Sort by
Items per page

Send to

Choose Destination

Search results

Items: 1 to 50 of 51


Transporters in Drug Development: 2018 ITC Recommendations for Transporters of Emerging Clinical Importance.

Zamek-Gliszczynski MJ, Taub ME, Chothe PP, Chu X, Giacomini KM, Kim RB, Ray AS, Stocker SL, Unadkat JD, Wittwer MB, Xia C, Yee SW, Zhang L, Zhang Y; International Transporter Consortium.

Clin Pharmacol Ther. 2018 Aug 8. doi: 10.1002/cpt.1112. [Epub ahead of print] Review.


ITC Commentary on Metformin Clinical Drug-Drug Interaction Study Design That Enables an Efficacy- and Safety-Based Dose Adjustment Decision.

Zamek-Gliszczynski MJ, Chu X, Cook JA, Custodio JM, Galetin A, Giacomini KM, Lee CA, Paine MF, Ray AS, Ware JA, Wittwer MB, Zhang L; International Transporter Consortium.

Clin Pharmacol Ther. 2018 May 15. doi: 10.1002/cpt.1082. [Epub ahead of print]


Hepatobiliary Disposition of Atovaquone: A Case of Mechanistically Unusual Biliary Clearance.

Patel M, Johnson M, Sychterz CJ, Lewis GJ, Watson C, Ellens H, Polli JW, Zamek-Gliszczynski MJ.

J Pharmacol Exp Ther. 2018 Jul;366(1):37-45. doi: 10.1124/jpet.117.247254. Epub 2018 Apr 13.


Emerging Clinical Importance of Hepatic Organic Cation Transporter 1 (OCT1) in Drug Pharmacokinetics, Dynamics, Pharmacogenetic Variability, and Drug Interactions.

Zamek-Gliszczynski MJ, Giacomini KM, Zhang L.

Clin Pharmacol Ther. 2018 May;103(5):758-760. doi: 10.1002/cpt.941. Epub 2017 Nov 28.


Industry Perspective on Contemporary Protein-Binding Methodologies: Considerations for Regulatory Drug-Drug Interaction and Related Guidelines on Highly Bound Drugs.

Di L, Breen C, Chambers R, Eckley ST, Fricke R, Ghosh A, Harradine P, Kalvass JC, Ho S, Lee CA, Marathe P, Perkins EJ, Qian M, Tse S, Yan Z, Zamek-Gliszczynski MJ.

J Pharm Sci. 2017 Dec;106(12):3442-3452. doi: 10.1016/j.xphs.2017.09.005. Epub 2017 Sep 18. Review.


Importance of Hepatic Transporters in Clinical Disposition of Drugs and Their Metabolites.

Patel M, Taskar KS, Zamek-Gliszczynski MJ.

J Clin Pharmacol. 2016 Jul;56 Suppl 7:S23-39. doi: 10.1002/jcph.671. Review.


The Effect of Dolutegravir on the Pharmacokinetics of Metformin in Healthy Subjects.

Song IH, Zong J, Borland J, Jerva F, Wynne B, Zamek-Gliszczynski MJ, Humphreys JE, Bowers GD, Choukour M.

J Acquir Immune Defic Syndr. 2016 Aug 1;72(4):400-7. doi: 10.1097/QAI.0000000000000983.


Glucose and lipid effects of the ileal apical sodium-dependent bile acid transporter inhibitor GSK2330672: double-blind randomized trials with type 2 diabetes subjects taking metformin.

Nunez DJ, Yao X, Lin J, Walker A, Zuo P, Webster L, Krug-Gourley S, Zamek-Gliszczynski MJ, Gillmor DS, Johnson SL.

Diabetes Obes Metab. 2016 Jul;18(7):654-62. doi: 10.1111/dom.12656. Epub 2016 Apr 21.


A first-in-human phase I study of the oral Notch inhibitor, LY900009, in patients with advanced cancer.

Pant S, Jones SF, Kurkjian CD, Infante JR, Moore KN, Burris HA, McMeekin DS, Benhadji KA, Patel BKR, Frenzel MJ, Kursar JD, Zamek-Gliszczynski MJ, Yuen ESM, Chan EM, Bendell JC.

Eur J Cancer. 2016 Mar;56:1-9. doi: 10.1016/j.ejca.2015.11.021. Epub 2016 Jan 19.


A first-in-human phase I dose-escalation, pharmacokinetic, and pharmacodynamic evaluation of intravenous LY2090314, a glycogen synthase kinase 3 inhibitor, administered in combination with pemetrexed and carboplatin.

Gray JE, Infante JR, Brail LH, Simon GR, Cooksey JF, Jones SF, Farrington DL, Yeo A, Jackson KA, Chow KH, Zamek-Gliszczynski MJ, Burris HA 3rd.

