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The emerging role of P-glycoprotein inhibitors in drug delivery: a patent review

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Pages 561-576 | Published online: 26 Feb 2011

Bibliography

  • Gottesman MM, Ling V. The molecular basis of multidrug resistance in cancer: the early years of P-glycoprotein research. FEBS Lett 2006;21:998-1009
  • Bansal T, Jaggi M, Khar RK, Talegaonkar S. Emerging significance of flavonoids as p-glycoprotein inhibitors in cancer chemotherapy. J Pharm Pharm Sci 2009;12(1):46-78
  • Shukla S, Wu CP, Ambudkar SV. Development of inhibitors of ATP-binding cassette drug transporters-present status and challenges. Expert Opin Drug Metab Toxicol 2008;4(2):205-23
  • Hennessy M, Spiers JP. A primer on the mechanics of P-glycoprotein the multidrug transporter. Pharmacol Res 2007;55:1-15
  • McDevitt CA, Callaghan R. How can we best use structural information on P-glycoprotein to design inhibitors? Pharmacol Ther 2007;113:429-41
  • Colabufo NA, Berardi F, Cantore M, Perspectives of P-glycoprotein modulating agents in oncology and neurodegenerative diseases: pharmaceutical, biological, and diagnostic potentials. J Med Chem 2010;53:1883-97
  • Krishna R, Mayer LD. Multidrug resistance (MDR) in cancer. Mechanisms, reversal using modulators of MDR and the role of MDR modulators in influencing the pharmacokinetics of anticancer drugs. Eur J Pharm Sci 2000;11:265-83
  • Varma MV, Ashokraj Y, Dey CS, Panchagnula R. Pglycoprotein inhibitors and their screening: a perspective from bioavailability enhancement. Pharmacol Res 2003;48:347-59
  • McKeegan KS, Borges-Walmsley MI, Walmsley AR. Structural understanding of efflux-mediated drug resistance: potential routes to efflux inhibition. Curr Opin Pharmacol 2004;4:479-86
  • Boesch D, Gaveriaux C, Jachez B, In vivo circumvention of P-glycoprotein-mediated multidrug resistance of tumor cells with SDZ PSC 833. Cancer Res 1991;51:4226-33
  • Thomas H, Coley HM. Overcoming multidrug resistance in cancer: an update on the clinical strategy of inhibiting p-glycoprotein. Cancer Control 2003;10(2):159-65
  • Coley HM. Overcoming multidrug resistance in cancer: clinical studies of p-glycoprotein inhibitors. Methods Mol Biol 2010;596:341-58
  • Ponte-Sucre A. Availability and applications of ATP-binding cassette (ABC) transporter blockers. Appl Microbiol Biotechnol 2007;76:279-86
  • Shukla S, Wu CP, Ambudkar SV. Development of inhibitors of ATP-binding cassette drug transporters-present status and challenges. Expert Opin Drug Metab Toxicol 2008;4(2):205-23
  • Bansal T, Akhtar N, Jaggi M, Novel formulation approaches for optimising delivery of anticancer drugs based on p-glycoprotein modulation. Drug Discov Today 2009;14:21-2
  • Lee BD, Li Z, French KJ, Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein. J Med Chem 2004;47(6):1413-22
  • Xenova Ltd. Anthranilic acid derivatives as multi drug resistance modulators. US6218393B1; 2001
  • Degenhardt CR, Eickhoff DJ. Substituted heterocyclic compounds for treating multidrug resistance. US7135483; 2006
  • Perez-Tomas R. Multidrug resistance: retrospect and prospects in anti-cancer drug treatment. Curr Med Chem 2006;13:1859-76
  • Huang M, Liu G. The study of innate drug resistance of human hepatocellular carcinoma Bel17402 cell line. Cancer Lett 1999;135:97-105
  • Pfizer, Inc. Compositions having improved bioavailability. US20020165120; 2002
  • Song XR, Cai Z, Zheng Y, Reversion of multidrug resistance by co-encapsulation of vincristine and verapamil in PLGA nanoparticles. Eur J Pharm Sci 2009;37:300-5
  • Bansal T, Mishra G, Jaggi M, Effect of p-glycoprotein inhibitor, verapamil, on oral bioavailability and pharmacokinetics of Irinotecan in rats. Eur J Pharm Sci 2009;36:580-90
