Maciej ZAMEK-GLISZCZYŃSKI (GlaxoSmithKline) SITE

  • Anal Chem. 2020;92:11851-11859. Direct automated MALDI Mass Spectrometry analysis of cellular transporter function: Inhibition of OATP2B1 uptake by 294 drugs. Unger MS, Schumacher L, Enzlein T, Weigt D, Zamek-Gliszczynski MJ, Schwab M, Nies AT, Drewes G, Schulz S, Reinhard FBM, Hopf C. PubMed
  • Clin Pharmacol Ther. 2020;In press.  Intestinal P-gp and putative hepatic OATP1B induction: International Transporter Consortium perspective on drug development implications. Zamek-Gliszczynski MJ, Patel M, Yang X, Lutz JD, Chu X, Brouwer KLR, Lai Y, Lee CA, Neuhoff S, Paine MF, Sugiyama Y, Taskar KS, Galetin A. PubMed
  • Mol Pharm. 2020;17:488-498. Clinically-relevant OATP2B1 inhibitors in marketed drug space. Unger MS, Mudunuru J, Schwab M, Hopf C, Drewes G, Nies AT, Zamek-Gliszczynski MJ, Reinhard F. PubMed
  • J Pharmacol Exp Ther. 2019;370:269-277. Mechanistic basis of cabotegravir-glucuronide disposition in humans. Patel M, Eberl HC, Wolf A, Pierre E, Polli JW, Zamek-Gliszczynski MJ. PubMed
  • Drug Metab Dispos. 2019;47:890-898. Clinical extrapolation of the effects of Dolutegravir and other HIV integrase inhibitors on folate transport pathways. Zamek-Gliszczynski MJ, Zhang X, Mudunuru J, Du Y, Chen JL, Taskar KS, Huang J, Huang Y, Romach EH. PubMed
  • Clin Pharmacol Ther. 2018;104:836-864. Clinical probes and endogenous biomarkers as substrates for transporter drug-drug interaction evaluation: Perspectives from the International Transporter Consortium. Chu X, Liao M, Shen H, Yoshida K, Zur AA, Arya V, Galetin A, Giacomini KM, Hanna I, Kusuhara H, Lai Y, Rodrigues D, Sugiyama Y, Zamek-Gliszczynski MJ, Zhang L; International Transporter Consortium. PubMed
  • Clin Pharmacol Ther. 2018;104:788-792. Dabigatran Etexilate and Digoxin: Comparison as clinical probe substrates for evaluation of P-gp inhibition. Chu X, Galetin A, Zamek-Gliszczynski MJ, Zhang L, Tweedie DJ; International Transporter Consortium. PubMed
  • Clin Pharmacol Ther. 2018;104:890-899. 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. PubMed
  • Clin Pharmacol Ther. 2018;104:781-784. 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. PubMed
  • J Pharmacol Exp Ther. 2018;366:37-45. 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. PubMed
  • Clin Pharmacol Ther. 2018;103:758-760. Emerging clinical importance of hepatic Organic Cation Transporter 1 (OCT1) in drug pharmacokinetics, dynamics, pharmacogenetic variability, and drug Interactions. Zamek-Gliszczynski MJ, Giacomini KM2, Zhang L. PubMed
  • J Pharm Sci. 2017;106:3442-3452. 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. PubMed
  • J Clin Pharmacol. 2016;56 Suppl 7:S23-39. Importance of hepatic transporters in clinical disposition of drugs and their metabolites.  Patel M, Taskar KS, Zamek-Gliszczynski MJ. PubMed
  • J Acquir Immune Defic Syndr. 2016;72:400-7. 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. PubMed
  • Diabetes Obes Metab. 2016;18:654-62. 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. PubMed
  • J Pharmacol Exp Ther. 2015;354:225-9. 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. PubMed
  • Drug Metab Dispos. 2014;42:1979-80. Breast cancer resistance protein substrate and inhibition evaluation: why, when, and how? Ware JA, Urquhart BL, Sugiyama Y, Zamek-Gliszczynski MJ. PubMed
  • Drug Metab Dispos. 2014;42:1780-4. Clinical CYP3A inhibitor alternatives to ketoconazole, clarithromycin and itraconazole, are not transported into the liver by hepatic organic anion transporting polypeptides and organic cation transporter 1. Higgins JW, Ke AB, Zamek-Gliszczynski MJ. PubMed
  • Clin Pharmacol Ther. 2014;95:473-6. Itraconazole and clarithromycin as ketoconazole alternatives for clinical CYP3A inhibition studies. Ke AB, Zamek-Gliszczynski MJ, Higgins JW, Hall SD. PubMed
  • Drug Metab Dispos. 2014;42:650-64. Understanding the transport properties of metabolites: case studies and considerations for drug development. Zamek-Gliszczynski MJ, Chu X, Polli JW, Paine MF, Galetin A. PubMed
