Theunis C Goosen

Theunis C Goosen

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Theunis C Goosen

Theunis C Goosen

Publications by authors named "Theunis C Goosen"

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Physiologically Based Pharmacokinetic Modeling Suggests Limited Drug-Drug Interaction for Fesoterodine When Coadministered With Mirabegron.

J Clin Pharmacol 2019 Nov 14;59(11):1505-1518. Epub 2019 May 14.

Pfizer Inc., New York, NY, USA.

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http://dx.doi.org/10.1002/jcph.1438DOI Listing
November 2019

6-Chloro-5-[4-(1-Hydroxycyclobutyl)Phenyl]-1-Indole-3-Carboxylic Acid is a Highly Selective Substrate for Glucuronidation by UGT1A1, Relative to -Estradiol.

Drug Metab Dispos 2018 12 7;46(12):1836-1846. Epub 2018 Sep 7.

Medicine Design, Pfizer Inc., Groton, Connecticut (K.L., J.L., J.N., C.O., M.N., L.D., T.C.G., S.R., K.R., H.E.); and Medicine Design, Pfizer Inc., Cambridge, Massachusetts (K.O.C., A.S.K.)

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http://dmd.aspetjournals.org/lookup/doi/10.1124/dmd.118.0837
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http://dx.doi.org/10.1124/dmd.118.083709DOI Listing
December 2018

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.

Drug Metab Dispos 2018 Sep 29;46(9):1285-1303. Epub 2018 Jun 29.

Genentech, South San Francisco, California (J.R.K.); Boehringer Ingelheim, Ridgefield, Connecticut (D.R.); Sekisui-XenoTech LLC, Kansas City, Kansas (D.B.B.); Janssen R&D, Spring House, Pennsylvania (S.D.); Vertex Pharmaceuticals, Boston, Massachusetts (C.F., N.H.); Eli Lilly and Company, Indianapolis, Indiana (M.M.); Novartis, East Hanover, New Jersey (H.J.E.); GlaxoSmithKline, King of Prussia, Pennsylvania (L.C.); Amgen Inc., Cambridge, Massachusetts (J.G.D.); Sanofi, Waltham, Massachusetts (M.F.); Pfizer Global Research and Development, Groton, Connecticut (T.C.G.); Eisai, Andover, Massachusetts (Y.A.S.); EMD Serono R&D Institute, Inc., Billerica, Massachusetts (R.L.W.); Corning Life Sciences, Woburn, Massachusetts (G.Z.); and Merck & Co., Inc., Kenilworth, New Jersey (D.T.).

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http://dx.doi.org/10.1124/dmd.118.081927DOI Listing
September 2018

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.

Drug Metab Dispos 2018 06 26;46(6):805-812. Epub 2018 Mar 26.

Centre for Applied Pharmacokinetic Research, Division of Pharmacy and Optometry, University of Manchester, Manchester, United Kingdom (B.A., Z.M.A.-M., A.R.-H., J.B.); Department of Pharmacokinetics, Dynamics, and Metabolism, Pfizer Inc., Groton, Connecticut (A.D., M.N., J.J.N., T.C.G.); and Simcyp Limited (a Certara Company), Blades Enterprise Centre, Sheffield, United Kingdom (A.R.-H.)

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http://dx.doi.org/10.1124/dmd.117.079475DOI Listing
June 2018

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

J Pharmacol Exp Ther 2018 05 12;365(2):262-271. Epub 2018 Feb 12.

Medicine Design, Pfizer Inc., Cambridge, Massachusetts (J.E.M., A.S.K., Y.W.), and Medicine Design, Pfizer Inc., Groton, Connecticut (K.N., N.J., Z.L., T.C.G.)

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http://dx.doi.org/10.1124/jpet.117.247296DOI Listing
May 2018

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

Drug Metab Dispos 2017 10 2;45(10):1102-1112. Epub 2017 Aug 2.

Centre for Applied Pharmacokinetic Research, Division of Pharmacy and Optometry, University of Manchester, Manchester, United Kingdom (B.A., J.B., A.R.-H.); Division of Pharmacoengineering and Molecular Pharmaceutics, Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina (J.K.F., P.C.S.); Department of Pharmacokinetics, Dynamics, and Metabolism, Pfizer Inc., Groton, Connecticut (A.D., M.N., J.J.N., T.C.G.); and Simcyp Limited (a Certara Company), Blades Enterprise Centre, Sheffield, United Kingdom (A.R.-H.)

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http://dx.doi.org/10.1124/dmd.117.076703DOI Listing
October 2017

In Vitro Kinetic Characterization of Axitinib Metabolism.

