Liver imaging

  • Br J Clin Pharmacol. 2019;191:105350. Hepatic exposure of Metformin in patients with non-alcoholic fatty liver disease. Sundelin EIO, Gormsen LC, Heebøll S, Vendelbo MH, Jakobsen S, Munk OL, Feddersen S, Brøsen K, Hamilton-Dutoit SJ, Pedersen SB, Grønbaek H, Jessen N. PubMed
  • Clin Pharmacol Ther. 2019; In press. PET imaging of [11 C]Rosuvastatin hepatic concentrations and hepatobiliary transport in humans in the absence and presence of Cyclosporine A. Billington S, Shoner S, Lee S, Clark-Snustad K, Pennington M, Lewis D, Muzi M, Rene S, Lee J, Nguyen TB, Kumar V, Ishida K, Chen L, Chu X, Lai Y, Salphati L, Hop CECA, Xiao G, Liao M, Unadkat JD. PubMed
  • AAPS J. 2019;21:61. Towards improved pharmacokinetic models for the analysis of transporter-mediated hepatic disposition of drug molecules with Positron Emission Tomography. Hernández Lozano I, Karch R, Bauer M, Blaickner M, Matsuda A, Wulkersdorfer B, Hacker M, Zeitlinger M, Langer O. PubMed
  • Methods Mol Biol. 2019;1981:87-98. In vivo measurement of hepatic drug transporter inhibition with radiolabeled bile acids. De Lombaerde S, Neyt S, Vanhove C, De Vos F. PubMed

Drugs and hepatocyte transport

  • J Steroid Biochem Mol Biol. 2019;pii: S0960-0760(19)30112-8.  Major glucuronide metabolites of testosterone are primarily transported by MRP2 and MRP3 in human liver, intestine and kidney. Li CY, Basit A, Gupta A, Gáborik Z, Kis E, Prasad B. PubMed
  • Br J Pharmacol. 2019;In press. Roles of OAT2 and ENT1 in hepatic disposition and antiviral activity of Entecavir during non-pregnancy and pregnancy. Ma Z, Lu S, Sun D, Bai M, Jiang T, Lin N, Zhou H, Zeng S, Jiang H. PubMed
  • Drug Metab Dispos. 2019;In press. Fexofenadine and Rosuvastatin pharmacokinetics in mice with targeted disruption of Organic Anion Transporting Polypeptide 2B1. Medwid S, Li MMJ, Knauer MJ, Lin K, Mansell SE, Schmerk CL, Zhu C, Griffin KE, Yousif MD, Dresser GK, Schwarz UI, Kim RB, Tirona RG. PubMed

Transporter function

  • Xenobiotica. 2019,In press. Genetic polymorphisms of human hepatic OATPs: functional consequences and effect on drug pharmacokinetics. Nie Y, Yang J, Liu S, Sun R, Chen H, Long N, Jiang R, Gui C. PubMed
  • Mol Pharmacol. 2019;in press. OATP1B3-1B7 (LST-3TM12) is a drug transporter that affects endoplasmic reticulum access and the metabolism of ezetimibe. Malagnino V, Duthaler U, Seibert I, Krahenbuhl S, Meyer Zu Schwabedissen HE. PubMed
  • Mol Pharm. 2019;16:2342-2353.  Dissecting the contribution of OATP1B1 to hepatic uptake of statins using the OATP1B1 selective inhibitor Estropipate. Zhang Y, Panfen E, Fancher M, Sinz M, Marathe P, Shen H. PubMed

Quantification of transporters

  • Clin Pharmacol Ther. 2019;In press. Interindividual and regional variability in drug transporter abundance at the human Blood-Brain Barrier measured by Quantitative Targeted Proteomics. Billington S, Salphati L, Hop CECA, Chu X, Evers R, Burdette D, Rowbottom C, Lai Y, Xiao G, Humphreys WG, Nguyen TB, Prasad B, Unadkat JD. Brain microvascular endothelial cells (BMECs) isolated from postmortem specimens. PubMed
  • Drug Metab Pharmacokinet. 2019;In press. Comparison of mRNA expression profiles of drug-metabolizing enzymes and transporters in fresh and cryopreserved cynomolgus monkey hepatocytes. Koeda A, Iwao T, Nakanishi A, Mizuno S, Yamashita M, Sakai Y, Nakamura K, Matsunaga T. PubMed

Drugs and intestinal microbiome

  • Clin Pharmacol Ther. 2019; In press. Capturing the complex interplay between drugs and the intestinal microbiome. Birer C, Wright ES. PubMed

