`
`SLC01~1
`0 -UGT-28-7---- - --
`CYP2B6
`GSTA2
`
`-5
`
`PPARG
`RXRA
`HNF4A
`ADH1A
`PPARA
`NAT1
`UGT1A1
`SLC22A7
`CYP2C19
`CYP1A2
`: CYP1A 1
`p
`Q 89
`: NR112
`earson r = .
`CYP3A5
`CYP2CB
`CYP3Al NR113
`p<Q.QQQ1
`CYP2C9 :
`-10 ~-----------r----------~----------~
`-5
`5
`0
`log2FC (IL-6 vs. Ctrl) in PHH
`
`Page 1 of 4
`
`SENJU EXHIBIT 2133
`LUPIN v. SENJU
`IPR2015-01097
`
`
`
`DRUG METABOLISM
`AND DISPOSITION
`
`A Publication of the American Society for Pharmacology and Experimental Therapeutics
`
`February 2015
`
`Vol. 43, No.2
`
`CONTENTS
`
`PERSPECTIVE
`
`Mass Cytometry: A Highly Multiplexed Single-Cell
`Technology for Advancing Drug Development.
`Xondala R. Atkuri, Jeffrey C. Stevens, and Hendrik
`Neubert. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 227
`
`SHORT COMMUNICATION
`
`[§] Quantitative Transporter Proteomics by Liquid Chroma(cid:173)
`tography with Tandem Mass Spectrometry: Address-
`ing Methodologic Issues of Plasma Membrane
`Isolation and Expression-Activity Relationship.
`Vineet Kumar, Bhagwat Prasad, Gabriela Patilea,
`Anshul Gupta, Laurent Salphati, Raymond Evers,
`Camelis E. C. A Hop, and Jashvant D. Unadkat. . . 284
`
`ARTICLES
`[§] Physiologically Based Pharmacokinetic Modeling to
`Predict Drug-Drug Interactions Involving Inhibitory
`Metabolite: A Case Study of Amiodarone. Yuan
`Chen, Jialin Mao, and Camelis E. C. A. Hop . . . . 182
`
`[§] Comparison of the Circulating Metabolite Profile of
`PF-04991532, a Hepatoselective Glucokinase Ac(cid:173)
`tivator, Across Preclinical Species and Humans:
`Potential Implications in Metabolites in Safety
`Testing Assessment. Raman Shamw, John Litcllfield,
`Arthur Bergnwn, Karen Atkil!Son, David Kazierad,
`Stephanie M Gustavson, Li Di, Jeffrey A. Pfefferkorn,
`and Amit S. Kalgutkar. . . . . . . . . . . . . . . . . . . 190
`
`Zinc Finger Nuclease-Mediated Gene Knockout Results
`in Loss of Transport Activity for P-Glycoprotein, BCRP,
`and MRP2 in Caco-2 Cells. Kathleen E. Sampson,
`Amanda Blinkn~ Jennifer Pratt, Neetu Venkatraman,
`Yongling Xiao, Jim Blasberg, Toni Steine1~ Maureen
`Boume1~ and David C. Thompson. . . . . . . . . . . . . . 199
`
`[§] Charactetization of CYP2B6 in a CYP2B6-Humanized
`Mouse Model: Inducibility in the Liver by Pheno(cid:173)
`barbital and Dexamethasone and Role in Nico(cid:173)
`tine Metabolism In Vivo. Zhihua Liu, Lei Li,
`Hong Wu, ling Hu, fun Ma, Qing-Yu Zhang,
`and Xinxin Ding . . . . . . . . . . . . . . . . . . . . . 208
`
`[§] Analysis of the Disposition of a Novel p38 MAPK
`Inhibitor, AKP-00 1, and Its Metabolites in Rats
`
`with a Simple Physiologically Based Pharma(cid:173)
`cokinetic Model. Kazuhiko Shirota, Makoto
`Kaneko, Makoto Sasaki, Kouichi Minato, Akira
`Fujikata, Shuji Ohta, Akihiro Hisaka, and Hiroshi
`Suzuki ...... .......................... 217
`
`[§] Investigation of the Impact of Substrate Selection on
`In Vitro Organic Anion Transporting Polypeptide
`lB 1 Inhibition Profiles for the Prediction of Drug(cid:173)
