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Items: 45


Considerations from the IQ 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 Jun 29. pii: dmd.118.081927. doi: 10.1124/dmd.118.081927. [Epub ahead of print]


Data Generated by Quantitative Liquid Chromatography-Mass Spectrometry Proteomics Are Only the Start and Not the Endpoint: Optimization of Quantitative Concatemer-Based Measurement of Hepatic Uridine-5'-Diphosphate-Glucuronosyltransferase Enzymes with Reference to Catalytic Activity.

Achour B, Dantonio A, Niosi M, Novak JJ, Al-Majdoub ZM, Goosen TC, Rostami-Hodjegan A, Barber J.

Drug Metab Dispos. 2018 Jun;46(6):805-812. doi: 10.1124/dmd.117.079475. Epub 2018 Mar 26.


Biosynthesis and Identification of Metabolites of Maraviroc and Their Use in Experiments to Delineate the Relative Contributions of Cytochrome P4503A4 versus 3A5.

Tseng E, Fate GD, Walker GS, Goosen TC, Obach RS.

Drug Metab Dispos. 2018 May;46(5):493-502. doi: 10.1124/dmd.117.079855. Epub 2018 Feb 23.


Establishing Transcriptional Signatures to Differentiate PXR-, CAR-, and AhR-Mediated Regulation of Drug Metabolism and Transport Genes in Cryopreserved Human Hepatocytes.

Moscovitz JE, Kalgutkar AS, Nulick K, Johnson N, Lin Z, Goosen TC, Weng Y.

J Pharmacol Exp Ther. 2018 May;365(2):262-271. doi: 10.1124/jpet.117.247296. Epub 2018 Feb 12.


Quantitative Characterization of Major Hepatic UDP-Glucuronosyltransferase Enzymes in Human Liver Microsomes: Comparison of Two Proteomic Methods and Correlation with Catalytic Activity.

Achour B, Dantonio A, Niosi M, Novak JJ, Fallon JK, Barber J, Smith PC, Rostami-Hodjegan A, Goosen TC.

Drug Metab Dispos. 2017 Oct;45(10):1102-1112. doi: 10.1124/dmd.117.076703. Epub 2017 Aug 2.


Induction of human cytochrome P450 3A4 by the irreversible myeloperoxidase inactivator PF-06282999 is mediated by the pregnane X receptor.

Moscovitz JE, Lin Z, Johnson N, Tu M, Goosen TC, Weng Y, Kalgutkar AS.

Xenobiotica. 2018 Jul;48(7):647-655. doi: 10.1080/00498254.2017.1353163. Epub 2017 Jul 24.


In Vitro Kinetic Characterization of Axitinib Metabolism.

Zientek MA, Goosen TC, Tseng E, Lin J, Bauman JN, Walker GS, Kang P, Jiang Y, Freiwald S, Neul D, Smith BJ.

Drug Metab Dispos. 2016 Jan;44(1):102-14. doi: 10.1124/dmd.115.065615. Epub 2015 Oct 28.


Discovery and Optimization of Imidazopyridine-Based Inhibitors of Diacylglycerol Acyltransferase 2 (DGAT2).

Futatsugi K, Kung DW, Orr ST, Cabral S, Hepworth D, Aspnes G, Bader S, Bian J, Boehm M, Carpino PA, Coffey SB, Dowling MS, Herr M, Jiao W, Lavergne SY, Li Q, Clark RW, Erion DM, Kou K, Lee K, Pabst BA, Perez SM, Purkal J, Jorgensen CC, Goosen TC, Gosset JR, Niosi M, Pettersen JC, Pfefferkorn JA, Ahn K, Goodwin B.

J Med Chem. 2015 Sep 24;58(18):7173-85. doi: 10.1021/acs.jmedchem.5b01006.


Metabolites in safety testing assessment in early clinical development: a case study with a glucokinase activator.

Sharma R, Litchfield J, Atkinson K, Eng H, Amin NB, Denney WS, Pettersen JC, Goosen TC, Di L, Lee E, Pfefferkorn JA, Dalvie DK, Kalgutkar AS.

Drug Metab Dispos. 2014 Nov;42(11):1926-39. doi: 10.1124/dmd.114.060087. Epub 2014 Aug 20.


Mechanism-based pharmacokinetic modeling to evaluate transporter-enzyme interplay in drug interactions and pharmacogenetics of glyburide.

Varma MV, Scialis RJ, Lin J, Bi YA, Rotter CJ, Goosen TC, Yang X.

AAPS J. 2014 Jul;16(4):736-48. doi: 10.1208/s12248-014-9614-7. Epub 2014 May 17.