  • Candussio L, Decorti G, Crivellato E, Toxicologic and pharmacokinetic study of low doses of verapamil combined with doxorubicin. Life Sci 2002;71:3109-19
  • Slater L, Sweet P, Wetzel M, Comparison of cyclosporine A, verapamil, PSC-833, and cremophor EL, as enhancing agents of VP-16 in murine lymphoid leukemias. Leuk Res 1995;19(8):543-48
  • Saito T, Zhang ZJ, Tokuriki M, Cyclosporine A inhibits the extrusion pump function of p-glycoprotein in the inner ear of mice treated with vinblastine and doxorubicin. Brain Res 2001;901:265-70
  • Teva North America. Method, compositions and kits for increasing the oral bioavailability of pharmaceutical agents. US200710060635A1; 2007
  • Zomanex LLC. Methods and formulations for converting intravenous and injectable drugs into oral dosage forms. US20090088393; 2009
  • Hayward NJ, Gefter ML. Methods for enhancing the bioavailability of a drug. US200510288222A1; 2005
  • Arimori K, Kuroki N, Hidaka M, Effect of p-glycoprotein modulator, cyclosporin A, on the gastrointestinal excretion of irinotecan and its metabolite SN-38 in rats. Pharm Res 2003;20(6):910-17
  • Ozben T. Mechanisms and strategies to overcome multiple drug resistance in cancer. FEBS Lett 2006;580:2903-09
  • Twentyman PR, Bleehen NM. Resistance modification by PSC-833, a novel non-immunosuppressive cyclosporin. Eur J Cancer 1991;27:1639-42
  • Lo Y, Liu F, Cherng J. Effect of PSC 833 liposomes and intralipid on the transport of epirubicin in Caco-2 cells and rat intestines. J Control Release 2001;76:1-10
  • Novartis. Combination comprising a P-gp inhibitor and an anti-epileptic drug. US20070142266; 2007
  • Van der Holt B, Lowenberg B, Burnett AK, The value of the MDR1 reversal agent PSC-833 in addition to daunorubicin and cytarabine in the treatment of elderly patients with previously untreated acute myeloid leukemia (AML), in relation to MDR1 status at diagnosis. Blood 2005;106:2646-54
  • Balayssac D, Authier N, Cayre A, Coudore F. Does inhibition of P-glycoprotein lead to drug–drug interactions? Toxicol Lett 2005;156:319-29
  • Robert J, Jarry C. Multidrug resistance reversal agents. J Med Chem 2003;46:4805-17
  • Hyafil F, Vergely C, Du Vignaud P, Grand-Perret T. In vitro and in vivo reversal of multidrug resistance by GF120918, an acridonecarboxamide derivative. Cancer Res 1993;53:4595-602
  • De Bruin M, Miyake K, Litman T, Reversal of resistance by GF120918 in cell lines expressing the ABC half-transporter, MXR. Cancer Lett 1999;146:117-26
  • Glaxo Group Ltd. Methods and compositions for increasing penetration of HIV protease inhibitors. WO1999064001; 1999
  • Van Tellingen. Methods and means for the treatment of cancer. US20090170880; 2009
  • Kawamura K, Yamasaki T, Yui J, In vivo evaluation of p-glycoprotein and breast cancer resistance protein modulation in the brain using [11C]gefitinib. Nucl Med Biol 2009;36:239-46
  • Agarwal S, Sane R, Gallardo JL, Distribution of gefitinib to the brain is limited by p-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) mediated active efflux. J Pharmacol Exp Ther 2010;334(1):147-55
  • Sugimoto H, Hirabayashi H, Kimura Y, Quantitative investigation of the impact of P-glycoprotein inhibition on drug transport across blood-brain barrier in rats. Drug Metab Dispos 2011;39(1):8-14
  • Pajeva IK, Wiese M. Structure-activity relationships of tariquidar analogs as multidrug resistance modulators. AAPS J 2009;11:435-44
  • Fox E, Bates SE. Tariquidar (XR9576) a P-glycoprotein drug efflux pump inhibitor. Exp Rev Anticancer Ther 2007;7(4):447-59
  • Kuntner C, Bankstahl JP, Bankstahl M, Dose-response assessment of tariquidar and elacridar and regional quantification of p-glycoprotein inhibition at the rat blood-brain barrier using (R)-[(11)C] verapamil PET. Eur J Nucl Med Mol Imaging 2010;37(5):942-53
