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Items: 45

1.

Discovery of a class of highly potent Janus Kinase 1/2 (JAK1/2) inhibitors demonstrating effective cell-based blockade of IL-13 signaling.

Zak M, Hanan EJ, Lupardus P, Brown DG, Robinson C, Siu M, Lyssikatos JP, Romero FA, Zhao G, Kellar T, Mendonca R, Ray NC, Goodacre SC, Crackett PH, McLean N, Hurley CA, Yuen PW, Cheng YX, Liu X, Liimatta M, Kohli PB, Nonomiya J, Salmon G, Buckley G, Lloyd J, Gibbons P, Ghilardi N, Kenny JR, Johnson A.

Bioorg Med Chem Lett. 2019 Jun 15;29(12):1522-1531. doi: 10.1016/j.bmcl.2019.04.008. Epub 2019 Apr 4.

PMID:
30981576
2.

Does In Vitro Cytochrome P450 Downregulation Translate to In Vivo Drug-Drug Interactions? Preclinical and Clinical Studies With 13-cis-Retinoic Acid.

Stevison F, Kosaka M, Kenny JR, Wong S, Hogarth C, Amory JK, Isoherranen N.

Clin Transl Sci. 2019 Jan 25. doi: 10.1111/cts.12616. [Epub ahead of print]

PMID:
30681285
3.

Lung-restricted inhibition of Janus kinase 1 is effective in rodent models of asthma.

Dengler HS, Wu X, Peng I, Rinderknecht CH, Kwon Y, Suto E, Kohli PB, Liimatta M, Barrett K, Lloyd J, Cain G, Briggs M, Addo S, Salmon G, Ubhayakar S, Deshmukh G, Shahidi-Latham SK, Quiason-Huynh CM, Jackman J, Liu J, Ray NC, Goodacre SC, Johnson A, McKenzie BS, Lee WP, Zak M, Kenny JR, Ghilardi N.

Sci Transl Med. 2018 Nov 21;10(468). pii: eaao2151. doi: 10.1126/scitranslmed.aao2151.

PMID:
30463918
4.

Improving Confidence in the Determination of Free Fraction for Highly Bound Drugs Using Bidirectional Equilibrium Dialysis.

Chen YC, Kenny JR, Wright M, Hop CECA, Yan Z.

J Pharm Sci. 2019 Mar;108(3):1296-1302. doi: 10.1016/j.xphs.2018.10.011. Epub 2018 Oct 14.

PMID:
30326208
5.

Development of a mass spectrometry-based tryptophan 2, 3-dioxygenase assay using liver cytosol from multiple species.

Wang J, Takahashi RH, DeMent K, Gustafson A, Kenny JR, Wong SG, Yan Z.

Anal Biochem. 2018 Sep 1;556:85-90. doi: 10.1016/j.ab.2018.06.025. Epub 2018 Jun 28.

PMID:
29959909
6.

Considerations from the Innovation and Quality Induction Working Group in Response to Drug-Drug Interaction Guidances from Regulatory Agencies: Focus on CYP3A4 mRNA In Vitro Response Thresholds, Variability, and Clinical Relevance.

Kenny JR, Ramsden D, Buckley DB, Dallas S, Fung C, Mohutsky M, Einolf HJ, Chen L, Dekeyser JG, Fitzgerald M, Goosen TC, Siu YA, Walsky RL, Zhang G, Tweedie D, Hariparsad N.

Drug Metab Dispos. 2018 Sep;46(9):1285-1303. doi: 10.1124/dmd.118.081927. Epub 2018 Jun 29.

PMID:
29959133
7.

Utility of Pooled Cryopreserved Human Enterocytes as an In vitro Model for Assessing Intestinal Clearance and Drug-Drug Interactions.

Wong S, Doshi U, Vuong P, Liu N, Tay S, Le H, Kosaka M, Kenny JR, Li AP, Yan Z.

Drug Metab Lett. 2018;12(1):3-13. doi: 10.2174/1872312812666171213114422.

PMID:
29237391
8.

Considerations from the IQ Induction Working Group in Response to Drug-Drug Interaction Guidance from Regulatory Agencies: Focus on Downregulation, CYP2C Induction, and CYP2B6 Positive Control.

Hariparsad N, Ramsden D, Palamanda J, Dekeyser JG, Fahmi OA, Kenny JR, Einolf H, Mohutsky M, Pardon M, Siu YA, Chen L, Sinz M, Jones B, Walsky R, Dallas S, Balani SK, Zhang G, Buckley D, Tweedie D.

Drug Metab Dispos. 2017 Oct;45(10):1049-1059. doi: 10.1124/dmd.116.074567. Epub 2017 Jun 23.