Drug Metab Dispos 2016 Jan 28;44(1):102-14. Epub 2015 Oct 28.

Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, Pfizer Inc., San Diego, California (M.A.Z, P.K., Y.J, S.F., D.N, B.J.S.); and Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, Pfizer Inc., Groton, Connecticut (T.C.G., E.T., J.L., J.N.B, G.S.W.).

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http://dx.doi.org/10.1124/dmd.115.065615DOI Listing
January 2016

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

Drug Metab Dispos 2014 11 20;42(11):1926-39. Epub 2014 Aug 20.

Pfizer Inc., Groton, Connecticut (R.S., K.A., H.E., J.C.P., T.C.G., L.D.), San Diego, California (D.K.D.), and Cambridge, Massachusetts (J.L., N.B.A., W.S.D., E.L., J.A.P., A.S.K.)

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http://dx.doi.org/10.1124/dmd.114.060087DOI Listing
November 2014

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

Drug Metab Dispos 2014 Jul 15;42(7):1163-73. Epub 2014 Apr 15.

Pfizer Inc., Groton, Connecticut (E.T., R.E.K., T.C.G,. R.S.O.) and La Jolla, California (M.A.Z.), and AstraZeneca, Waltham, Massachusetts (R.L.W., R.A.L., J.J.H.)

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http://dx.doi.org/10.1124/dmd.114.057000DOI Listing
July 2014

Intestinal targeting of drugs: rational design approaches and challenges.

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

Cardiovascular, Metabolic, and Endocrine Diseases Chemistry, Pfizer Worldwide Research and Development, Cambridge, MA 02139, USA.

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http://dx.doi.org/10.2174/1568026611313070002DOI Listing
April 2014

Undesired versus designed enzymatic cleavage of linkers for liver targeting.

Bioorg Med Chem Lett 2014 Feb 8;24(4):1144-7. Epub 2014 Jan 8.

Department of Chemistry, The Scripps Research Institute, 10550 N. Torrey Pines Rd., La Jolla, CA 92037, USA. Electronic address:

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http://dx.doi.org/10.1016/j.bmcl.2013.12.126DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4319531PMC
February 2014

Targeted precise quantification of 12 human recombinant uridine-diphosphate glucuronosyl transferase 1A and 2B isoforms using nano-ultra-high-performance liquid chromatography/tandem mass spectrometry with selected reaction monitoring.

Drug Metab Dispos 2013 Dec 17;41(12):2076-80. Epub 2013 Sep 17.

Division of Molecular Pharmaceutics, Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina (J.K.F., P.C.S.); and Department. of Pharmacokinetics, Dynamics, and Metabolism, Pfizer Inc., Andover, Massachusetts, (H.N.) and Groton, Connecticut, (T.C.G.).

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http://dx.doi.org/10.1124/dmd.113.053801DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3834135PMC
December 2013

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

Drug Metab Dispos 2013 Dec 24;41(12):1975-93. Epub 2013 Sep 24.

Pfizer Inc., Groton, Connecticut.

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http://dx.doi.org/10.1124/dmd.113.054031DOI Listing
December 2013

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

J Proteome Res 2013 Oct 26;12(10):4402-13. Epub 2013 Sep 26.

Division of Molecular Pharmaceutics, Eshelman School of Pharmacy, University of North Carolina at Chapel Hill , Chapel Hill, North Carolina 27599, United States.

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http://dx.doi.org/10.1021/pr4004213DOI Listing
October 2013

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

Drug Metab Dispos 2013 Jul 22;41(7):1375-88. Epub 2013 Apr 22.

Pharmacokinetics, Dynamics, and Metabolism-New Chemical Entities, Pfizer Worldwide Research and Development, Cambridge, MA 02139, USA.

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http://dx.doi.org/10.1124/dmd.113.051839DOI Listing
July 2013

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

Drug Metab Dispos 2013 May 7;41(5):966-74. Epub 2013 Feb 7.

Department of Pharmacokinetics, Dynamics, and Metabolism, MS 8220-2451, Pfizer World Wide Research and Development, Pfizer Inc., Groton, CT 06340, USA.

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http://dx.doi.org/10.1124/dmd.112.050583DOI Listing
May 2013

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

Pharm Res 2013 Apr 10;30(4):1188-99. Epub 2013 Jan 10.

Pharmacokinetcis, Dynamics and Metabolism, Pfizer Inc., Groton, Connecticut, USA.

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http://dx.doi.org/10.1007/s11095-012-0956-5DOI Listing
April 2013

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

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

Pfizer Worldwide Research and Development, Department of Pharmacokinetics, Dynamics and Metabolism, Eastern Point Road, Groton, CT 06340, USA.

