2019 August: RECENT PUBLICATIONS

Liver imaging

  • Appl Radiat Isot. 2019;152:172-179. Radiolabeling of protected tryptophan with [18F]fluoromethyl tosylate: Formation of [18F]fluoromethyl ester of tryptophan instead of 1-N-[18F]fluoromethyl tryptophan methylester. Venkatachalam TK, Stimson DHR, Frisch K, Pierens GK, Bhalla R, Reutens DC. PubMed
  • Nucl Med Biol. 2019;72-73:55-61. Human biodistribution, dosimetry, radiosynthesis and quality control of the bile acid PET tracer [N-methyl-11C]cholylsarcosine. Frisch K, Kjærgaard K, Horsager J, Schacht AC, Munk OL. PubMed
  • J Cereb Blood Flow Metab. 2019;in press. Measurement of cerebral ABCC1 transport activity in wild-type and APP/PS1-21 mice with positron emission tomography. Zoufal V, Mairinger S, Krohn M, Wanek T, Filip T, Sauberer M, Stanek J, Kuntner C, Pahnke J, Langer O. PubMed

Biology of hepatocytes

  • J Cell Biol. 2019;218:2096-2112. The cell biology of the hepatocyte: A membrane trafficking machine. Schulze RJ, Schott MB, Casey CA, Tuma PL, McNiven MA. In this Beyond the Cell review, the authors detail central features of hepatocytes and highlight how membrane transport processes play a key role in healthy liver function and how they are affected by disease. PubMed
  • Clin Pharmacol Ther. 2019;106:568-575. Induction of mild hyperbilirubinemia: Hype or real therapeutic opportunity? Vitek L, Bellarosa C, Tiribelli C. PubMed
  • Arch Toxicol. 2019;93:819-829. A simple approach for restoration of differentiation and function in cryopreserved human hepatocytes. Ölander M, Wiśniewski JR, Flörkemeier I, Handin N, Urdzik J, Artursson P. PubMed

Transporters and liver disease

  • Clin Pharmacol Ther. 2019; in press. Sorafenib activity and disposition in liver cancer does not depend on organic cation transporter 1 (OCT1). Chen M, Neul C, Schaeffeler E, Frisch F, Winter S, Schwab M, Koepsell H, Hu S, Laufer S, Baker SD, Sparreboom A, Nies AT. PubMed
  • Drug Metab Dispos. 2019;47:899-906. Altered expression and function of hepatic transporters in a rodent model of Polycystic Kidney Disease. Bezençon J, Beaudoin JJ, Ito K, Fu D, Roth SE, Brock WJ, Brouwer KLR. PubMed

Quantification of transporters

  • Clin Pharmacol Ther. 2019;106:525-543. Toward a consensus on applying Quantitative Liquid Chromatography-Tandem Mass Spectrometry Proteomics in translational pharmacology research: A white paper. Prasad B, Achour B, Artursson P, Hop CECA, Lai Y, Smith PC, Barber J, Wisniewski JR, Spellman , Uchida Y9, Zientek MA, Unadkat JD, Rostami-Hodjegan A. PubMed
  • Drug Metab Dispos. 2019;47:802-808. Kidney cortical transporter expression across species using quantitative proteomics. Basit A, Radi Z, Vaidya VS, Karasu M, Prasad B. PubMed
  • Sci Rep. 2019;9:9709. A repository of protein abundance data of drug metabolizing enzymes and transporters for applications in physiologically based pharmacokinetic (PBPK) modelling and simulation. Ladumor MK, Thakur A, Sharma S, Rachapally A, Mishra S, Bobe P, Rao VK, Pammi P, Kangne H, Levi D, Balhara A, Ghandikota S, Joshi A, Nautiyal V, Prasad B, Singh S. PubMed
  • J Pharmacol Toxicol Methods. 2019;98:106590. Targeted quantitative proteomic analysis of drug metabolizing enzymes and transporters by nano LC-MS/MS in the sandwich cultured human hepatocyte model. Khatri R, Fallon JK, Rementer RJB, Kulick NT, Lee CR, Smith PC. PubMed
  • Drug Metab Dispos. 2019;47:854-864. The regional-specific relative and absolute expression of gut transporters in adult Caucasians: A meta-analysis. Harwood MD, Zhang M, Pathak SM, Neuhoff S. PubMed
  • Drug Metab Dispos. 2019;47:802-808. Kidney cortical transporter expression across species using quantitative proteomics. Basit A, Radi Z, Vaidya VS, Karasu M, Prasad B. 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
  • Clin Pharmacol Ther. 2019;in press. A comprehensive analysis of ontogeny of renal drug transporters: mRNA analyses, quantitative proteomics, and localization. Cheung KWK, van Groen BD, Spaans E, van Borselen MD, de Bruijn ACJM, Simons-Oosterhuis Y, Tibboel D, Samsom JN, Verdijk RM, Smeets B, Zhang L, Huang SM, Giacomini KM, de Wildt SN. PubMed

