Transporters and imaging

  • Nucl Med Biol. 2020;90-91:49-54. [131I]MIBG exports via MRP transporters and inhibition of the MRP transporters improves accumulation of [131I]MIBG in neuroblastoma. Kobayashi M, Mizutani A, Nishi K, Muranaka Y, Nishii R, Shikano N, Nakanishi T, Tamai I, Kleinerman ES, Kawai K. PubMed
  • Clin Pharmacol Ther. 2020;In press. Impaired clearance from the brain increases the brain exposure to metoclopramide in elderly subjects. Bauer M, Bamminger K, Pichler V, Weber M, Binder S, Maier-Salamon A, Tahir A, Jäger W, Haslacher H, Tournier N, Hacker M, Zeitlinger M, Langer O. PubMed
  • Drug Metab Dispos. 2020;In press. Successful prediction of PET-imaged metformin hepatic uptake clearance in humans using the quantitative proteomics-informed relative expression factor approach. Sachar M, Kumar V, Gormsen LC, Munk OL, Unadkat JD. PubMed
  • Clin Pharmacol Ther. 2020;In press. Abundance of P-Glycoprotein and other drug transporters at the human Blood-Brain Barrier in Alzheimer's disease: A quantitative targeted proteomic study. Storelli F, Billington S, Kumar AR, Unadkat JD. PubMed

PK modeling

  • Drug Metab Pharmacokinet. 2020;35:432-440. Mathematical modeling analysis of hepatic uric acid disposition using human sandwich-cultured hepatocytes. Wada S, Matsunaga N, Tamai I. In press. PubMed
  • Clin Pharmacol Ther. 2020;In press. Physiologically-Based Pharmacokinetic (PBPK) model of Morphine and Morphine-3-Glucuronide in Nonalcoholic Steatohepatitis (NASH). Sjöstedt N, Neuhoff S, Brouwer KLR. PubMed
  • Clin Pharmacol Ther. 2020;In press. Proteomics-informed prediction of rosuvastatin plasma profiles in patients with a wide range of body weight. Wegler C, Prieto Garcia L, Klinting S, Robertsen I, Wiśniewski JR, Hjelmesaeth J, Åsberg A, Jansson-Löfmark R, Andersson TB, Artursson P. PubMed
  • AAPS J. 2020;In press. Construction and verification of Physiologically Based Pharmacokinetic models for four drugs majorly cleared by Glucuronidation: Lorazepam, Oxazepam, Naloxone, and Zidovudine. Docci L, Umehara K, Krähenbühl S, Fowler S, Parrott N. PubMed

Induction of OATP1B expression

  • J Pharmacol Exp Ther. 2020;375:139-151. Absence of OATP1B (Organic Anion-Transporting Polypeptide) induction by rifampin in Cynomolgus monkeys: Determination using the endogenous OATP1B marker Coproporphyrin and tissue gene expression. Zhang Y, Chen C, Chen SJ, Chen XQ, Shuster DJ, Puszczalo PD, Fancher RM, Yang Z, Sinz M, Shen H. PubMed

Hepatic clearance

  • Drug Metab Dispos. 2020;48:849-860. 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, DiaLenarda E, Klammers F, Ekiciler A, Parrott N, Fowler S, Ullah M. PubMed
  • Drug Metab Dispos. 2020;In press. In vitro hepatic uptake in human and monkey hepatocytes in the presence and absence of serum protein and its in vitro to in vivo extrapolation. Liang X, Park Y, DeForest N, Hao J, Zhao X, Niu C, Wang K, Smith BJ, Lai Y. PubMed
  • J Med Chem. 2020;In press. Predicting the human hepatic clearance of acidic and zwitterionic drugs. Tess DA, Eng H, Kalgutkar AS, Litchfield J, Edmonds DJ, Griffith DA, Varma MVS. PubMed
  • Eur J Pharm Sci. 2020;In press. Mechanistic insights on clearance and inhibition discordance between liver microsomes and hepatocytes when clearance in liver microsomes is higher than in hepatocytes. Keefer C, Chang G, Carlo A, Novak JJ, Banker M, Carey J, Cianfrogna J, Eng H, Jagla C, Johnson N, Jones R, Jordan S, Lazzaro S, Liu J, Scott Obach R, Riccardi K, Tess D, Umland J, Racich J, Varma M, Visswanathan R, Di L. PubMed