Drug-induced liver injury

  • J Hepatol. 2019 Jun;70:1222-1261. EASL clinical practice guidelines: drug-induced liver injury. European Association for the Study of the Liver. Andrade RJ, Aithal GP, Björnsson ES, Kaplowitz N, Kullak-Ublick GA, Larrey D, Karlsen TH. PubMed
  • Gastroenterology. 2019;156:1707-1716.e2. A missense variant in PTPN22 is a risk factor for drug-induced liver injury. Cirulli ET, Nicoletti P, Abramson K, Andrade RJ, Bjornsson ES, Chalasani N, Fontana RJ, Hallberg P, Li YJ, Lucena MI, Long N, Molokhia M, Nelson MR, Odin JA, Pirmohamed M, Rafnar T, Serrano J, Stefánsson K, Stolz A, Daly AK, Aithal GP, Watkins PB; Drug-Induced Liver Injury Network (DILIN) investigators; International DILI consortium (iDILIC). PubMed
  • Toxicol Sci. 2019;in press. Use of a Bile Salt Export Pump knockdown rat susceptibility model to interrogate mechanism of drug induced liver toxicity. Li Y, Evers R, Hafey MJ, Cheon K, Duong H, Lynch D, LaFranco-Scheuch L, Pacchione S, Tamburino A, Tanis K, Geddes K, Holder D, Rena Zhang N, Kang W, Gonzalez RJ, Galijatovic-Idrizbegovic A, Pearson K, Lebron J, Glaab WE, Sistare FD. PubMed
  • Mol Pharmacol. 2019 Jun ;In press. Severe hepatotoxicity of Mithramycin therapy caused by altering expression of hepatocellular bile transporters. Sissung TM, Huang PA, Hauke RJ, McCrea EM, Peer CJ, Barbier RH, Strope JD, Ley AM, Zhang M, Hong JA, Venzon D, Jackson JP, Brouwer KR, Grohar P, Glod J, Widemann BC, Heller T, Schrump DS, Figg WD. PubMed


  • Pharmacol Res. 2019;in press. Drugs and hepatic transporters: A review. Jetter A, Kullak-Ublick GA. PubMed
  • Methods Mol Biol. 2019;1981:55-73. Vesicle- and hepatocyte-based assays for identification of drug candidates inhibiting BSEP function. Van Brantegem P, Deferm N, Qi B, De Vocht T, Annaert P. PubMed
  • Methods Mol Biol. 2019;1981:273-289.  Zebrafish as a model to study cholestatic liver diseases. Pham DH, Yin C. PubMed
  • Clin Pharmacol Ther. 2019;In press. Towards a consensus on applying quantitative LC-MS/MS proteomics in translational pharmacology research: a white paper. Prasad B, Achour B, Artursson P, Hop CE, Lai Y, Smith PC, Barber J, Wisniewski JR, Spellman D, Uchida Y, Zientek M, Unadkat JD, Rostami-Hodjegan. Quantitative translation of information on drug absorption, disposition, receptor engagement and drug-drug interactions from bench to bedside requires models informed by physiological parameters that link in vitro studies to in vivo outcomes. To predict in vivo outcomes, biochemical data from experimental systems are routinely scaled using protein quantity in these systems and relevant tissues. Although several laboratories have generated useful quantitative proteomic data using state-of-the-art mass spectrometry, no harmonized guidelines exit for sample analysis and data integration to in vivo translation practices. To address this gap, a workshop was held on September 27th and 28th 2018, in Cambridge, MA, with 100 experts attending from academia, the pharmaceutical industry and regulators. Various aspects of quantitative proteomics and its applications in translational pharmacology were debated. PubMed

Inhibitor preincubation and transporter function

  • Drug Metab Dispos. 2019,In press. A systematic in vitro investigation of the inhibitor preincubation effect on multiple classes of clinically relevant transporters. Tatrai P, Schweigler P, Poller B, Domange N, de Wilde R, Hanna I, Gaborik Z, Huth F. PubMed
  • J Pharm Sci. 2019:In press. Preincubation with Everolimus and Sirolimus reduces Organic Anion-Transporting Polypeptide (OATP)1B1- and 1B3-mediated transport independently of mTOR kinase inhibition: implication in assessing OATP1B1- and OATP1B3-mediated drug-drug interactions. Farasyn T, Crowe A, Hatley O, Neuhoff S, Alam K, Kanyo J, Lam TT, Ding K, Yue W. PubMed

Liver Microphysiological Systems

  • Clin Pharmacol Ther. 2019;In press. Liver Microphysiological Systems for predicting and evaluating drug effects. Ribeiro AJS, Yang X, Patel V, Madabushi R, Strauss DG. PubMed

Transporter regulation

  • Hepatology. 2019;In press. Blocking sodium-taurocholate cotransporting polypeptide stimulates biliary cholesterol and phospholipid secretion. Roscam Abbing RLP, Slijepcevic D, Donkers JM, Havinga R, Duijst S, Paulusma CC, Kuiper J, Kuipers F, Groen AK, Oude Elferink RPJ, van de Graaf SFJ. PubMed
  • Hepatology. 2019;In press. Rat OATP1A1 interacts directly with OATP1A4 facilitating its maturation and trafficking to the hepatocyte plasma membrane. Wang P, Wang WJ, Choi-Nurvitadhi J, Lescaille Y, Murray JW, Wolkoff AW. PubMed
  • Biochem Pharmacol. 2019;164:311-320. Role of ERK1/2 in TNFα-induced internalization of Abcc2 in rat hepatocyte couplets. Ciriaci N, Andermatten RB, Razori MV, Schuck VS, Miszczuk GS, Medeot AC, Crocenzi FA, Roma MG, Barosso IR, Ruiz ML, Sánchez Pozzi EJ. PubMed