PMID:
28646080
9.

Prediction of Drug-Drug Interactions Arising from CYP3A induction Using a Physiologically Based Dynamic Model.

Almond LM, Mukadam S, Gardner I, Okialda K, Wong S, Hatley O, Tay S, Rowland-Yeo K, Jamei M, Rostami-Hodjegan A, Kenny JR.

Drug Metab Dispos. 2016 Jun;44(6):821-32. doi: 10.1124/dmd.115.066845. Epub 2016 Mar 29. Erratum in: Drug Metab Dispos. 2016 Jun;44(6):877.

10.

Evaluation of Time Dependent Inhibition Assays for Marketed Oncology Drugs: Comparison of Human Hepatocytes and Liver Microsomes in the Presence and Absence of Human Plasma.

Mao J, Tay S, Khojasteh CS, Chen Y, Hop CE, Kenny JR.

Pharm Res. 2016 May;33(5):1204-19. doi: 10.1007/s11095-016-1865-9. Epub 2016 Feb 11.

PMID:
26869174
11.

Development of a Physiologically Based Pharmacokinetic Model for Itraconazole Pharmacokinetics and Drug-Drug Interaction Prediction.

Chen Y, Ma F, Lu T, Budha N, Jin JY, Kenny JR, Wong H, Hop CE, Mao J.

Clin Pharmacokinet. 2016 Jun;55(6):735-49. doi: 10.1007/s40262-015-0352-5.

PMID:
26692192
12.

Assessment of Disease-Related Therapeutic Protein Drug-Drug Interaction for Etrolizumab in Patients With Moderately to Severely Active Ulcerative Colitis.

Wei X, Kenny JR, Dickmann L, Maciuca R, Looney C, Tang MT.

J Clin Pharmacol. 2016 Jun;56(6):693-704. doi: 10.1002/jcph.649. Epub 2016 Jan 11.

13.

Exploring concepts of in vitro time-dependent CYP inhibition assays.

Stresser DM, Mao J, Kenny JR, Jones BC, Grime K.

Expert Opin Drug Metab Toxicol. 2014 Feb;10(2):157-74. doi: 10.1517/17425255.2014.856882. Epub 2013 Nov 21. Review.

PMID:
24256452
14.

Design and evaluation of novel 8-oxo-pyridopyrimidine Jak1/2 inhibitors.

Labadie S, Barrett K, Blair WS, Chang C, Deshmukh G, Eigenbrot C, Gibbons P, Johnson A, Kenny JR, Kohli PB, Liimatta M, Lupardus PJ, Shia S, Steffek M, Ubhayakar S, van Abbema A, Zak M.

Bioorg Med Chem Lett. 2013 Nov 1;23(21):5923-30. doi: 10.1016/j.bmcl.2013.08.082. Epub 2013 Aug 27.

PMID:
24042009
15.

2-Amino-[1,2,4]triazolo[1,5-a]pyridines as JAK2 inhibitors.

Siu M, Pastor R, Liu W, Barrett K, Berry M, Blair WS, Chang C, Chen JZ, Eigenbrot C, Ghilardi N, Gibbons P, He H, Hurley CA, Kenny JR, Cyrus Khojasteh S, Le H, Lee L, Lyssikatos JP, Magnuson S, Pulk R, Tsui V, Ultsch M, Xiao Y, Zhu BY, Sampath D.

Bioorg Med Chem Lett. 2013 Sep 1;23(17):5014-21. doi: 10.1016/j.bmcl.2013.06.008. Epub 2013 Jun 15.

PMID:
23870430
16.

Therapeutic protein drug-drug interactions: navigating the knowledge gaps-highlights from the 2012 AAPS NBC Roundtable and IQ Consortium/FDA workshop.

Kenny JR, Liu MM, Chow AT, Earp JC, Evers R, Slatter JG, Wang DD, Zhang L, Zhou H.

AAPS J. 2013 Oct;15(4):933-40. doi: 10.1208/s12248-013-9495-1. Epub 2013 Jun 21.

17.

Critical review of preclinical approaches to investigate cytochrome p450-mediated therapeutic protein drug-drug interactions and recommendations for best practices: a white paper.

Evers R, Dallas S, Dickmann LJ, Fahmi OA, Kenny JR, Kraynov E, Nguyen T, Patel AH, Slatter JG, Zhang L.

Drug Metab Dispos. 2013 Sep;41(9):1598-609. doi: 10.1124/dmd.113.052225. Epub 2013 Jun 21. Review.

PMID:
23792813
18.