Unbound fraction of drugs

  • Drug Metab Dispos. 2020;48:894-902. Seeking nonspecific binding: Assessing the reliability of tissue dilutions for calculating fraction unbound. Jusko WJ, Molins EAG, Ayyar VS. PubMed
  • J Pharmacol Exp Ther. 2020;In press. Physiologically-Based Pharmacokinetic modeling involving nonlinear plasma and tissue binding: Application to Prednisolone and Prednisone in rats. Li X, DuBois DC, Almon RR, Jusko WJ. PubMed

DMD special section on natural products

  • Drug Metab Dispos. 2020;48:966-971. Multidrug Resistance-Associated Protein 3 is responsible for the efflux transport of Curcumin Glucuronide from hepatocytes to the blood. Jia YM, Zhu T, Zhou H, Ji JZ, Tai T, Xie HG. PubMed
  • Drug Metab Dispos. 2020 Oct;48(10):972-979. The effects of traditional Chinese Medicine on P-Glycoprotein-Mediated Multidrug Resistance and approaches for studying the herb-P-Glycoprotein interactions. Cao Y, Shi Y, Cai Y, Hong Z, Chai Y. PubMed
  • Drug Metab Dispos. 2020;48:1064-1073. Effects of Chrysin and its major conjugated metabolites Chrysin-7-Sulfate and Chrysin-7-Glucuronide on Cytochrome P450 enzymes and on OATP, P-gp, BCRP, and MRP2 transporters. Mohos V, Fliszár-Nyúl E, Ungvári O, Bakos É, Kuffa K, Bencsik T, Zsidó BZ, Hetényi C, Telbisz Á, Özvegy-Laczka C, Poór M. PubMed

Hepatic bile excretion

  • Am J Physiol Gastrointest Liver Physiol. 2020;In press. Javitt NB. Hepatic bile formation: Bile acid transport and water flow in the canalicular conduit. PubMed
  • Drug Metab Dispos. 2020;In press. A two-tiered in vitro approach to de-risk drug candidates for potential bile salt export pump inhibition liabilities in drug discovery. Hafey MJ, Houle R, Tanis KQ, Knemeyer I, Shang J, Chen Q, Baudy A, Monroe J, Sistare FD, Evers R. PubMed

Transporter function

  • Clin Pharmacol Ther. 2020:In press. Identification of Glycochenodeoxycholate 3-O-Glucuronide and Glycodeoxycholate 3-O-Glucuronide as highly sensitive and specific OATP1B1 biomarkers. Neuvonen M, Hirvensalo P, Tornio A, Rago B, West M, Lazzaro S, Mathialagan S, Varma M, Cerny MA, Costales C, Ramanathan R, Rodrigues AD, Niemi M. PubMed
  • Pharmaceutics. 2020 Apr 24;12(4):390. Acamprosate is a substrate of the human Organic Anion Transporter (OAT) 1 without OAT3 inhibitory properties: Implications for renal Acamprosate secretion and Drug-Drug interactions. Antonescu IE, Karlgren M, Pedersen ML, Simoff I, Bergström CAS, Neuhoff S, Artursson P, Steffansen B, Nielsen CU. PubMed
  • Clin Pharmacol Ther. 2020 Aug 31. 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
  • Xenobiotica. 2020:1-10. 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

Passive permeability

  • Chem Med Chem. 2020;In press. The critical role of passive permeability in designing successful drugs. Di L, Artursson P, Avdeef A, Benet LZ, Houston JB, Kansy M, Kerns EH, Lennernäs H, Smith DA, Sugano K. PubMed

Human liver cells

  • Liver Int. 2020;40:1770-1780. Cell-type-resolved proteomic analysis of the human liver. Ölander M, Wiśniewski JR, Artursson P. PubMed

Hepatocyte spheroids

  • Toxicol In Vitro. 2020;In press. Characterization of primary mouse hepatocyte spheroids as a model system to support investigations of drug-induced liver injury. Nautiyal M, Qasem RJ, Fallon JK, Wolf KK, Liu J, Dixon D, Smith PC, Mosedale M. PubMed