. Fujino R, Hashizume K, Aoyama S, Maeda K, Ito K, Toshimoto K, Lee W, Ninomiya SI, Sugiyama Y. PubMed
  • Drug Metab Dispos. 2019;in press.  The Presence of a transporter-induced protein binding shift: A new explanation for protein-facilitated uptake and improvement for in vitro-in vivo extrapolation. Bowman CM, Okochi H, Benet LZ. PubMed
  • Drug Metab Dispos. 2018; in press. Hepatic OATP-mediated clearance in the Beagle dog: assessing in vitro-in vivo relationships and applying cross species empirical scaling factors to improve prediction of human clearance. Matsunaga N, Ufuk A, Morse BL, Bedwell DW, Bao J, Mohutsky MA, Hillgren KM, Hall SD, Houston JB, Galetin A. PubMed

Hepatocellular concentrations

  • Clin Pharmacol Ther. 2019;105:190-200. OCT1 deficiency affects hepatocellular concentrations and pharmacokinetics of Cycloguanil, the active metabolite of the antimalarial drug Proguanil. Matthaei J, Seitz T, Jensen O, Tann A, Prukop T, Tadjerpisheh S, Brockmöller J, Tzvetkov MV. PubMed

Quantification of transporters

  • Clin Pharmacol Ther. 2018;In press. Protein abundance of clinically relevant drug transporters in the human liver and intestine: a comparative analysis in paired tissue specimens. Drozdzik M, Busch D, Lapczuk J, Müller J, Ostrowski M, Kurzawski M, Oswald S. PubMed
  • Drug Metab Dispos. 2019; in press. A comparison of total and plasma membrane abundance of transporters in suspended, plated, Sandwich-Cultured Human Hepatocytes vs. human liver tissue using quantitative targeted proteomics and cell-surface biotinylation. Kumar V, Salphati L, Hop CECA, Xiao G, Lai Y, Mathias A, Chu X, Humphreys WG, Liao M, Heyward S, Unadkat JD. PubMed
  • Proteomics. 2018;In press. GASP and FASP are complementary for LC-MS/MS proteomic analysis of drug-metabolizing enzymes and transporters in pig liver. Howard M, Achour B, Al-Majdoub Z, Rostami-Hodjegan A, Barber J. PubMed
  • Eur J Pharm Sci. 2019:in press. Protein expression and function of organic anion transporters in short-term and long-term cultures of Huh7 human hepatoma cells. Malinen MM, Ito K, Kang HE, Honkakoski P, Brouwer KLR. PubMed

Transporter inhibition

  • Mol Pharm. Novel in vitro method reveals drugs that inhibit Solute Transporter Alpha/Beta (OSTα/β). Malinen MM, Kauttonen A, Beaudoin JJ, Sjöstedt N, Honkakoski P, Brouwer KLR. PubMed
  • Mol Pharm. 2019 ;in press. Effect of a common genetic variant (p.V444A) in the Bile Salt Export Pump on the inhibition of bile acid transport by cholestatic medications. Ali I, Khalid S, Stieger B, Brouwer KLR. PubMed
  • Phytomedicine. 2018; in press. Piperine enhances the bioavailability of silybin via inhibition of efflux transporters BCRP and MRP2. Bi X, Yuan Z, Qu B, Zhou H, Liu Z, Xie Y. PubMed
  • Clin Pharmacol Ther. 2019; in press. Clinical aspects of transporter-mediated Drug-Drug Interactions. Gessner A, König J, Fromm MF. PubMed

Drug hepatotoxicity

  • Drug Metab Dispos. 2019;47:155-163. Altered hepatobiliary disposition of Tolvaptan and selected Tolvaptan metabolites in a rodent model of Polycystic Kidney Disease. Beaudoin JJ, Bezençon J, Cao Y, Mizuno K, Roth SE, Brock WJ, Brouwer KLR. PubMed
  • J Appl Toxicol. 2018;In press. Prediction of clinically relevant drug-induced liver injury from structure using machine learning. Hammann F, Schöning V, Drewe J. PubMed
  • Toxicol Sci. 2018;In press. Quantitative systems toxicology analysis of in vitro mechanistic assays reveals the importance of bile acid accumulation and mitochondrial dysfunction in TAK-875-induced liver injury. Longo DM, Woodhead JL, Walker P, Herédi-Szabó K, Mogyorósi K, Wolenski FS, Dragan YP, Mosedale M, Siler SQ, Watkins PB, Howell BA. PubMed

Interaction efflux transporter function and glucuronidation

  • Mol Pharm. 2018 ;In press. Interplay of efflux transporters with glucuronidation and its impact on subcellular Aglycone and glucuronide disposition: A case study with Kaempferol. Li Y, Lu L, Wang L, Qu W, Liu W, Xie Y, Zheng H, Wang Y, Qi X, Hu M, Zhu L, Liu Z. PubMed

Pharmaceutical excipients and intestinal drug transporters

  • Clin Pharmacol Ther. 2019;105:323-325. Impact of pharmaceutical excipients on oral drug absorption: A focus on intestinal drug transporters. Zou L, Ni Z, Tsakalozou E, Giacomini KM. PubMed
  • Pharmacol Ther. 2018;in press. Organic anion transporting polypeptide 2B1 - More than a glass-full of drug interactions. McFeely SJ, Wu L, Ritchie TK, Unadkat J. PubMed