`Drug Interactions. Saki Izumi, Yoshitane Nozaki,
`Kazuya Maeda, Takafumi Komori, Osamu Takenaka,
`Hiroyuki Kusuhara, and Yuichi Sugiyama ...... ~ . 235
`
`[§] Mass Spectrometric Evaluation of Mephedrone In
`Identification of
`Vivo Human Metabolism:
`Phase I and Phase II Metabolites, Including
`a Novel Succinyl Conjugate. Oscar J. Pozo,
`Marla lbaliez, Juan V. Sancho, Julio Lahoz(cid:173)
`Beneytez, Mag{ Fan·e, Esther Papaseit, Rafael
`de la Torre, and Felix Hernandez. . . . . . . . . . 248
`
`Drug-Metabolizing and Antioxidant Enzymes in
`Monosodium L-Glutamate Obese Mice. Petra
`Matouskova, Hana Bartfkova, Iva Bousova,
`Lucie Levorova, Barbara Szotakova, and Lenka
`Skdlova . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 258
`
`[§] Renal Xenobiotic Transporter Expression is Altered in
`Multiple Expetimental Models of Nonalcoholic
`Steatohepatitis. Mark J. Canet, Rhiannon N.
`Hardwick, April D. Lake, Anika L. Dzierlenga,
`John D. Clarke, Michael J. Goedken, and Nathan
`J. Cherrington . . . . . . . . . . . . . . . . . . . . . . . . . 266
`
`[§] A Systematic Comparison of the Impact of Inflam(cid:173)
`matory Signaling on Absorption, Distribution,
`Metabolism, and Excretion Gene Expression and
`Activity in Primary Human Hepatocytes and
`HepaRG Cells. Marcus Klein, Maria Thomas,
`Ute Hofmann, Daniel Seehafer, Georg Damm,
`and Ulrich M. Zanger. . . . . . . . . . . . . . . . . . 273
`
`[§] Absorption, Metabolism, and Excretion of Oral 14C
`Radiolabeled Ibrutinib: An Open-Label, Phase I,
`Single-Dose Study in Healthy Men. Ellen Scheers,
`Laurent Leclercq, Jan de long, Nini Bode, Marc
`
`Continued on next page
`
`Page 2 of 4
`
`
`
`Contents (cont'd.)
`
`Bockx, Aline Laenen, Filip Cuyckens, Donna Skee,
`Joe Murphy, Juthamas Sukbunthemg, and Geert
`Mannens . ............................ 289
`
`NOTICE OF RETRACTION
`Notice of Retraction. . . . . . . . . . . . . . . . . . . . . . . . 234
`
`NOTICE OF CONCERN
`Notice of Concern. . . . . . . . . . . . . . . . . . . . . . . . . 298
`
`[ID Supplemental material is available online at http://dmd.aspetjournals.org.
`
`About the cover: Correlation of IL-6-induced gene expression changes in PHH and HepaRG cells. See the article by Klein et al.
`(dx.doi.org/10.1124/dmd.ll4.060962)
`
`Page 3 of 4
`
`
`
`Notice of Retraction
`
`Re: Kadam RS, Vooturi SK, Kompella UB. Immunohistochemical and functional characterization of
`peptide, organic cation, neutral and basic amino acid, and monocarboxylate drug transporters in human
`ocular tissues. Drug Metab Dispos February 2013 41:466---474; doi:l0.1124/dmd.112.045674
`
`The University of Colorado and authors have requested that this article be withdrawn due to data integrity
`problems with some LC-MS/MS peak areas in Figure 10 (A-D) and Figure 11 (A-C). The data were found
`to be falsified to improve the differences or kinetics. Dmg Metab Dispos has retracted this article.
`
`234
`
`Page 4 of 4
`
`