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http://dx.doi.org/10.1517/17425255.2013.759210DOI Listing
April 2013

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

Pharm Res 2012 Oct 26;29(10):2860-73. Epub 2012 May 26.

Pharmacokinetcis, Dynamics and Metabolism, Pfizer Inc., Groton, Connecticut, USA.

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http://dx.doi.org/10.1007/s11095-012-0792-7DOI Listing
October 2012

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

Chem Res Toxicol 2012 Oct 27;25(10):2138-52. Epub 2012 Sep 27.

Pharmacokinetics, Dynamics, and Metabolism-New Chemical Entities, Pfizer Worldwide Research and Development, Groton, Connecticut 06340, USA.

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http://dx.doi.org/10.1021/tx300243vDOI Listing
October 2012

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

Drug Metab Dispos 2012 Aug 11;40(8):1527-37. Epub 2012 May 11.

Department of Pharmacokinetics, Dynamics, and Metabolism, MS 8220-2451, Pfizer World Wide Research and Development, Pfizer, Inc., Groton, CT 06340, USA.

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http://dx.doi.org/10.1124/dmd.112.044628DOI Listing
August 2012

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

Drug Metab Dispos 2012 May 22;40(5):1051-65. Epub 2012 Feb 22.

Department of Pharmacokinetics, Dynamics, and Metabolism, Pfizer Inc., Groton, Connecticut 06340, USA.

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http://dx.doi.org/10.1124/dmd.111.043117DOI Listing
May 2012

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

Mol Pharm 2011 Aug 11;8(4):1303-13. Epub 2011 Jul 11.

Pharmacokinetics Dynamics and Metabolism, Pfizer Global Research and Development, Pfizer Inc., Groton, Connecticut 06340, USA.

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http://dx.doi.org/10.1021/mp200103hDOI Listing
August 2011

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

Drug Metab Dispos 2010 Mar 25;38(3):448-58. Epub 2009 Nov 25.

Pharmaceutical Candidate Optimization, Bristol-Myers Squibb Research and Development, Princeton, New Jersey 08543, USA.

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http://dx.doi.org/10.1124/dmd.109.029694DOI Listing
March 2010

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

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

Department of Pharmacokinetics, Dynamics and Metabolism, Pfizer Global Research and Development, Ann Arbor, MI 48105, USA.

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http://dx.doi.org/10.1111/j.1365-2125.2007.02923.xDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2048551PMC
October 2007

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

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

Department of Pharmacokinetics, Dynamics and Metabolism, Pfizer Global Research and Development, 2800 Plymouth Rd., Ann Arbor, MI 48105, USA.

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http://dx.doi.org/10.1124/dmd.107.015230DOI Listing
August 2007

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

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

Department of Pharmacology, North-West University, South Africa.

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http://dx.doi.org/10.1177/0091270006288732DOI Listing
July 2006

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

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

Department of Pharmacokinetics, Pfizer Inc., 2800 Plymouth Road, Ann Arbor, Michigan 48105, USA.

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http://dx.doi.org/10.1021/tx050317iDOI Listing
May 2006

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

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

Department of Pharmacokinetics, Dynamics and Metabolism, Pfizer Global Research and Development, Ann Arbor, MI 48105, USA.

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http://dx.doi.org/10.1124/dmd.105.005108DOI Listing
September 2005

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

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

Pharmacokinetics, Dynamics and Metabolism, Pfizer Global Research and Development, 2800 Plymouth Road, Ann Arbor, MI 48105, USA.

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http://dx.doi.org/10.1124/dmd.104.000794DOI Listing
November 2004

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

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

Department of Pharmacology, The University of Michigan, Ann Arbor, MI 48109, USA.

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http://dx.doi.org/10.1124/dmd.32.6.587DOI Listing
June 2004

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

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

School of Pharmacy, Technikon Pretoria, Pretoria, South Africa.

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http://dx.doi.org/10.1016/s0939-6411(03)00110-3DOI Listing
September 2003

Percutaneous delivery of thalidomide and its N-alkyl analogs.

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

Department of Pharmaceutics, School of Pharmacy, Potchefstroom University for Christian Higher Education, Republic of South Africa.

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http://dx.doi.org/10.1023/a:1015183310000DOI Listing
April 2002

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

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

Department of Pharmaceutics, School of Pharmacy, Potchefstroom, University for Christian Higher Education, Republic of South Africa.

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http://dx.doi.org/10.1023/a:1013643013244DOI Listing
January 2002