Transporters and imaging

  • J Hepatol. 2020;In press. Obeticholic acid improves hepatic bile acid excretion in patients with primary biliary cholangitis. Kjærgaard K, Frisch K, Sørensen M, Munk OL, Hofmann AF, Horsager J, Schacht AC, Erickson M, Shapiro D, Keiding S. PubMed
  • J Hepatol. 2020;In press. Advances in functional and molecular MRI technologies in chronic liver diseases. Zhou IY, Catalano OA, Caravan P. PubMed
  • J Nucl Med. 2020;61:1050-1057. Imaging P-Glycoprotein induction at the Blood-Brain Barrier of a β-Amyloidosis mouse model with 11C-Metoclopramide PET. Zoufal V, Mairinger S, Brackhan M, Krohn M, Filip T, Sauberer M, Stanek J, Wanek T, Tournier N, Bauer M, Pahnke J, Langer O. PubMed

Transporters and DDI

  • Drug Metab Pharmacokinet. Increased plasma concentrations of an antidyslipidemic drug pemafibrate co-administered with rifampicin or cyclosporine A in cynomolgus monkeys genotyped for the organic anion transporting polypeptide 1B1. Ogawa SI, Shimizu M, Kamiya Y, Uehara S, Suemizu H, Yamazaki H.  2020;35:354-360. PubMed
  • Clin Pharmacol Ther. 2020;In press. A microdose cocktail to evaluate drug interactions in patients with renal impairment. Tatosian DA, Yee KL, Zhang Z, Mostoller K, Paul E, Sutradhar S, Larson P, Chhibber A, Wen J, Wang YJ, Lassman M, Latham AH, Pang J, Crumley T, Gillespie A, Marricco NC, Marenco T, Murphy M, Lasseter KC, Marbury TC, Tweedie D, Chu X, Evers R, Stoch SA. PubMed
  • Drug Metab Dispos. 2020:In press. Detection of weak Organic Anion-Transporting Polypeptide (OATP) 1B inhibition by Probenecid (PROB) with plasma-based Coproporphyrin in humans. Zhang Y, Holenarsipur VK, Kandoussi H, Zeng J, Mariappan TT, Sinz M, Shen H. PubMed
  • Drug Metab Dispos. 2020;48:750-758. Static model-based Assessment of OATP1B1-mediated drug interactions with preincubation-dependent inhibitors based on inactivation and recovery kinetics. Taguchi T, Masuo Y, Futatsugi A, Kato Y. PubMed
  • Clin Pharmacol Ther. 2020;In press. Identification of appropriate endogenous biomarker for risk assessment of multidrug and toxin extrusion protein-mediated drug-drug interactions in healthy volunteers. Miyake T, Kimoto E, Luo L, Mathialagan S, Horlbogen LM, Ramanathan R, Wood LS, Johnson JG, Le VH, Vourvahis M, Rodrigues AD, Muto C, Furihata K, Sugiyama Y, Kusuhara H. PubMed

Drug hepatocyte clearance

  • Drug Metab Pharmacokinet. 2020;35: 389-396. Predicted values for human total clearance of a variety of typical compounds with differently humanized-liver mouse plasma data. Nakayama K, Kamimura H, Suemizu H, Yoneda N, Nishiwaki M, Iwamoto K, Mizunaga M, Negoro T, Ito S, Yamazaki H, Nomura Y. PubMed
  • Drug Metab Dispos. 2020.In press. Comparison of in vitro to in vivo extrapolation approaches for predicting transporter-mediated hepatic uptake clearance using suspended rat hepatocytes. Li N, Badrinarayanan A, Li X, Roberts J, Hayashi M, Virk M, Gupta A. PubMed
  • Drug Metab Dispos. 2020:In press. Application of the Extended Clearance Classification System (ECCS) in drug discovery and development: Selection of appropriate in vitro tools and clearance prediction. Umehara K, Cantrill C, Wittwer MB, Di Lenarda E, Klammers F, Ekiciler A, Parrott N, Fowler S, Ullah M. PubMed
  • Life Sci. 2020;257:118079. The inhibition of hepatic Pxr-Oatp2 pathway mediating decreased hepatic uptake of rosuvastatin in rats with high-fat diet-induced obesity. Zhang F, Duan Y, Wei Y, Zhang J, Ma X, Tian H, Wang X, Saad AAA, Li B, Wu X. PubMed

Transporter deficiency

  • J Pharmacol Exp Ther. 2020;374:38-43. ABCG2 deficiency does not alter Dolutegravir metabolism and pharmacokinetics. Zhu J, Tian X, Shehu AI, McMahon DK, Ma X. PubMed
  • Pharmacol Res. 2020 Aug 17:105155. Schwabedissen HEMZ, Seibert I, Grube M, Alter CL, Siegmund W, Hussner J. Genetic variants of SLCO1B7 are of relevance for the transport function of OATP1B3-1B7. PubMed

