February 2021: RECENT PUBLICATIONS

Prestigious publication in Nat Rev Drug Discov

  • Nat Rev Drug Discov. 2020;19:801-818. Phase 0/microdosing approaches: time for mainstream application in drug development? Burt T, Young G, Lee W, Kusuhara H, Langer O, Rowland M, Sugiyama Y. PubMed


PK modelling

  • CPT Pharmacometrics Syst Pharmacol. 2020;9:282-293. Mechanistic models as framework for understanding biomarker disposition: Prediction of Creatinine-drug interactions. Scotcher D, Arya V, Yang X, Zhao P, Zhang L, Huang SM, Rostami-Hodjegan A, Galetin A. PubMed
  • CPT Pharmacometrics Syst Pharmacol. 2020;9:310-32. A novel physiologically based model of Creatinine renal disposition to integrate current knowledge of systems parameters and clinical observations. Scotcher D, Arya V, Yang X, Zhao P, Zhang L, Huang SM, Rostami-Hodjegan A, Galetin A. PubMed
  • CPT Pharmacometrics Syst Pharmacol. 2020;10:137-147. Application of PBPK model for coproporphyrin I to evaluate the impact of SLCO1B1 genotype, ethnicity, and sex on its inter-individual variability. Takita H, Barnett S, Zhang Y, Ménochet K, Shen H, Ogungbenro K, Galetin A. PubMed
  • CPT Pharmacometrics Syst Pharmacol.  2020;9:695-706. Takita H, Scotcher D, Chinnadurai R, Kalra PA, Galetin A. Physiologically-Based Pharmacokinetic modelling of Creatinine-drug interactions in the chronic kidney disease population. PubMed


Transporters and imaging

  • Mol Imaging Biol. 2021;In press. Human biodistribution and radiation dosimetry of the P-Glycoprotein radiotracer [11C]Metoclopramide. Bauer M, Barna S, Blaickner M, Prosenz K, Bamminger K, Pichler V, Tournier N, Hacker M, Zeitlinger M, Karanikas G, Langer O. PubMed

Transporters and endogenous biomakers

  • Drug Metab Pharmacokinet. 2021;109:55-64. Current progress in identifying endogenous biomarker candidates for drug transporter phenotyping and their potential application to drug development. Mochizuki T, Mizuno T, Maeda K, Kusuhara H. PubMed

