• Clin Pharmacol Ther. 2019;105:1345-1361. Clinical studies on Drug-Drug Interactions involving metabolism and transport: Methodology, pitfalls, and interpretation. Tornio A, Filppula AM, Niemi M, Backman JT. The authors present considerations related to general DDI study designs, recommended enzyme and transporter index substrates and inhibitors, pharmacogenetic perspectives, index drug cocktails, endogenous substrates, limited sampling strategies, physiologically-based pharmacokinetic modeling, complex DDIs, methodological pitfalls, and interpretation of DDI information. PubMed
  • Clin Pharmacol Ther. 2019;in press. The Clinical Pharmacogenetics Implementation Consortium: 10 years later. Relling MV, Klein TE, Gammal RS, Whirl-Carrillo M, Hoffman JM, Caudle KE. In 2009, the Clinical Pharmacogenetics Implementation Consortium (CPIC), is a shared project between Pharmacogenomics Knowledge Base (PharmGKB), and the Pharmacogenomics Research Network (PGRN). It was created to provide freely available, evidence-based, peer-reviewed, and updated pharmacogenetic clinical practice guidelines. To date, CPIC has published 23 guidelines (of which 11 have been updated), covering 19 genes and 46 drugs across several therapeutic areas. PubMed

Hepatic transporters and pharmacogenetics

  • Pulm Pharmacol Ther. 2019;In press. Fevipiprant has a low risk of influencing co-medication pharmacokinetics: Impact on simvastatin and rosuvastatin in different SLCO1B1 genotypes. Poller B, Woessner R, Barve A, Tillmann HC, Vemula J, Nica A, Elbast W, Schiller H, End P, Camenisch G, Weiss M. PubMed
  • AAPS J. 2019;21:69. Estimating in vivo fractional contribution of OATP1B1 to human hepatic active uptake by mechanistically modeling pharmacogenetic data. Li R. PubMed
  • Clin Pharmacol Ther. 2019;in press.  Global pharmacogenomics within Precision Medicine: challenges and opportunities. Chenoweth MJ, Giacomini KM, Pirmohamed M, Hill SL, van Schaik RHN, Schwab M, Shuldiner AR, Relling MV, Tyndale RF. PubMed
  • Clin Pharmacol Ther. 2019;in press. Genomewide association study of statin-induced myopathy in patients recruited using the UK Clinical Practice Research Datalink. Carr DF, Francis B, Jorgensen AL, Zhang E, Chinoy H, Heckbert SR, Bis JC, Brody JA, Floyd JS, Psaty BM, Molokhia M, Lapeyre-Mestre M, Conforti A, Alfirevic A, van Staa T, Pirmohamed M. PubMed
  • Clin Pharmacol Ther. 2019;106:936-938. Pharmacogenomics in practice. Wang L, Weinshilboum R. PubMed
  • Clin Pharmacol Ther. 2019;106:668-680. Enantiospecific pharmacogenomics of Fluvastatin. Hirvensalo P, Tornio A, Neuvonen M, Kiander W, Kidron H, Paile-Hyvärinen M, Tapaninen T, Backman JT, Niemi M. PubMed
  • Clin Pharmacol Ther. 2019;106:329-337. Diabetes: Is there a future for pharmacogenomics guided treatment? Pearson ER. PubMed

Liver imaging

  • Mol Pharm. 2019;In press.  Measurement of hepatic ABCB1 and ABCG2 transport activity with [11C]tariquidar and PET in humans and mice. Hernandez Lozano I, Bauer M, Wulkersdorfer B, Traxl A, Philippe C, Weber M, Häusler S, Stieger B, Jäger W, Mairinger S, Wanek T, Hacker M, Zeitlinger M, Langer O. PubMed


  • J Pharmacol Exp Ther. 2019;371:385-393. A pharmacokinetic natural product-disease-drug interaction: A double hit of Silymarin and Nonalcoholic Steatohepatitis on hepatic transporters in a rat model. Montonye ML, Tian DD, Arman T, Lynch KD, Hagenbuch B, Paine MF, Clarke JD. PubMed