Identification of C-2 hydroxyethyl imidazopyrrolopyridines as potent JAK1 inhibitors with favorable physicochemical properties and high selectivity over JAK2.

Zak M, Hurley CA, Ward SI, Bergeron P, Barrett K, Balazs M, Blair WS, Bull R, Chakravarty P, Chang C, Crackett P, Deshmukh G, DeVoss J, Dragovich PS, Eigenbrot C, Ellwood C, Gaines S, Ghilardi N, Gibbons P, Gradl S, Gribling P, Hamman C, Harstad E, Hewitt P, Johnson A, Johnson T, Kenny JR, Koehler MF, Bir Kohli P, Labadie S, Lee WP, Liao J, Liimatta M, Mendonca R, Narukulla R, Pulk R, Reeve A, Savage S, Shia S, Steffek M, Ubhayakar S, van Abbema A, Aliagas I, Avitabile-Woo B, Xiao Y, Yang J, Kulagowski JJ.

J Med Chem. 2013 Jun 13;56(11):4764-85. doi: 10.1021/jm4004895. Epub 2013 May 31.

PMID:
23659214
19.

Novel triazolo-pyrrolopyridines as inhibitors of Janus kinase 1.

Hurley CA, Blair WS, Bull RJ, Chang C, Crackett PH, Deshmukh G, Dyke HJ, Fong R, Ghilardi N, Gibbons P, Hewitt PR, Johnson A, Johnson T, Kenny JR, Kohli PB, Kulagowski JJ, Liimatta M, Lupardus PJ, Maxey RJ, Mendonca R, Narukulla R, Pulk R, Ubhayakar S, van Abbema A, Ward SI, Waszkowycz B, Zak M.

Bioorg Med Chem Lett. 2013 Jun 15;23(12):3592-8. doi: 10.1016/j.bmcl.2013.04.018. Epub 2013 Apr 17.

PMID:
23642482
20.

A physiologically based pharmacokinetic modeling approach to predict disease-drug interactions: suppression of CYP3A by IL-6.

Machavaram KK, Almond LM, Rostami-Hodjegan A, Gardner I, Jamei M, Tay S, Wong S, Joshi A, Kenny JR.

Clin Pharmacol Ther. 2013 Aug;94(2):260-8. doi: 10.1038/clpt.2013.79. Epub 2013 Apr 10.

PMID:
23588308
21.

Predictive DMPK: in silico ADME predictions in drug discovery.

Kenny JR.

Mol Pharm. 2013 Apr 1;10(4):1151-2. doi: 10.1021/mp400102t. No abstract available.

PMID:
23540938
22.

Application of in vitro-in vivo extrapolation (IVIVE) and physiologically based pharmacokinetic (PBPK) modelling to investigate the impact of the CYP2C8 polymorphism on rosiglitazone exposure.

Yeo KR, Kenny JR, Rostami-Hodjegan A.

Eur J Clin Pharmacol. 2013 Jun;69(6):1311-20. doi: 10.1007/s00228-012-1467-3. Epub 2013 Jan 11.

PMID:
23307233
23.

Discovery and Biological Profiling of Potent and Selective mTOR Inhibitor GDC-0349.

Pei Z, Blackwood E, Liu L, Malek S, Belvin M, Koehler MF, Ortwine DF, Chen H, Cohen F, Kenny JR, Bergeron P, Lau K, Ly C, Zhao X, Estrada AA, Truong T, Epler JA, Nonomiya J, Trinh L, Sideris S, Lesnick J, Bao L, Vijapurkar U, Mukadam S, Tay S, Deshmukh G, Chen YH, Ding X, Friedman LS, Lyssikatos JP.

ACS Med Chem Lett. 2012 Nov 29;4(1):103-7. doi: 10.1021/ml3003132. eCollection 2013 Jan 10.

24.

Structure-based discovery of C-2 substituted imidazo-pyrrolopyridine JAK1 inhibitors with improved selectivity over JAK2.

Labadie S, Dragovich PS, Barrett K, Blair WS, Bergeron P, Chang C, Deshmukh G, Eigenbrot C, Ghilardi N, Gibbons P, Hurley CA, Johnson A, Kenny JR, Kohli PB, Kulagowski JJ, Liimatta M, Lupardus PJ, Mendonca R, Murray JM, Pulk R, Shia S, Steffek M, Ubhayakar S, Ultsch M, van Abbema A, Ward S, Zak M.

Bioorg Med Chem Lett. 2012 Dec 15;22(24):7627-33. doi: 10.1016/j.bmcl.2012.10.008. Epub 2012 Oct 11.

PMID:
23107482
25.

Discovery of potent and selective pyrazolopyrimidine janus kinase 2 inhibitors.