Intracellular concentrations

  • Drug Metab Dispos. 2019;47:779-784. Regulatory recommendations for calculating the unbound maximum hepatic inlet concentration: A complicated story with a surprising and happy ending. Parkinson A. PubMed
  • Drug Metab Dispos. 2019;47:665-672. Intracellular and intraorgan concentrations of small molecule drugs: Theory, uncertainties in infectious diseases and oncology, and promise. Smith DA, Rowland M. PubMed
  • Drug Metab Dispos. 2019;In press. Drug concentration asymmetry in tissues and plasma for small molecule-related therapeutic modalities. Zhang D, Hop CE, Patilea-Vrana G, Gampa G, Seneviratne HK, Unadkat JD, Kenny JR, Nagapudi K, Di L, Zhou L, Zak M, Wright MR, Bumpus NN, Zang R, Liu X, Lai Y, Khojasteh SC. PubMed
  • AAPS J. 2019;21:77. Impact of intracellular concentrations on metabolic drug-drug interaction studies. Treyer A, Ullah M, Parrott N, Molitor B, Fowler S, Artursson P. PubMed

Transporter function

  • Drug Metab Dispos. 2019;47:715-723. Coexpression of ABCB1 and ABCG2 in a cell line model reveals both independent and additive transporter function. Robinson AN, Tebase BG, Francone SC, Huff LM, Kozlowski H, Cossari D, Lee JM, Esposito D, Robey RW, Gottesman MM. PubMed
  • Mol Pharmacol. 2019;96:138-147. Generation and characterization of an Abcc1 humanized mouse model (hABCC1flx/flx) with Knockout capability. Krohn M, Zoufal V, Mairinger S, Wanek T, Paarmann K, Brüning T, Eiriz I, Brackhan M, Langer O, Pahnke J. PubMed
  • Am J Physiol Gastrointest Liver Physiol. 2019;in press. Deletion of organic cation transporter Oct3 promotes hepatic fibrosis via upregulation of TGFbeta. Vollmar J, Kim YO, Marquardt JU, Becker D, Galle PR, Schuppan D, Zimmermann T. PubMed
  • Basic Clin Pharmacol Toxicol. 2019,in press. Efflux transport of Nicotine, Cotinine and Trans-3'-hydroxycotinine glucuronides by human hepatic transporters. Järvinen E, Sjöstedt N, Koenderink JB, Kidron H, Finel M. PubMed
  • Br J Pharmacol. 2019 Jun;in press.  Roles of organic anion transporter 2 and equilibrative nucleoside transporter 1 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;47:832-842. 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