  • Pusztai L, Wagner P, Ibrahim N, Phase II study of tariquidar, a selective P-glycoprotein inhibitor, in patients with chemotherapy-resistant advanced breast cancer. Cancer 2005;104:682-91
  • Nobili S, Landini I, Giglioni B, Mini E. Pharmacological strategies for overcoming multidrug resistance. Curr Drug Targets 2006;7:861-79
  • Sato W, Fukazawa N, Suzuki T, Circumvention of multidrug resistance by a newly synthesized quinoline derivative, MS-073. Cancer Res 1991;51:2420-4
  • Dantzig AH, Shepard RL, Law KL, Selectivity of the multidrug resistance modulator, LY335979, for P-glycoprotein and effect on cytochrome P-450 activities. J Pharmacol Exp Ther 1999;290:854-62
  • Kember EM, Cleypool C, Boogerd W, The influence of the P-glycoprotein inhibitor zosuquidar trihydrochloride (LY335979) on the brain penetration in mice. Cancer Chemother Pharmacol 2004;53(2)173-8
  • Hugger ED, Novak BL, Burton PS, A comparison of commonly used polyethoxylated pharmaceutical excipients on their ability to inhibit P-glycoprotein activity in vitro. J Pharm Sci 2002;91:1991-02
  • Rege BD, Kaob JPY, Pollia JE. Effects of nonionic surfactants on membrane transporters in Caco-2 cell monolayers. Eur J Pharm Sci 2002;16:237-46
  • Collnot EM, Baldes C, Wempe MF, Influence of vitamin E TPGS poly(ethylene glycol) chain length on apical efflux transporters in Caco-2 cell monolayers. J Control Release 2006;111:35-40
  • Varma MVS, Panchagnula R. Enhanced oral paclitaxel absorption with vitamin E-TPGS: effect on solubility and permeability in vitro, in situ and in vivo. Eur J Pharm Sci 2005;25:445-53
  • Wempe MF, Lehr CM, Collnot EM, Methods and pharmaceutical formulations for increasing bioavailability. US20070060610; 2007
  • Zhang L, Zhang YD, Strong JM. A regulatory viewpoint on transporter-based drug interactions. Xenobiotica 2008;38:709-24
  • Hyatt JA, Zima GC, Edgar KJ, Pharmaceutical formulations containing vitamin E TPGS molecules that solubilize lipophilic drugs without significant efflux inhibition, and use of such formulations. US200610165769A1; 2006
  • Shen Q, Lin Y, Handa T. Modulation of intestinal P-glycoprotein function by polyethylene glycols and their derivatives by in vitro transport and in situ absorption studies. Int J Pharm 2006;313:49-56
  • Aventis Pharmaceuticals, Inc. Method of enhancing bioavailability of fexofenadine and its derivatives. US6451815; 2002
  • Cornaire G, Woodley J, Hermann P, Impact of excipients on the absorption of p-glycoprotein substrates in vitro and in vivo. Int J Pharm 2004;278:119-31
  • Lin Y, Shen Q, Katsumi H, Effects of labrasol and other pharmaceutical excipients on the intestinal transport and absorption of rhodamine123, a P-glycoprotein substrate, in rats. Biol Pharm Bull 2007;7:1301-7
  • Shire Laboratories, Inc. Micellar systems useful for delivery of lipophilic or hydrophobic compounds. US20050191343; 2005
  • Sri International. Orally-absorbed solid dose formulation for vancomycin. US20090111736; 2009
  • Aventis Pharma. Galenic applications of self-emulsifying mixtures of lipidic excipients. US20080193519; 2008
  • Werle M. Natural and synthetic polymers as inhibitors of drug efflux pumps. Pharm Res 2008;25:500-11
  • Werle M, Hoffer M. Glutathione and thiolated chitosan inhibit multidrug resistance P-glycoprotein activity in excised small intestine. J Control Release 2006;111:41-6
  • Thio Matrix Forschungs. Use of compounds containing thiol groups as efflux pump inhibitors. US20080200563; 2008
  • Iqbal J, Hombach J, Matuszczak B, Bernkop-Schnurch A. Design and in vitro evaluation of a novel polymeric P-glycoprotein (P-gp) inhibitor. J Control Release 2010;147(1):62-9
  • Iqbal J, Sarti F, Perera G, Development and in vivo evaluation of an oral drug delivery system for paclitaxel. Biomaterials 2011;32(1):170-5