Hanan EJ, van Abbema A, Barrett K, Blair WS, Blaney J, Chang C, Eigenbrot C, Flynn S, Gibbons P, Hurley CA, Kenny JR, Kulagowski J, Lee L, Magnuson SR, Morris C, Murray J, Pastor RM, Rawson T, Siu M, Ultsch M, Zhou A, Sampath D, Lyssikatos JP.

J Med Chem. 2012 Nov 26;55(22):10090-107. doi: 10.1021/jm3012239. Epub 2012 Oct 24.

PMID:
23061660
26.

Comparative assessment of In Vitro-In Vivo extrapolation methods used for predicting hepatic metabolic clearance of drugs.

Poulin P, Hop CE, Ho Q, Halladay JS, Haddad S, Kenny JR.

J Pharm Sci. 2012 Nov;101(11):4308-26. doi: 10.1002/jps.23288. Epub 2012 Aug 13.

PMID:
22890957
27.

Discovery and optimization of C-2 methyl imidazopyrrolopyridines as potent and orally bioavailable JAK1 inhibitors with selectivity over JAK2.

Zak M, Mendonca R, Balazs M, Barrett K, Bergeron P, Blair WS, Chang C, Deshmukh G, Devoss J, Dragovich PS, Eigenbrot C, Ghilardi N, Gibbons P, Gradl S, Hamman C, Hanan EJ, Harstad E, Hewitt PR, Hurley CA, Jin T, Johnson A, Johnson T, Kenny JR, Koehler MF, Bir Kohli P, Kulagowski JJ, Labadie S, Liao J, Liimatta M, Lin Z, Lupardus PJ, Maxey RJ, Murray JM, Pulk R, Rodriguez M, Savage S, Shia S, Steffek M, Ubhayakar S, Ultsch M, van Abbema A, Ward SI, Xiao L, Xiao Y.

J Med Chem. 2012 Jul 12;55(13):6176-93. doi: 10.1021/jm300628c. Epub 2012 Jun 28.

PMID:
22698084
28.

Discovery of novel PI3-kinase δ specific inhibitors for the treatment of rheumatoid arthritis: taming CYP3A4 time-dependent inhibition.

Safina BS, Baker S, Baumgardner M, Blaney PM, Chan BK, Chen YH, Cartwright MW, Castanedo G, Chabot C, Cheguillaume AJ, Goldsmith P, Goldstein DM, Goyal B, Hancox T, Handa RK, Iyer PS, Kaur J, Kondru R, Kenny JR, Krintel SL, Li J, Lesnick J, Lucas MC, Lewis C, Mukadam S, Murray J, Nadin AJ, Nonomiya J, Padilla F, Palmer WS, Pang J, Pegg N, Price S, Reif K, Salphati L, Savy PA, Seward EM, Shuttleworth S, Sohal S, Sweeney ZK, Tay S, Tivitmahaisoon P, Waszkowycz B, Wei B, Yue Q, Zhang C, Sutherlin DP.

J Med Chem. 2012 Jun 28;55(12):5887-900. doi: 10.1021/jm3003747. Epub 2012 Jun 11.

PMID:
22626259
29.

Identification of imidazo-pyrrolopyridines as novel and potent JAK1 inhibitors.

Kulagowski JJ, Blair W, Bull RJ, Chang C, Deshmukh G, Dyke HJ, Eigenbrot C, Ghilardi N, Gibbons P, Harrison TK, Hewitt PR, Liimatta M, Hurley CA, Johnson A, Johnson T, Kenny JR, Bir Kohli P, Maxey RJ, Mendonca R, Mortara K, Murray J, Narukulla R, Shia S, Steffek M, Ubhayakar S, Ultsch M, van Abbema A, Ward SI, Waszkowycz B, Zak M.

J Med Chem. 2012 Jun 28;55(12):5901-21. doi: 10.1021/jm300438j. Epub 2012 Jun 11.

PMID:
22591402
30.

Drug-drug interaction potential of marketed oncology drugs: in vitro assessment of time-dependent cytochrome P450 inhibition, reactive metabolite formation and drug-drug interaction prediction.

Kenny JR, Mukadam S, Zhang C, Tay S, Collins C, Galetin A, Khojasteh SC.

Pharm Res. 2012 Jul;29(7):1960-76. doi: 10.1007/s11095-012-0724-6. Epub 2012 Mar 14.

PMID:
22415140
31.

Evaluation of time-dependent cytochrome p450 inhibition in a high-throughput, automated assay: introducing a novel area under the curve shift approach.

Mukadam S, Tay S, Tran D, Wang L, Delarosa EM, Khojasteh SC, Halladay JS, Kenny JR.