Transporter inhibition and endogenous substrates

  • Clin Pharmacol Ther. 2019;in press. Dose-dependent inhibition of OATP1B by rifampicin in healthy volunteers: Comprehensive evaluation of candidate biomarkers and OATP1B probe drugs. Mori D, Kimoto E, Rago B, Kondo Y, King-Ahmad A, Ramanathan R, Wood LS, Johnson JG, Le VH, Vourvahis M, Rodrigues AD, Muto C, Furihata K, Sugiyama Y, Kusuhara H. To address the most appropriate endogenous biomarker for drug-drug interaction risk assessment, 8 healthy subjects received rifampicin (150, 300 and 600 mg) and a probe drug cocktail (atorvastatin, pitavastatin, rosuvastatin and valsartan). In addition to coproporphyrin I, direct bilirubin, glycochenodeoxycholate-3-glucuronide, glycocheno-deoxycholate-3-sulfate, and hexadecanedioate had good sensitivity and dynamic range in terms of rifampicin dose-dependent change in area under the plasma concentration-time curve ratio (AUCR). Their suitability as OATP1B biomarkers was also supported by the good correlation of AUC0-24h between the endogenous compounds and the probe drugs, and by non-linear regression analysis (AUCR-1 versus rifampicin plasma Cmax) to yield an estimate of the inhibition constant of rifampicin. These endogenous substrates can complement existing OATP1B-mediated drug-drug interaction risk assessment approaches based on agency guidelines in early clinical trials. PubMed
  • Clin Pharmacol Ther. 2019;In press. Complex DDI by Fenebrutinib and the use of transporter endogenous biomarkers to elucidate the mechanism of DDI. Jones NS, Yoshida K, Salphati L, Kenny JR, Durk MR, Chinn LW. PubMed
  • Drug Metab Dispos. 2019;47:1270-1280. Elucidation of N 1-methyladenosine as a potential surrogate biomarker for drug interaction studies involving renal Organic Cation Transporters. Miyake T, Mizuno T, Takehara I, Mochizuki T, Kimura M, Matsuki S, Irie S, Watanabe N, Kato Y, Ieiri I, Maeda K, Ando O, Kusuhara H. PubMed

Transporters at the Blood-Brain Barrier

  • Clin Pharmacol Ther. 2019;in press. Protein expression and functional relevance of efflux and uptake drug transporters at the Blood-Brain Barrier of human brain and glioblastoma. Bao X, Wu J, Xie Y, Kim S, Michelhaugh S, Jiang J, Mittal S, Sanai N, Li J. PubMed

PBPK and membrane transporter

  • Clin Pharmacol Ther. 2019;In press. PBPK models for evaluating membrane transporter mediated DDIs: Current capabilities, case studies, future opportunities and recommendations. Taskar K, Pilla Reddy V, Howard B, Posada MM, Varma M, Zheng M, Ullah M, Emami Riedmaier A, Umehara KI, Snoeys J, Nakakariya M, Chu X, Beneton M, Chen Y, Huth F, Narayanan R, Mukherjee D, Dixit V1, Sugiyama Y, Neuhoff S. This review provides a reflection on the current trends in PBPK modelling for tDDIs and provides a framework to promote continuous use, verification and improvement in industrialisation of the transporter PBPK modelling. PubMed
  • Drug Metab Dispos. 2019;In press. Mechanistic modeling of the hepatic disposition of Estradiol-17β-Glucuronide in Sandwich-Cultured Human Hepatocytes. Ito K, Sjostedt N, Brouwer KLR. PubMed
  • Drug Metab Dispos. 2019;47:1066-1079. Prediction of Atorvastatin pharmacokinetics in high-fat diet and low-dose Streptozotocin-induced diabetic rats using a semi-Physiologically Based Pharmacokinetic model involving both enzymes and transporters. Wang Z, Yang H, Xu J, Zhao K, Chen Y, Liang L, Li P, Chen N, Geng D, Zhang X, Liu X, Liu L. PubMed

Inhibitor preincubation

  • Drug Metab Dispos. 2019;47:1352-1360. Enhanced and persistent inhibition of Organic Cation Transporter 1 activity by preincubation of Cyclosporine A. Panfen E, Chen W, Zhang Y, Sinz M, Marathe P, Gan J, Shen H. PubMed