  • Drug Metab Dispos. 2014;42:182-92. 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. PubMed
  • Drug Metab Dispos. 2013;41:1967-71. 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. PubMed
  • Clin Pharmacol Ther. 2013;94:64-79. 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. PubMed
  • Clin Pharmacol Ther. 2013;94:80-94. 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. PubMed
  • Drug Metab Dispos. 2013;41:1174-8. 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. PubMed
  • Clin Pharmacol Ther. 2012;92:553-6. Highlights from the International Transporter Consortium second workshop. Zamek-Gliszczynski MJ, Hoffmaster KA, Tweedie DJ, Giacomini KM, Hillgren KM. PubMed
  • Drug Metab Dispos. 2012;40:1825-33. 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. PubMed
  • Drug Metab Dispos. 2012;40:1170-7. 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. PubMed
  • Drug Metab Dispos. 2011;39:1794-800. Efflux transport is an important determinant of ethinylestradiol glucuronide and ethinylestradiol sulfate pharmacokinetics. Zamek-Gliszczynski MJ, Day JS, Hillgren KM, Phillips DL. PubMed
  • J Pharm Sci. 2011;100:2498-507. 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. PubMed
  • Nat Rev Drug Discov. 2010;9:215-36. 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. PubMed
  • Drug Metab Dispos. 2009;37:386-90. Relationship between drug/metabolite exposure and impairment of excretory transport function. Zamek-Gliszczynski MJ, Kalvass JC, Pollack GM, Brouwer KL. PubMed
  • Drug Metab Dispos. 2008;36:2156-8. Apparent differences in mechanisms of harmol sulfate biliary excretion in mice and rats.  Zamek-Gliszczynski MJ, Hoffmaster KA, Nezasa K, Brouwer KL. PubMed
  • Drug Metab Dispos. 2008;36:911-5. 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. PubMed
  • Toxicol Appl Pharmacol. 2008;228:17-23. 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. PubMed
  • Antimicrob Agents Chemother. 2007;51:3230-4.  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. PubMed
  • J Pharmacol Exp Ther. 2006;319:1485-91. Evaluation of the role of multidrug resistance-associated protein (Mrp) 3 and Mrp4 in hepatic basolateral excretion of sulfate and glucuronide metabolites of acetaminophen, 4-methylumbelliferone, and harmol in Abcc3-/- and Abcc4-/- mice. Zamek-Gliszczynski MJ, Nezasa K, Tian X, Bridges AS, Lee K, Belinsky MG, Kruh GD, Brouwer KL. PubMed
  • Mol Pharmacol. 2006;70:2127-33. 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. PubMed
  • J Pharmacol Exp Ther. 2006;319:459-67. 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. PubMed
  • Eur J Pharm Sci. 2006;27:447-86. 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. PubMed
  • Drug Metab Dispos. 2006;34:718-23. 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. PubMed
  • Drug Metab Rev. 2005;37:705-23. Knocking down transport: applications of RNA interference in the study of drug transport proteins. Tian X, Zhang P, Zamek-Gliszczynski MJ, Brouwer KL. PubMed
  • Drug Metab Dispos. 2005;33:1158-65. 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. PubMed
  • Drug Metab Dispos. 2005;33:287-93. 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. PubMed
  • Toxicol Sci. 2005;83:207-14. Xenobiotics inhibit hepatic uptake and biliary excretion of taurocholate in rat hepatocytes. Kemp DC, Zamek-Gliszczynski MJ, Brouwer KL. PubMed
  • J Pharmacol Exp Ther. 2004;311:1203-10. Hepatobiliary disposition of the metabolically stable opioid peptide [D-Pen2, D-Pen5]-enkephalin (DPDPE): pharmacokinetic consequences of the interplay between multiple transport systems. Hoffmaster KA, Zamek-Gliszczynski MJ, Pollack GM, Brouwer KL. PubMed
  • Mol Pharmacol. 2003;64:154-9. 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. PubMed
  • J Pharmacol Exp Ther. 2003;304:801-9. Pharmacokinetics of 5 (and 6)-carboxy-2',7'-dichlorofluorescein and its diacetate promoiety in the liver. Zamek-Gliszczynski MJ, Xiong H, Patel NJ, Turncliff RZ, Pollack GM, Brouwer KL. PubMed

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Last update: April 2021