Relative contributions of cytochrome CYP3A4 versus CYP3A5 for CYP3A-cleared drugs assessed in vitro using a CYP3A4-selective inactivator (CYP3cide).

Tseng E, Walsky RL, Luzietti RA Jr, Harris JJ, Kosa RE, Goosen TC, Zientek MA, Obach RS.

Drug Metab Dispos. 2014 Jul;42(7):1163-73. doi: 10.1124/dmd.114.057000. Epub 2014 Apr 15.


Undesired versus designed enzymatic cleavage of linkers for liver targeting.

Chirapu SR, Bauman JN, Eng H, Goosen TC, Strelevitz TJ, Sinha SC, Dow RL, Finn MG.

Bioorg Med Chem Lett. 2014 Feb 15;24(4):1144-7. doi: 10.1016/j.bmcl.2013.12.126. Epub 2014 Jan 8.


A perspective on the prediction of drug pharmacokinetics and disposition in drug research and development.

Di L, Feng B, Goosen TC, Lai Y, Steyn SJ, Varma MV, Obach RS.

Drug Metab Dispos. 2013 Dec;41(12):1975-93. doi: 10.1124/dmd.113.054031. Epub 2013 Sep 24.


Targeted quantitative proteomics for the analysis of 14 UGT1As and -2Bs in human liver using NanoUPLC-MS/MS with selected reaction monitoring.

Fallon JK, Neubert H, Hyland R, Goosen TC, Smith PC.

J Proteome Res. 2013 Oct 4;12(10):4402-13. doi: 10.1021/pr4004213. Epub 2013 Sep 26.


Elucidation of the biochemical basis for a clinical drug-drug interaction between atorvastatin and 5-(N-(4-((4-ethylbenzyl)thio)phenyl)sulfamoyl)-2-methyl benzoic acid (CP-778875), a subtype selective agonist of the peroxisome proliferator-activated receptor alpha.

Kalgutkar AS, Chen D, Varma MV, Feng B, Terra SG, Scialis RJ, Rotter CJ, Frederick KS, West MA, Goosen TC, Gosset JR, Walsky RL, Francone OL.

Xenobiotica. 2013 Nov;43(11):963-72. doi: 10.3109/00498254.2013.791004. Epub 2013 Apr 30.


Reactive metabolite trapping studies on imidazo- and 2-methylimidazo[2,1-b]thiazole-based inverse agonists of the ghrelin receptor.

Kalgutkar AS, Ryder TF, Walker GS, Orr ST, Cabral S, Goosen TC, Lapham K, Eng H.

Drug Metab Dispos. 2013 Jul;41(7):1375-88. doi: 10.1124/dmd.113.051839. Epub 2013 Apr 22.


Intestinal targeting of drugs: rational design approaches and challenges.

Filipski KJ, Varma MV, El-Kattan AF, Ambler CM, Ruggeri RB, Goosen TC, Cameron KO.

Curr Top Med Chem. 2013;13(7):776-802. Review.


Response to the comment on the article "physiologically based modeling of pravastatin transporter-mediated hepatobiliary disposition and drug-drug interactions".

Varma MV, Lai Y, Feng B, Litchfield J, Goosen TC, Bergman A.

Pharm Res. 2013 Jun;30(6):1469-70. doi: 10.1007/s11095-013-0987-6. Epub 2013 Mar 6. No abstract available.


Quantitative prediction of repaglinide-rifampicin complex drug interactions using dynamic and static mechanistic models: delineating differential CYP3A4 induction and OATP1B1 inhibition potential of rifampicin.

Varma MV, Lin J, Bi YA, Rotter CJ, Fahmi OA, Lam JL, El-Kattan AF, Goosen TC, Lai Y.

Drug Metab Dispos. 2013 May;41(5):966-74. doi: 10.1124/dmd.112.050583. Epub 2013 Feb 7.


Investigating the enteroenteric recirculation of apixaban, a factor Xa inhibitor: administration of activated charcoal to bile duct-cannulated rats and dogs receiving an intravenous dose and use of drug transporter knockout rats.

Zhang D, Frost CE, He K, Rodrigues AD, Wang X, Wang L, Goosen TC, Humphreys WG.

Drug Metab Dispos. 2013 Apr;41(4):906-15. doi: 10.1124/dmd.112.050575. Epub 2013 Feb 5.


Model-based approaches to predict drug-drug interactions associated with hepatic uptake transporters: preclinical, clinical and beyond.

Barton HA, Lai Y, Goosen TC, Jones HM, El-Kattan AF, Gosset JR, Lin J, Varma MV.