Drug Metab Lett. 2012 Mar;6(1):43-53.

PMID:
22372554
32.

Application of IVIVE and PBPK modeling in prospective prediction of clinical pharmacokinetics: strategy and approach during the drug discovery phase with four case studies.

Chen Y, Jin JY, Mukadam S, Malhi V, Kenny JR.

Biopharm Drug Dispos. 2012 Mar;33(2):85-98. doi: 10.1002/bdd.1769. Epub 2012 Jan 24.

PMID:
22228214
33.

In vitro-in vivo extrapolation of clearance: modeling hepatic metabolic clearance of highly bound drugs and comparative assessment with existing calculation methods.

Poulin P, Kenny JR, Hop CE, Haddad S.

J Pharm Sci. 2012 Feb;101(2):838-51. doi: 10.1002/jps.22792. Epub 2011 Oct 18.

PMID:
22009717
34.

Novel mechanism for dehalogenation and glutathione conjugation of dihalogenated anilines in human liver microsomes: evidence for ipso glutathione addition.

Zhang C, Kenny JR, Le H, Deese A, Ford KA, Lightning LK, Fan PW, Driscoll JP, Halladay JS, Hop CE, Khojasteh SC.

Chem Res Toxicol. 2011 Oct 17;24(10):1668-77. doi: 10.1021/tx2002228. Epub 2011 Sep 25.

PMID:
21905702
35.

Chemical inhibitors of cytochrome P450 isoforms in human liver microsomes: a re-evaluation of P450 isoform selectivity.

Khojasteh SC, Prabhu S, Kenny JR, Halladay JS, Lu AY.

Eur J Drug Metab Pharmacokinet. 2011 Mar;36(1):1-16. doi: 10.1007/s13318-011-0024-2. Epub 2011 Feb 19. Review.

PMID:
21336516
36.

Preclinical assessment of the absorption, distribution, metabolism and excretion of GDC-0449 (2-chloro-N-(4-chloro-3-(pyridin-2-yl)phenyl)-4-(methylsulfonyl)benzamide), an orally bioavailable systemic Hedgehog signalling pathway inhibitor.

Wong H, Chen JZ, Chou B, Halladay JS, Kenny JR, La H, Marsters JC Jr, Plise E, Rudewicz PJ, Robarge K, Shin Y, Wong S, Zhang C, Khojasteh SC.

Xenobiotica. 2009 Nov;39(11):850-61. doi: 10.3109/00498250903180289.

PMID:
19845436
37.

Inhibitory properties of trapping agents: glutathione, potassium cyanide, and methoxylamine, against major human cytochrome p450 isoforms.

Zhang C, Wong S, Delarosa EM, Kenny JR, Halladay JS, Hop CE, Khojasteh-Bakht SC.

Drug Metab Lett. 2009 Apr;3(2):125-9.

PMID:
19601875
38.

Evaluation of multiple in vitro systems for assessment of CYP3A4 induction in drug discovery: human hepatocytes, pregnane X receptor reporter gene, and Fa2N-4 and HepaRG cells.

McGinnity DF, Zhang G, Kenny JR, Hamilton GA, Otmani S, Stams KR, Haney S, Brassil P, Stresser DM, Riley RJ.

Drug Metab Dispos. 2009 Jun;37(6):1259-68. doi: 10.1124/dmd.109.026526. Epub 2009 Mar 23.

PMID:
19307295
39.
40.
41.

Evaluation of time-dependent cytochrome P450 inhibition using cultured human hepatocytes.

McGinnity DF, Berry AJ, Kenny JR, Grime K, Riley RJ.

Drug Metab Dispos. 2006 Aug;34(8):1291-300. Epub 2006 May 5.

PMID:
16679385
42.
43.

Formation and protein binding of the acyl glucuronide of a leukotriene B4 antagonist (SB-209247): relation to species differences in hepatotoxicity.

Kenny JR, Maggs JL, Tettey JN, Harrell AW, Parker SG, Clarke SE, Park BK.

Drug Metab Dispos. 2005 Feb;33(2):271-81. Epub 2004 Nov 2.

PMID:
15523047
44.

Syntheses and characterization of the acyl glucuronide and hydroxy metabolites of diclofenac.

Kenny JR, Maggs JL, Meng X, Sinnott D, Clarke SE, Park BK, Stachulski AV.

J Med Chem. 2004 May 20;47(11):2816-25.

PMID:
15139759
45.

A gift from Gheeus.

Kenny JR, Justice S.

Weather Vane. 1984 Dec;53(6):6-8. No abstract available.

PMID:
6570080

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