Invest New Drugs. 2015 Dec;33(6):1187-96. doi: 10.1007/s10637-015-0278-7. Epub 2015 Sep 25.


Metformin's Intrinsic Blood-to-Plasma Partition Ratio (B/P): Reconciling the Perceived High In Vivo B/P > 10 with the In Vitro Equilibrium Value of Unity.

Xie F, Ke AB, Bowers GD, Zamek-Gliszczynski MJ.

J Pharmacol Exp Ther. 2015 Aug;354(2):225-9. doi: 10.1124/jpet.115.225698. Epub 2015 Jun 10.


Breast cancer resistance protein (ABCG2) in clinical pharmacokinetics and drug interactions: practical recommendations for clinical victim and perpetrator drug-drug interaction study design.

Lee CA, O'Connor MA, Ritchie TK, Galetin A, Cook JA, Ragueneau-Majlessi I, Ellens H, Feng B, Taub ME, Paine MF, Polli JW, Ware JA, Zamek-Gliszczynski MJ.

Drug Metab Dispos. 2015 Apr;43(4):490-509. doi: 10.1124/dmd.114.062174. Epub 2015 Jan 13. Review.


Identification of LY2510924, a novel cyclic peptide CXCR4 antagonist that exhibits antitumor activities in solid tumor and breast cancer metastatic models.

Peng SB, Zhang X, Paul D, Kays LM, Gough W, Stewart J, Uhlik MT, Chen Q, Hui YH, Zamek-Gliszczynski MJ, Wijsman JA, Credille KM, Yan LZ.

Mol Cancer Ther. 2015 Feb;14(2):480-90. doi: 10.1158/1535-7163.MCT-14-0850. Epub 2014 Dec 12.


Breast cancer resistance protein substrate and inhibition evaluation: why, when, and how?

Ware JA, Urquhart BL, Sugiyama Y, Zamek-Gliszczynski MJ.

Drug Metab Dispos. 2014 Dec;42(12):1979-80. doi: 10.1124/dmd.114.060970. No abstract available.


ITC commentary on the prediction of digoxin clinical drug-drug interactions from in vitro transporter assays.

Lee CA, Kalvass JC, Galetin A, Zamek-Gliszczynski MJ.

Clin Pharmacol Ther. 2014 Sep;96(3):298-301. doi: 10.1038/clpt.2014.94.


Itraconazole and clarithromycin as ketoconazole alternatives for clinical CYP3A inhibition studies.

Ke AB, Zamek-Gliszczynski MJ, Higgins JW, Hall SD.

Clin Pharmacol Ther. 2014 May;95(5):473-6. doi: 10.1038/clpt.2014.41.


Understanding the transport properties of metabolites: case studies and considerations for drug development.

Zamek-Gliszczynski MJ, Chu X, Polli JW, Paine MF, Galetin A.

Drug Metab Dispos. 2014 Apr;42(4):650-64. doi: 10.1124/dmd.113.055558. Epub 2013 Dec 17. Review.


Utility of Oatp1a/1b-knockout and OATP1B1/3-humanized mice in the study of OATP-mediated pharmacokinetics and tissue distribution: case studies with pravastatin, atorvastatin, simvastatin, and carboxydichlorofluorescein.

Higgins JW, Bao JQ, Ke AB, Manro JR, Fallon JK, Smith PC, Zamek-Gliszczynski MJ.

Drug Metab Dispos. 2014 Jan;42(1):182-92. doi: 10.1124/dmd.113.054783. Epub 2013 Nov 5.


Metformin sinusoidal efflux from the liver is consistent with negligible biliary excretion and absence of enterohepatic cycling.

Zamek-Gliszczynski MJ, Bao JQ, Day JS, Higgins JW.

Drug Metab Dispos. 2013 Nov;41(11):1967-71. doi: 10.1124/dmd.113.053025. Epub 2013 Sep 5.


ITC recommendations for transporter kinetic parameter estimation and translational modeling of transport-mediated PK and DDIs in humans.

Zamek-Gliszczynski MJ, Lee CA, Poirier A, Bentz J, Chu X, Ellens H, Ishikawa T, Jamei M, Kalvass JC, Nagar S, Pang KS, Korzekwa K, Swaan PW, Taub ME, Zhao P, Galetin A; International Transporter Consortium.

Clin Pharmacol Ther. 2013 Jul;94(1):64-79. doi: 10.1038/clpt.2013.45. Epub 2013 Feb 25. Review.


Why clinical modulation of efflux transport at the human blood-brain barrier is unlikely: the ITC evidence-based position.

Kalvass JC, Polli JW, Bourdet DL, Feng B, Huang SM, Liu X, Smith QR, Zhang LK, Zamek-Gliszczynski MJ; International Transporter Consortium.