Expert Opin Drug Metab Toxicol. 2013 Apr;9(4):459-72. doi: 10.1517/17425255.2013.759210. Epub 2013 Jan 21. Review.


Mechanistic modeling to predict the transporter- and enzyme-mediated drug-drug interactions of repaglinide.

Varma MV, Lai Y, Kimoto E, Goosen TC, El-Kattan AF, Kumar V.

Pharm Res. 2013 Apr;30(4):1188-99. doi: 10.1007/s11095-012-0956-5. Epub 2013 Jan 10.


Insights into the novel hydrolytic mechanism of a diethyl 2-phenyl-2-(2-arylacetoxy)methyl malonate ester-based microsomal triglyceride transfer protein (MTP) inhibitor.

Ryder T, Walker GS, Goosen TC, Ruggeri RB, Conn EL, Rocke BN, Lapham K, Steppan CM, Hepworth D, Kalgutkar AS.

Chem Res Toxicol. 2012 Oct 15;25(10):2138-52. doi: 10.1021/tx300243v. Epub 2012 Sep 27.


Selective mechanism-based inactivation of CYP3A4 by CYP3cide (PF-04981517) and its utility as an in vitro tool for delineating the relative roles of CYP3A4 versus CYP3A5 in the metabolism of drugs.

Walsky RL, Obach RS, Hyland R, Kang P, Zhou S, West M, Geoghegan KF, Helal CJ, Walker GS, Goosen TC, Zientek MA.

Drug Metab Dispos. 2012 Sep;40(9):1686-97. doi: 10.1124/dmd.112.045302. Epub 2012 May 29.


Physiologically based modeling of pravastatin transporter-mediated hepatobiliary disposition and drug-drug interactions.

Varma MV, Lai Y, Feng B, Litchfield J, Goosen TC, Bergman A.

Pharm Res. 2012 Oct;29(10):2860-73. doi: 10.1007/s11095-012-0792-7. Epub 2012 May 26.


Physicochemical property space of hepatobiliary transport and computational models for predicting rat biliary excretion.

Varma MV, Chang G, Lai Y, Feng B, El-Kattan AF, Litchfield J, Goosen TC.

Drug Metab Dispos. 2012 Aug;40(8):1527-37. doi: 10.1124/dmd.112.044628. Epub 2012 May 11.


Optimized assays for human UDP-glucuronosyltransferase (UGT) activities: altered alamethicin concentration and utility to screen for UGT inhibitors.

Walsky RL, Bauman JN, Bourcier K, Giddens G, Lapham K, Negahban A, Ryder TF, Obach RS, Hyland R, Goosen TC.

Drug Metab Dispos. 2012 May;40(5):1051-65. doi: 10.1124/dmd.111.043117. Epub 2012 Feb 22.


pH-sensitive interaction of HMG-CoA reductase inhibitors (statins) with organic anion transporting polypeptide 2B1.

Varma MV, Rotter CJ, Chupka J, Whalen KM, Duignan DB, Feng B, Litchfield J, Goosen TC, El-Kattan AF.

Mol Pharm. 2011 Aug 1;8(4):1303-13. doi: 10.1021/mp200103h. Epub 2011 Jul 11.


Discovery of novel hepatoselective HMG-CoA reductase inhibitors for treating hypercholesterolemia: a bench-to-bedside case study on tissue selective drug distribution.

Pfefferkorn JA, Litchfield J, Hutchings R, Cheng XM, Larsen SD, Auerbach B, Bush MR, Lee C, Erasga N, Bowles DM, Boyles DC, Lu G, Sekerke C, Askew V, Hanselman JC, Dillon L, Lin Z, Robertson A, Olsen K, Boustany C, Atkinson K, Goosen TC, Sahasrabudhe V, Chupka J, Duignan DB, Feng B, Scialis R, Kimoto E, Bi YA, Lai Y, El-Kattan A, Bakker-Arkema R, Barclay P, Kindt E, Le V, Mandema JW, Milad M, Tait BD, Kennedy R, Trivedi BK, Kowala M.

Bioorg Med Chem Lett. 2011 May 1;21(9):2725-31. doi: 10.1016/j.bmcl.2010.11.103. Epub 2010 Nov 26.


In vitro assessment of metabolic drug-drug interaction potential of apixaban through cytochrome P450 phenotyping, inhibition, and induction studies.

Wang L, Zhang D, Raghavan N, Yao M, Ma L, Frost CE, Maxwell BD, Chen SY, He K, Goosen TC, Humphreys WG, Grossman SJ.