  • Pfizer, Inc. Method of increasing the bioavailability and tissue penetration of azithromycin. US20040091527; 2004
  • Foger F, Malaivijitnond S, Wannaprasert T, Effect of a thiolated polymer on oral paclitaxel absorption and tumor growth in rats. J Drug Target 2008;16(2):149-55
  • Sachs-Barrable K, Thamboo A, Lee DS, Wasan KM. Lipid excipients Peceol and Gelucire 44/14 decrease P-glycoprotein mediated efflux of rhodamine 123 partially due to modifying P-glycoprotein protein expression within Caco-2 cells. J Pharm Pharm Sci 2007;10:319-31
  • D-Pharm Ltd. Use of branched chain fatty acids and derivatives thereof for inhibition of p-glycoprotein. US6605638B1; 2003
  • Lienau P, Backensfeld T, Reichel A, Jung T. Pharmaceutical preparations, use of these preparations and process for increasing the biovailability of pharmaceutical substances to be administered perorally. US200410223983A1; 2004
  • Hanmi Pharm CoLtd. P-glycoprotein inhibitor, method for preparing the same and pharmaceutical composition comprising the same. US20070072900A1; 2007
  • Eli Lilly and Co. Drug resistance and multidrug resistance modulators. US6180633; 2001
  • Smith CD. Compounds for enhancing chemotherapy. US6693112B2; 2004
  • Merrell Pharmaceuticals, Inc. Diarylalkyl piperidines useful as multi-drug resistant tumor agents. US5648365; 1997
  • Merrell Pharmaceuticals, Inc. Reversal of multi-drug resistance by triphenyl-azacycloalkane derivatives. US5670521; 1997
  • Pfizer, Inc. Compounds enhancing antitumor activity of other cytotoxic agents. US6130217; 2000
  • Berardi F, Colabufo NA, Perrone R, 1-Phenylalcoxy-2-beta-phenylethyl derivatives as p-glycoprotein (P-gp) inhibitors useful in drug resistance events. US20090093493; 2009
  • Schering Corp. Methods for treating multidrug resistance. US6703400B2; 2004
  • Medlen CE, Anderson R, O'Sullivan JF. MDR resistance treatment and novel pharmaceutically active riminophenazines. US5763443; 1998
  • Badalian AM. Aryl-indane compounds. US20020128231A1; 2002
  • Limtrakul P, Khantamat O, Pintha K. Inhibition of P-glycoprotein function and expression by kaempferol and quercetin. J Chemother 2005;17:86-95
  • Aqil M, Ahad A, Sultana Y, Ali A. Status of terpenes as skin penetration enhancers. Drug Discov Today 2007;2:601-7
  • Ahad A, Aqil M, Kohli K, Chemical penetration enhancers: a patent review. Expert Opin Ther Pat 2009;19(7):969-88
  • Av Max, Inc. Use of essential oils to increase bioavailability of orally administered pharmaceutical compounds. US6121234; 2000
  • Av Max, Inc. Use of benzoin gum to inhibit p-glycoprotein-mediated resistance of pharmaceutical compounds. US5916566; 1999
  • Eurand International. Compositions with enhanced oral bioavailability. WO2001052896; 2001
  • Pain Therapeutics, Inc. Inhibitors of ABC drug transporters at the blood-brain barrier. US7034036B2; 2006
  • Pain Therapeutics, Inc. Inhibitors of ABC drug transporters at the blood-brain barrier. US200710054932A1; 2007
  • Chung H, Jeong SY, Kwon IC, P-glycoprotein inhibitor comprising octilonium bromide as an effective ingredient. US200610141033A1; 2006
  • Salphati L, Benet LZ. Effects of ketoconazole on digoxin absorption and disposition in rat. Pharmacology 1998;56:308-13
  • Benet L, Wu CY. Screening method for the identification of bioenhancers through the inhibition of p-glycoprotein transport in the gut of a mammal. US5567592; 1996
  • Benet LZ, Wu CY. Method for increasing bioavailability of oral pharmaceutical compositions. US6028054; 2000
  • Pfizer, Inc. Method of increasing the bioavailability and tissue penetration of azithromycin. US200410091527A1; 2004
  • Mitra AK, Majumdar S, Jain R, Nashed Y. Peptidyl prodrugs that resist p-glycoprotein mediated drug efflux. US200710142302A1; 2007

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