Transporter function and regulation

  • Drug Metab Dispos. 2021;49:3-11. Functional investigation of Solute Carrier Family 35, Member F2, in three cellular models of the primate Blood-Brain Barrier. Mochizuki T, Mizuno T, Kurosawa T, Yamaguchi T, Higuchi K, Tega Y, Nozaki Y, Kawabata K, Deguchi Y, Kusuhara H. PubMed
  • J Pharmacol Exp Ther. 2021;376:29-39. Transporter activity changes in Nonalcoholic Steatohepatitis: Assessment with plasma Coproporphyrin I and III. Chatterjee S, Mukherjee S, Sankara Sivaprasad LVJ, Naik T, Gautam SS, Murali BV, Hadambar AA, Gunti GR, Kuchibhotla V, Deyati A, Basavanthappa S, Ramarao M, Mariappan TT, Zinker BA, Zhang Y, Sinz M, Shen H. PubMed
  • J Biol Chem. 2020;295:17349-17364. Post-translational regulation of the major drug transporters in the families of organic anion transporters and organic anion-transporting polypeptides. Lee W, Ha JM, Sugiyama Y. PubMed
  • J Pharmacol Exp Ther. 2021;In press. OATP1B1/1B3-mediated hepatic uptake determines the pharmacokinetics of large lipophilic acids: In vitro-in vivo evaluation in cynomolgus monkey. Eng H, Bi YA, West MA, Ryu S, Yamaguchi E, Kosa RE, Tess DA, Griffith DA, Litchfield JE, Kalgutkar AS, Varma MVS. PubMed
  • Drug Metab Dispos. 2021;In press. Function and expression of Bile Salt Export Pump in suspension human hepatocytes. Chothe PP, Pemberton R, Hariparsad N. PubMed
  • Biochim Biophys Acta Biomembr. 2021;1863:183554. Leucine heptad motifs within transmembrane domains affect function and oligomerization of human organic anion transporting polypeptide 1B1. Ni C, Wang X, Chen J, Xu S, Ye W, Hong M. PubMed
  • J Hepatol. 2020;In press. Synthetic human ABCB4 mRNA therapy rescues severe liver disease phenotype in a BALB/c.Abcb4-/- mouse model of PFIC3. Wei G, Cao J, Huang P, An P, Badlani D, Vaid K, Zhao S, Q-H Wang D, Zhuo J, Yin L, Frassetto A, Markel A, Presnyak V, Gandham S, Hua S, Lukacs C, Finn PF, Giangrande PH, Martini PG, Popov YV. PubMed
  • Hum Exp Toxicol. 2020;In press. Effects of psoralen on hepatic bile acid transporters in rats. Huang J, Wang Q, Chen M, Bi Y, Shi H, Zhou K. PubMed
  • Int J Mol Sci. 2021;22:784. The Bile Salt Export Pump: Molecular structure, study models and small-molecule drugs for the treatment of inherited BSEP deficiencies. Sohail MI, Dönmez-Cakil Y, Szöllősi D, Stockner T, Chiba P. PubMed
  • J Control Release. 2020;330:173-184. Multivalent rubber-like RNA nanoparticles for targeted co-delivery of paclitaxel and MiRNA to silence the drug efflux transporter and liver cancer drug resistance. Wang H, Ellipilli S, Lee WJ, Li X, Vieweger M, Ho YS, Guo P. PubMed
  • Eur J Pharm Sci. 2021;159:105740. The role of drug efflux and uptake transporters ABCB1 (P-gp), ABCG2 (BCRP) and OATP1A/1B and of CYP3A4 in the pharmacokinetics of the CDK inhibitor milciclib. Martínez-Chávez A, Broeders J, Lebre MC, Tibben MT, Rosing H, Beijnen JH, Schinkel AH. PubMed
  • Drug Metab Dispos. 2021;49:254-264. Evaluation of the utility of PXB chimeric mice for predicting human liver partitioning of hepatic Organic Anion-Transporting Polypeptide Transporter substrates. Feng B, Pemberton R, Dworakowski W, Ye Z, Zetterberg C, Wang G, Morikawa Y, Kumar S. PubMed

Lysosomal drug concentrations

  • Drug Metab Dispos. 2021;49:53-61. Extension of the mechanistic tissue distribution model of Rodgers and Rowland by systematic incorporation of lysosomal trapping: Impact on unbound partition coefficient and volume of distribution predictions in the rat. Schmitt MV, Reichel A, Liu X, Fricker G, Lienau P. PubMed

Transporter DDI

  • J Pharm Sci. 2021;110:517-528. Improved prediction of the Drug-Drug Interactions of Pemafibrate caused by Cyclosporine A and Rifampicin via PBPK modeling: Consideration of the albumin-mediated hepatic uptake of Pemafibrate and inhibition constants with preincubation against OATP1B. Park JE, Shitara Y, Lee W, Morita S, Sahi J, Toshimoto K, Sugiyama Y. PubMed
  • Drug Metab Dispos. 2021;49:152-158. Impact of direction of transport on the evaluation of inhibition potencies of Multidrug and Toxin Extrusion Protein 1 inhibitors. Saito A, Ishiguro N, Takatani M, Bister B, Kusuhara H. PubMed
  • Drug Metab Dispos. 2020;In press. Prediction of transporter-mediated drug-drug interactions and phenotyping of hepatobiliary transporters involved in the clearance of E7766, a novel macrocycle-bridged dinucleotide. Jiang R, Hart A, Burgess L, Kim DS, Lai WG, Dixit V. PubMed

In vitro hepatocyte model

  • Drug Metab Dispos. 2021;In press. Functional proliferating human hepatocytes: in vitro hepatocyte model for drug metabolism, excretion and toxicity. Qiao S, Feng S, Wu Z, He T, Ma C, Peng Z, Tian E, Pan G. PubMed

Drug clearance and protein binding

  • Drug Metab Dispos. 2021;In press. Impact of plasma protein binding in drug clearance prediction: a database analysis of published studies and implications for in vitro in vivo extrapolation. Francis LJ, Houston B, Hallifax D. PubMed