Drug Metab Dispos. 2010 Mar;38(3):448-58. doi: 10.1124/dmd.109.029694. Epub 2009 Nov 25. Erratum in: Drug Metab Dispos. 2010 May;38(5):887. Frost, Charles A [corrected to Frost, Charles E].


Limited influence of UGT1A1*28 and no effect of UGT2B7*2 polymorphisms on UGT1A1 or UGT2B7 activities and protein expression in human liver microsomes.

Peterkin VC, Bauman JN, Goosen TC, Menning L, Man MZ, Paulauskis JD, Williams JA, Myrand SP.

Br J Clin Pharmacol. 2007 Oct;64(4):458-68. Epub 2007 Jun 6.


Atorvastatin glucuronidation is minimally and nonselectively inhibited by the fibrates gemfibrozil, fenofibrate, and fenofibric acid.

Goosen TC, Bauman JN, Davis JA, Yu C, Hurst SI, Williams JA, Loi CM.

Drug Metab Dispos. 2007 Aug;35(8):1315-24. Epub 2007 Apr 30.


Drug-drug interaction after single oral doses of the furanocoumarin methoxsalen and cyclosporine.

Rheeders M, Bouwer M, Goosen TC.

J Clin Pharmacol. 2006 Jul;46(7):768-75.


Kinetics of acetaminophen glucuronidation by UDP-glucuronosyltransferases 1A1, 1A6, 1A9 and 2B15. Potential implications in acetaminophen-induced hepatotoxicity.

Mutlib AE, Goosen TC, Bauman JN, Williams JA, Kulkarni S, Kostrubsky S.

Chem Res Toxicol. 2006 May;19(5):701-9.


Udp-glucuronosyltransferase 2b7 is the major enzyme responsible for gemcabene glucuronidation in human liver microsomes.

Bauman JN, Goosen TC, Tugnait M, Peterkin V, Hurst SI, Menning LC, Milad M, Court MH, Williams JA.

Drug Metab Dispos. 2005 Sep;33(9):1349-54. Epub 2005 Jun 24.


Bergamottin contribution to the grapefruit juice-felodipine interaction and disposition in humans.

Goosen TC, CilliƩ D, Bailey DG, Yu C, He K, Hollenberg PF, Woster PM, Cohen L, Williams JA, Rheeders M, Dijkstra HP.

Clin Pharmacol Ther. 2004 Dec;76(6):607-17.


Drug-drug interactions for UDP-glucuronosyltransferase substrates: a pharmacokinetic explanation for typically observed low exposure (AUCi/AUC) ratios.

Williams JA, Hyland R, Jones BC, Smith DA, Hurst S, Goosen TC, Peterkin V, Koup JR, Ball SE.

Drug Metab Dispos. 2004 Nov;32(11):1201-8. Epub 2004 Aug 10. Review.


Silybin inactivates cytochromes P450 3A4 and 2C9 and inhibits major hepatic glucuronosyltransferases.

Sridar C, Goosen TC, Kent UM, Williams JA, Hollenberg PF.

Drug Metab Dispos. 2004 Jun;32(6):587-94.


Effect of oral contraceptives on the transport of chlorpromazine across the CACO-2 intestinal epithelial cell line.

Brown D, Goosen TC, Chetty M, Hamman JH.

Eur J Pharm Biopharm. 2003 Sep;56(2):159-65.


Chemical stabilities and biological activities of thalidomide and its N-alkyl analogs.

Goosen C, Laing TJ, du Plessis J, Goosen TC, Rao TB, Flynn GL.

Pharm Res. 2002 Aug;19(8):1232-5.


Percutaneous delivery of thalidomide and its N-alkyl analogs.

Goosen C, Laing TJ, du Plessis J, Goosen TC, Lu GW, Flynn GL.

Pharm Res. 2002 Apr;19(4):434-9.


Physicochemical characterization and solubility analysis of thalidomide and its N-alkyl analogs.

Goosen C, Laing TJ, du PJ, Goosen TC, Flynn GL.

Pharm Res. 2002 Jan;19(1):13-9.


Inactivation of cytochrome P450 2B1 by benzyl isothiocyanate, a chemopreventative agent from cruciferous vegetables.

Goosen TC, Kent UM, Brand L, Hollenberg PF.

Chem Res Toxicol. 2000 Dec;13(12):1349-59.


Effects of benzyl isothiocyanate on rat and human cytochromes P450: identification of metabolites formed by P450 2B1.

Goosen TC, Mills DE, Hollenberg PF.

J Pharmacol Exp Ther. 2001 Jan;296(1):198-206.

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