Hepatocyte concentrations of imaging substrates

  • Eur Radiol Exp. 2021;5:42. Concentrations and pharmacokinetic parameters of MRI and SPECT hepatobiliary agents in rat liver compartments. Pastor CM, Joly F, Vilgrain V, Millet P. PubMed. Imaging point-of-view: compartmental distribution of liver concentrations, comparisons between hepatocyte and liver concentrations, new understanding of hepatobiliary imaging
  • Drug Metab Dispos. 2021;In press. New pharmacokinetic parameters of imaging substrates quantified from rat liver compartments. Pastor CM, Brouwer KL. PubMed. Pharmacokinetic point-of-view: compartmental distribution of liver concentrations, concentration ratios between all hepatic compartments, clearances in normal rat livers.
  • Cells. 2021;10:2733. Steatosis alters the activity of hepatocyte membrane transporters in obese rats. Pastor CM, Vilgrain V. PubMed. Pharmacokinetic point-of-view: compartmental distribution of liver concentrations, concentration ratios between all hepatic compartments, clearances in rat livers with steatosis

Transporter expression and function

  • Drug Metab Pharmacokinet. 2021;40:100411. Downregulated expression of organic anion transporting polypeptide (Oatp) 2b1 in the small intestine of rats with acute kidney injury Takeda F, Oda M, Terasaki M, Kubota A, Asada K, Ichimura Y, Kojima H, Saitoh H. PubMed
  • Clin Pharmacol Ther. 2021;In press. Performance of plasma Coproporphyrin I and III as OATP1B1 biomarkers in humans. Neuvonen M, Tornio A, Hirvensalo P, Backman JT, Niemi M. PubMed
  • Clin Transl Sci. 2021;In press. Pharmacogenomics of celiprolol - evidence for a role of P-glycoprotein and organic anion transporting polypeptide 1A2 in celiprolol pharmacokinetics.  Hirvensalo P, Tornio A, Tapaninen T, Paile-Hyvärinen M, Neuvonen M, Backman JT, Niemi M. PubMed
  • Life Sci. 2021:In press. Induction of P-glycoprotein expression and activity by prolactin in female rat liver. Ceré LI, Sedlmeier MG, Semeniuk M, Luquita MG, Francés D, Ronco MT, Rigalli JP, Ruiz ML, Catania VA. PubMed

Experimental models

  • J Pharm Pharm Sci. 2021;24:475-483. Development of a rat Sandwich-Cultured Hepatocytes model expressing functional human Organic Anion Transporting Polypeptide (OATP) 1B3: A potential screening tool for liver-targeting compounds. Farasyn T, Xu C, Yue W. PubMed
  • Drug Metab Dispos. 2021;49:780-789. Evaluation of normothermic machine perfusion of porcine livers as a novel preclinical model to predict biliary clearance and transporter-mediated drug-drug interactions using statins. Stevens LJ, Zhu AZX, Chothe PP, Chowdhury SK, Donkers JM, Vaes WHJ, Knibbe CAJ, Alwayn IPJ, van de Steeg E. PubMed

Preclinical models of DILI

  • J Hepatol. 2021;75:935-959. Advanced preclinical models for evaluation of drug-induced liver injury - consensus statement by the European Drug-Induced Liver Injury Network [PRO-EURO-DILI-NET]. Fernandez-Checa JC, Bagnaninchi P, Ye H, Sancho-Bru P, Falcon-Perez JM, Royo F, Garcia-Ruiz C, Konu O, Miranda J, Lunov O, Dejneka A, Elfick A, McDonald A, Sullivan GJ, Aithal GP, Lucena MI, Andrade RJ, Fromenty B, Kranendonk M, Cubero FJ, Nelson LJ. PubMed

Quantitative proteomics

  • Mol Pharm. 2021;18:3563-3577. Non-uniformity of changes in drug-metabolizing enzymes and transporters in liver cirrhosis: Implications for drug dosage adjustment. El-Khateeb E, Achour B, Al-Majdoub ZM, Barber J, Rostami-Hodjegan A. PubMed
  • Clin Pharmacol Ther. 2021; In press. Quantitative proteomic map of enzymes and transporters in the human kidney: Stepping closer to mechanistic kidney models to define local kinetics. Al-Majdoub ZM, Scotcher D, Achour B, Barber J, Galetin A, Rostami-Hodjegan A. PubMed

Uptake of highly permeable LMW acid drugs

  • Drug Metab Dispos. 2021;49:648-657. Passive influx and ion trapping are more relevant to the cellular accumulation of highly permeable low-molecular-weight acidic drugs than is Organic Anion Transporter 2. Dallas Bednarczyk. PubMed

 Anti-COVID drugs and transporters

  • Sci Rep. 2021;11:17810. Interactions of anti-COVID-19 drug candidates with hepatic transporters may cause liver toxicity and affect pharmacokinetics. Ambrus C, Bakos É, Sarkadi B, Özvegy-Laczka C, Telbisz Á. PubMed
  • Pharmaceutics. 2021;13:81. Interactions of potential anti-COVID-19 compounds with multispecific ABC and OATP drug transporters. Telbisz Á, Ambrus C, Mózner O, Szabó E, Várady G, Bakos É, Sarkadi B, Özvegy-Laczka C. PubMed

Drug-drug interactions

  • CPT Pharmacometrics Syst Pharmacol. 2021;10:1018-1031. Quantitative prediction of breast cancer resistant protein mediated drug-drug interactions using physiologically-based pharmacokinetic modeling. Costales C, Lin J, Kimoto E, Yamazaki S, Gosset JR, Rodrigues AD, Lazzaro S, West MA, West M, Varma MVS. PubMed
  • Front Pharmacol. 2021;12:715577. Evaluation of a clinically relevant Drug-Drug Interaction between Rosuvastatin and Clopidogrel and the risk of hepatotoxicity. Ning C, Su S, Li J, Kong D, Cai H, Qin Z, Xing H, Chen X, He J. PubMed
  • Clin Pharmacol Ther. 2021;In press. Biomarker-informed model-based risk assessment of Organic Anion Transporting Polypeptide 1B Mediated Drug-Drug Interactions. Kimoto E, Costales C, West MA, Bi YA, Vourvahis M, David Rodrigues A, Varma MVS. PubMed

Physiology of bile

  • Hepatology. 2021;In press. On the mechanisms of biliary flux. Vartak N, Drasdo D, Geisler F, Itoh T, Oude Elferink RPJ, van de Graaf SFJ, Chiang J, Keitel V, Trauner M, Jansen P, Hengstler JG. PubMed

Transporters and disease

  • Clin Pharmacol Ther. 2021;In press. Clinical and molecular perspectives on inflammation-mediated regulation of drug metabolism and transport.  Dunvald AD, Järvinen E, Mortensen C, Stage TB. PubMed
  • Sci Rep. 2021;11:19125. Curcumin inhibited hepatitis B viral entry through NTCP binding.  Thongsri P, Pewkliang Y, Borwornpinyo S, Wongkajornsilp A, Hongeng S, Sa-Ngiamsuntorn K. PubMed
  • Drug Metab Dispos. 2021;In press. Exogenous drug disposition as a diagnostic biomarker strategy for Non-Alcoholic Steatohepatitis.  Marie S, Tripp DKK, Cherrington NJ. PubMed