Hepatic transporter expression

  • Clin Pharmacol Ther. 2019;in press. Protein abundance of hepatic drug transporters in patients with different forms of liver damage. Drozdzik M, Szelag-Pieniek S, Post M, Zeair S, Wrzesinski M, Kurzawski M, Prieto J, Oswald S. PubMed
  • Int J Mol Sci. 2019;20. pii: E5303. Protein abundance of clinically relevant drug transporters in the human kidneys. Oswald S, Müller J, Neugebauer U, Schröter R, Herrmann E, Pavenstädt H, Ciarimboli G. PubMed
  • Onco Targets Ther. 2019;12:6013-6022. Role of OCT1 in hepatocellular carcinoma. Li J, Yang Z, Tuo B. PubMed
  • Biomed Pharmacother. 2019;114:108864. Increased expression of SLC46A3 to oppose the progression of hepatocellular carcinoma and its effect on sorafenib therapy. Zhao Q, Zheng B, Meng S, Xu Y, Guo J, Chen LJ, Xiao J, Zhang W, Tan ZR, Tang J, Chen L, Chen Y. SLC46A3 might serve as a potential prognostic biomarker and therapeutic target in HCC. PubMed

Hepatic transport function

  • Drug Metab Dispos. 2019;in press. Pharmacokinetics of Organic Cation Transporter 1 (OCT1) substrates in Oct1/2 Knockout mice and species difference in hepatic OCT1-mediated uptake. Morse BL, Kolur A, Hudson LR, Hogan AT, Chen LH, Brackman RM, Sawada GA, Fallon JK, Smith PC, Hillgren KM. PubMed
  • Clin Pharmacol Ther. 2019;In press. Variability and heritability of Thiamine pharmacokinetics with focus on OCT1 effects on membrane transport and pharmacokinetics in humans. Jensen O, Matthaei J, Blome F, Schwab M, Tzvetkov MV, Brockmöller J. PubMed
  • Biochem Pharmacol. 2019;168:384-391. Protein-protein interactions of drug uptake transporters that are important for liver and kidney. Zhang Y, Hagenbuch B. PubMed

Inhibition of bile acid transporters

  • Toxicol Sci. 2019;in press. High-throughput screening to evaluate inhibition of bile acid transporters using human hepatocytes isolated from chimeric mice. Kohara H, Bajaj P, Yamanaka K, Miyawaki A, Harada K, Miyamoto K, Matsui T, Okai Y, Wagoner M, Shinozawa T. PubMed

Drug-induced liver injury

  • Crit Rev Toxicol. 2019;49:520-548. Current insights in the complexities underlying drug-induced cholestasis. Deferm N, De Vocht T, Qi B, Van Brantegem P, Gijbels E, Vinken M, de Witte P, Bouillon T, Annaert P. PubMed
  • Liver Int. 2019;In press. Tanshinone IIA prevents rifampicin-induced liver injury by regulating BSEP/NTCP expression via epigenetic activation of NRF2. Yang Y, Liu L, Zhang X, Jiang X, Wang L. PubMed
  • Adv Exp Med Biol. 2019;1141:293-340. Roles of hepatic drug transporters in drug disposition and liver toxicity. Pan G. PubMed

Regulation of transporter genes

  • Drug Metab Dispos. 2019;47:1433-1442. Organic Anion-Transporting Polypeptide genes are not induced by the Pregnane X Receptor activator rifampin: Studies in hepatocytes in vitro and in Monkeys in vivo. Niu C, Wang Y, Zhao X, Tep S, Murakami E, Subramanian R, Smith B, Lai Y. PubMed

Transporters and pesticides

  • Pest Manag Sci. 2019;In press. Implication of human drug transporters to toxicokinetics and toxicity of pesticides. Guéniche N, Bruyere A, Le Vée M, Fardel O. PubMed
  • J Biochem Mol Toxicol. 2019;33:e22379. Neonicotinoid pesticides poorly interact with human drug transporters. Le Vée M, Bacle A, Bruyere A, Fardel O. PubMed