Transporter regulation

  • Drug Metab Dispos. 2020;48:708-722. Impact of microbiome on hepatic metabolizing enzymes and transporters in mice during pregnancy. Han LW, Wang L, Shi Y, Dempsey JL, Pershutkina OV, Dutta M, Bammler TK, Cui JY, Mao Q. PubMed
  • Cell Chem Biol. 2020;27:728-739. Targeted degradation of SLC transporters reveals amenability of multi-pass transmembrane proteins to ligand-induced proteolysis. Bensimon A, Pizzagalli MD, Kartnig F, Dvorak V, Essletzbichler P, Winter GE, Superti-Furga G. PubMed
  • Sci Rep. 2020;10:13110. Reduced Mrp2 surface availability as PI3Kγ-mediated hepatocytic dysfunction reflecting a hallmark of cholestasis in sepsis. Beer AJ, Hertz D, Seemann E, Beretta M, Westermann M, Bauer R, Bauer M, Kessels MM, Qualmann B. PubMed
  • Mol Pharm. 2020;17:2821-2830. Regulation of Organic Anion Transporting Polypeptide 2B1 expression by MicroRNA in the human liver. Tajiri A, Hirota T, Kawano S, Yonamine A, Ieiri I. PubMed

RESOLUTE Consortium

  • Nat Rev Drug Discov. 2020;19:429-430. The RESOLUTE consortium: unlocking SLC transporters for drug discovery. Superti-Furga G, Lackner D, Wiedmer T, Ingles-Prieto A, Barbosa B, Girardi E, Goldmann U, Gürtl B, Klavins K, Klimek C, Lindinger S, Liñeiro-Retes E, Müller AC, Onstein S, Redinger G, Reil D, Sedlyarov V, Wolf G, Crawford M, Everley R, Hepworth D, Liu S, Noell S, Piotrowski M, Stanton R, Zhang H, Corallino S, Faedo A, Insidioso M, Maresca G, Redaelli L, Sassone F, Scarabottolo L, Stucchi M, Tarroni P, Tremolada S, Batoulis H, Becker A, Bender E, Chang YN, Ehrmann A, Müller-Fahrnow A, Pütter V, Zindel D, Hamilton B, Lenter M, Santacruz D, Viollet C, Whitehurst C, Johnsson K, Leippe P, Baumgarten B, Chang L, Ibig Y, Pfeifer M, Reinhardt J, Schönbett J, Selzer P, Seuwen K, Bettembourg C, Biton B, Czech J, de Foucauld H, Didier M, Licher T, Mikol V, Pommereau A, Puech F, Yaligara V, Edwards A, Bongers BJ, Heitman LH, IJzerman AP, Sijben HJ, van Westen GJP, Grixti J, Kell DB, Mughal F, Swainston N, Wright-Muelas M, Bohstedt T, Burgess-Brown N, Carpenter L, Dürr K, Hansen J, Scacioc A, Banci G, Colas C, Digles D, Ecker G, Füzi B, Gamsjäger V, Grandits M, Martini R, Troger F, Altermatt P, Doucerain C, Dürrenberger F, Manolova V, Steck AL, Sundström H, Wilhelm M, Steppan CM. PubMed

Human Sandwich-Cultured Hepatocytes

  • AAPS J. 2020;22:110. Pitfalls in predicting hepatobiliary drug transport using human Sandwich-Cultured Hepatocytes. Kumar V, Li CY, Ishida K, Kis E, Gáborik Z, Unadkat JD. PubMed

Transporter function

  • Xenobiotica. 2020:In press. MRP4 is responsible for the efflux transport of mycophenolic acid β-D glucuronide (MPAG) from hepatocytes to blood. Berthier J, Benmameri M, Sauvage FL, Fabre G, Chantemargue B, Arnion H, Marquet P, Trouillas P, Picard N, Saint-Marcoux F. PubMed
  • Drug Metab Pharmacokinet. 2020:In press. Mathematical modeling analysis of hepatic uric acid disposition using human sandwich-cultured hepatocytes. Wada S, Matsunaga N, Tamai I. PubMed

Drug-induced hyperbilirubinemia

  • Pharmaceutics. 2020;12:E755. Prediction of drug-induced hyperbilirubinemia by in vitro testing. Tátrai P, Krajcsi P. PubMed

NTCP and virus

  • Viruses. 2020;12:E828. Innovative HBV animal models based on the entry receptor NTCP. Wettengel JM, Burwitz BJ. PubMed
  • Cells. 2020;9:1486. Hepatitis B virus entry into cells. Herrscher C, Roingeard P, Blanchard E. PubMed

Hepatotoxicity and biliary efflux

  • Clin Pharmacol Ther. 2020:In press. Quantitative systems toxicology modeling predicts that reduced biliary efflux contributes to Tolvaptan hepatotoxicity. Beaudoin JJ, Brock WJ, Watkins PB, Brouwer KLR. PubMed
  • Toxicol Appl Pharmacol. 2020;403:115170. Effects of ablation and activation of Nrf2 on bile acid homeostasis in male mice. Zhang Y, Lickteig AJ, Liu J, Csanaky IL, Klaassen CD. PubMed