Clin Pharmacol Ther. 2013 Jul;94(1):80-94. doi: 10.1038/clpt.2013.34. Epub 2013 Feb 14. Review.


Minor compensatory changes in SAGE Mdr1a (P-gp), Bcrp, and Mrp2 knockout rats do not detract from their utility in the study of transporter-mediated pharmacokinetics.

Zamek-Gliszczynski MJ, Goldstein KM, Paulman A, Baker TK, Ryan TP.

Drug Metab Dispos. 2013 Jun;41(6):1174-8. doi: 10.1124/dmd.113.051409. Epub 2013 Apr 8.


Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure.

Zamek-Gliszczynski MJ, Abraham TL, Alberts JJ, Kulanthaivel P, Jackson KA, Chow KH, McCann DJ, Hu H, Anderson S, Furr NA, Barbuch RJ, Cassidy KC.

Drug Metab Dispos. 2013 Apr;41(4):714-26. doi: 10.1124/dmd.112.048488. Epub 2013 Jan 10.


Highlights from the International Transporter Consortium second workshop.

Zamek-Gliszczynski MJ, Hoffmaster KA, Tweedie DJ, Giacomini KM, Hillgren KM.

Clin Pharmacol Ther. 2012 Nov;92(5):553-6. doi: 10.1038/clpt.2012.126.


Characterization of SAGE Mdr1a (P-gp), Bcrp, and Mrp2 knockout rats using loperamide, paclitaxel, sulfasalazine, and carboxydichlorofluorescein pharmacokinetics.

Zamek-Gliszczynski MJ, Bedwell DW, Bao JQ, Higgins JW.

Drug Metab Dispos. 2012 Sep;40(9):1825-33. doi: 10.1124/dmd.112.046508. Epub 2012 Jun 18.


Ablation of both organic cation transporter (OCT)1 and OCT2 alters metformin pharmacokinetics but has no effect on tissue drug exposure and pharmacodynamics.

Higgins JW, Bedwell DW, Zamek-Gliszczynski MJ.

Drug Metab Dispos. 2012 Jun;40(6):1170-7. doi: 10.1124/dmd.112.044875. Epub 2012 Mar 9.


How well do lipophilicity parameters, MEEKC microemulsion capacity factor, and plasma protein binding predict CNS tissue binding?

Zamek-Gliszczynski MJ, Sprague KE, Espada A, Raub TJ, Morton SM, Manro JR, Molina-Martin M.

J Pharm Sci. 2012 May;101(5):1932-40. doi: 10.1002/jps.23081. Epub 2012 Feb 17.


Efflux transport is an important determinant of ethinylestradiol glucuronide and ethinylestradiol sulfate pharmacokinetics.

Zamek-Gliszczynski MJ, Day JS, Hillgren KM, Phillips DL.

Drug Metab Dispos. 2011 Oct;39(10):1794-800. doi: 10.1124/dmd.111.040162. Epub 2011 Jun 27.


Validation of 96-well equilibrium dialysis with non-radiolabeled drug for definitive measurement of protein binding and application to clinical development of highly-bound drugs.

Zamek-Gliszczynski MJ, Ruterbories KJ, Ajamie RT, Wickremsinhe ER, Pothuri L, Rao MV, Basavanakatti VN, Pinjari J, Ramanathan VK, Chaudhary AK.

J Pharm Sci. 2011 Jun;100(6):2498-507. doi: 10.1002/jps.22452. Epub 2011 Jan 6.


Membrane transporters in drug development.

International Transporter Consortium, Giacomini KM, Huang SM, Tweedie DJ, Benet LZ, Brouwer KL, Chu X, Dahlin A, Evers R, Fischer V, Hillgren KM, Hoffmaster KA, Ishikawa T, Keppler D, Kim RB, Lee CA, Niemi M, Polli JW, Sugiyama Y, Swaan PW, Ware JA, Wright SH, Yee SW, Zamek-Gliszczynski MJ, Zhang L.

Nat Rev Drug Discov. 2010 Mar;9(3):215-36. doi: 10.1038/nrd3028. Review.


Relationship between drug/metabolite exposure and impairment of excretory transport function.

Zamek-Gliszczynski MJ, Kalvass JC, Pollack GM, Brouwer KL.

Drug Metab Dispos. 2009 Feb;37(2):386-90. doi: 10.1124/dmd.108.023648. Epub 2008 Nov 20.


Apparent differences in mechanisms of harmol sulfate biliary excretion in mice and rats.

Zamek-Gliszczynski MJ, Hoffmaster KA, Nezasa K, Brouwer KL.

Drug Metab Dispos. 2008 Nov;36(11):2156-8. doi: 10.1124/dmd.108.022053. Epub 2008 Aug 21.


Impact of basolateral multidrug resistance-associated protein (Mrp) 3 and Mrp4 on the hepatobiliary disposition of fexofenadine in perfused mouse livers.