Progress and future

  • Clin Pharmacol Ther. 2019;105:1407-1420. From endogenous compounds as biomarkers to plasma-derived nanovesicles as liquid biopsy; Has the golden age of translational pharmacokinetics-absorption, distribution, metabolism, excretion, drug-drug interaction science finally arrived? Rodrigues D, Rowland A. PubMed
  • Clin Pharmacol Ther. 2019;105:1289-1291. Drug-drug interactions: Progress over the past decade and looking ahead to the future. Derendorf H, von Richter O, Hermann R, Rostami-Hodjegan A. In 2009, the current authors founded a focused meeting dedicated to regulatory requirements and scientific aspects of preclinical and clinical investigations of drug-drug Interactions (DDIs), held at Marbach Castle, Germany. The meeting, initially, was intended to be a one-off event. However, it has been repeated annually and will celebrate its 10th anniversary in 2019. One may ask “what are these rapidly changing elements that necessitate an annual review of the moving pieces?” PubMed

Drug-drug interactions

  • Clin Pharmacol Ther. 2019;105:1386-1394. Clinical aspects of transporter-mediated drug-drug interactions. Gessner A, König J, Fromm MF. PubMed
  • Clin Pharmacol Ther. 2019; In press. A clinical drug-drug interaction study assessing a novel drug transporter phenotyping cocktail with Adefovir, Sitagliptin, Metformin, Pitavastatin, and Digoxin. Trueck C, Hsin CH, Scherf-Clavel O, Schaeffeler E, Lenssen R, Gazzaz M, Gersie M, Taubert M, Quasdorff M, Schwab M, Kinzig M, Sörgel F, Stoffel MS, Fuhr U. PubMed
  • Clin Pharmacol Drug Dev. 2019;In press. Drug-drug interactions of Tacrolimus or Cyclosporine with Glecaprevir and Pibrentasvir in healthy subjects. Kosloski MP, Zhao W, Li H, Pugatch D, Asatryan A, Kort J, Mensa FJ, Liu W. PubMed
  • Sci Rep. 2019;9:5850. Improved predictions of time-dependent drug-drug interactions by determination of cytosolic drug concentrations. Filppula AM, Parvizi R, Mateus A, Baranczewski P, Artursson P. PubMed
  • J Pharmacol Exp Ther. 2019;in press. Translation of in vitro transport inhibition studies to clinical drug-drug interactions for Glecaprevir and Pibrentasvir. Kosloski MP, Bow DAJ, Kikuchi R, Wang H, Kim EJ, Marsh K, Mensa F, Kort J, Liu W. PubMed

Drug-induced liver injury

  • International Journal of Pharmacy and Chemistry. 2019; 5: 15-19. Drug-induced liver injury predictions: Extended clearance model and its use for prospective transporter and enzyme-based hepatic cell stress grading. Camenisch G. PubMed
  • Mol Pharmacol. 2019;96:158-167. Severe hepatotoxicity of Mithramycin therapy caused by altered 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
  • Toxicol Sci. 2019;170:180-198. 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 AM, Tanis KQ, Geddes K, Holder D, Zhang NR, Kang W, Gonzalez RJ, Galijatovic-Idrizbegovic A, Pearson KM, Lebron JA, Glaab WE, Sistare FD. PubMed

Transporter inhibition and endogenous substrates

  • Drug Metab Pharmacokinet. 2019;in press. Estimation of changes in serum creatinine and creatinine clearance caused by renal transporter inhibition in healthy subjects. Nakada T, Kudo T, Kume T, Kusuhara H, Ito K. PubMed
  • Drug Metab Dispos. 2019;in press. GDC-0810 pharmacokinetics and transporter-mediated drug interaction evaluation with an endogenous biomarker in the first-in-human, dose escalation study. Cheung KWK, Yoshida K, Cheeti S, Chen B, Morley R, Chan IT, Sahasranaman S, Liu L. PubMed
  • Clin Pharmacol Ther. 2019;in press. Complex drug-drug interaction (DDI) by fenebrutinib and the use of transporter endogenous biomarker to elucidate the mechanism of DDI. Jones N, Yoshida K, Salphati L, Kenny JR, Durk M, Chinn L. PubMed

Genetic polymorphism

  • Xenobiotica. 2019 Jun 24:1-21. 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