Tian X, Swift B, Zamek-Gliszczynski MJ, Belinsky MG, Kruh GD, Brouwer KL.

Drug Metab Dispos. 2008 May;36(5):911-5. doi: 10.1124/dmd.107.019273. Epub 2008 Feb 14.


Modulation of trabectedin (ET-743) hepatobiliary disposition by multidrug resistance-associated proteins (Mrps) may prevent hepatotoxicity.

Lee JK, Leslie EM, Zamek-Gliszczynski MJ, Brouwer KL.

Toxicol Appl Pharmacol. 2008 Apr 1;228(1):17-23. doi: 10.1016/j.taap.2007.11.020. Epub 2007 Dec 3.


Multidrug resistance-associated protein 2 is primarily responsible for the biliary excretion of fexofenadine in mice.

Tian X, Zamek-Gliszczynski MJ, Li J, Bridges AS, Nezasa K, Patel NJ, Raub TJ, Brouwer KL.

Drug Metab Dispos. 2008 Jan;36(1):61-4. Epub 2007 Oct 3.


Roles of P-glycoprotein, Bcrp, and Mrp2 in biliary excretion of spiramycin in mice.

Tian X, Li J, Zamek-Gliszczynski MJ, Bridges AS, Zhang P, Patel NJ, Raub TJ, Pollack GM, Brouwer KL.

Antimicrob Agents Chemother. 2007 Sep;51(9):3230-4. Epub 2007 Jun 18.


The important role of Bcrp (Abcg2) in the biliary excretion of sulfate and glucuronide metabolites of acetaminophen, 4-methylumbelliferone, and harmol in mice.

Zamek-Gliszczynski MJ, Nezasa K, Tian X, Kalvass JC, Patel NJ, Raub TJ, Brouwer KL.

Mol Pharmacol. 2006 Dec;70(6):2127-33. Epub 2006 Sep 7.


Differential involvement of Mrp2 (Abcc2) and Bcrp (Abcg2) in biliary excretion of 4-methylumbelliferyl glucuronide and sulfate in the rat.

Zamek-Gliszczynski MJ, Hoffmaster KA, Humphreys JE, Tian X, Nezasa K, Brouwer KL.

J Pharmacol Exp Ther. 2006 Oct;319(1):459-67. Epub 2006 Jul 20.


Integration of hepatic drug transporters and phase II metabolizing enzymes: mechanisms of hepatic excretion of sulfate, glucuronide, and glutathione metabolites.

Zamek-Gliszczynski MJ, Hoffmaster KA, Nezasa K, Tallman MN, Brouwer KL.

Eur J Pharm Sci. 2006 Apr;27(5):447-86. Epub 2006 Feb 10. Review.


Altered hepatobiliary disposition of 5 (and 6)-carboxy-2',7'-dichlorofluorescein in Abcg2 (Bcrp1) and Abcc2 (Mrp2) knockout mice.

Nezasa K, Tian X, Zamek-Gliszczynski MJ, Patel NJ, Raub TJ, Brouwer KL.

Drug Metab Dispos. 2006 Apr;34(4):718-23. Epub 2006 Jan 24.


Knocking down transport: applications of RNA interference in the study of drug transport proteins.

Tian X, Zhang P, Zamek-Gliszczynski MJ, Brouwer KL.

Drug Metab Rev. 2005;37(4):705-23. Review.


Multiple mechanisms are involved in the biliary excretion of acetaminophen sulfate in the rat: role of Mrp2 and Bcrp1.

Zamek-Gliszczynski MJ, Hoffmaster KA, Tian X, Zhao R, Polli JW, Humphreys JE, Webster LO, Bridges AS, Kalvass JC, Brouwer KL.

Drug Metab Dispos. 2005 Aug;33(8):1158-65. Epub 2005 Apr 28.


Multiple transport systems mediate the hepatic uptake and biliary excretion of the metabolically stable opioid peptide [D-penicillamine2,5]enkephalin.

Hoffmaster KA, Zamek-Gliszczynski MJ, Pollack GM, Brouwer KL.

Drug Metab Dispos. 2005 Feb;33(2):287-93. Epub 2004 Nov 4.


Xenobiotics inhibit hepatic uptake and biliary excretion of taurocholate in rat hepatocytes.

Kemp DC, Zamek-Gliszczynski MJ, Brouwer KL.

Toxicol Sci. 2005 Feb;83(2):207-14. Epub 2004 Oct 27.


Phenobarbital alters hepatic Mrp2 function by direct and indirect interactions.

Patel NJ, Zamek-Gliszczynski MJ, Zhang P, Han YH, Jansen PL, Meier PJ, Stieger B, Brouwer KL.

Mol Pharmacol. 2003 Jul;64(1):154-9.

Supplemental Content

Loading ...
Support Center