Considerations in the design and development of transport inhibitors as adjuncts to drug therapy

Advanced Drug Delivery Reviews

Volumn 55, Issue 1, 2003, Pages 133-150

  Dantzig, Anne H ^a   De Alwis, Dinesh P ^a   Burgess, Michael ^a  

^a ELI LILLY AND COMPANY   (United States)

Author keywords

ATP binding cassette transporter; MDR modulator; Multidrug resistance associated protein; P Glycoprotein

Indexed keywords

DISEASES; PHARMACOKINETICS; PROTEINS; TOXICITY; TUMORS;

DRUG EFFLUX TRANSPORTERS; MULTIDRUG RESISTANCE;

DRUG THERAPY;

5 [3 (4 DIPHENYLACETYL 1 PIPERAZINYL) 2 HYDROXYPROPOXY]QUINOLINE; ALKALOID; AMSACRINE; ANTHRACYCLINE DERIVATIVE; CALCIUM CHANNEL BLOCKING AGENT; DACTINOMYCIN; DAUNORUBICIN; DOCETAXEL; DOXORUBICIN; DOXORUBICINOL; ELACRIDAR; EPIPODOPHYLLOTOXIN; EPIRUBICIN; ETOPOSIDE; GLYCOPROTEIN P; GLYCOPROTEIN P INHIBITOR; IDARUBICIN; IRINOTECAN; LANIQUIDAR; MITOMYCIN C; MITOXANTRONE; NAVELBINE; OC 144 093; PACLITAXEL; PROTEIN INHIBITOR; TARIQUIDAR; TAXANE DERIVATIVE; TENIPOSIDE; TOPOTECAN; TRIMETREXATE; UNCLASSIFIED DRUG; UNINDEXED DRUG; VALSPODAR; VINBLASTINE; VINCRISTINE; VINDESINE; ZOSUQUIDAR;

CELL; CLINICAL TRIAL; DRUG DESIGN; DRUG DISTRIBUTION; DRUG EFFICACY; DRUG EXCRETION; DRUG METABOLISM; DRUG SELECTIVITY; DRUG TARGETING; DRUG TISSUE LEVEL; DRUG TRANSPORT; HUMAN; MULTIDRUG RESISTANCE; PRIORITY JOURNAL; PROTEIN EXPRESSION; REVIEW; TOXICITY;

EID: 0037457796     PISSN: 0169409X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0169-409X(02)00175-8     Document Type: Article

References (122)

1. Dean M., Hamon Y., Chimini G. The human ATP-binding cassette (ABC) transporter superfamily. J. Lipid Res. 42:2001;1007-1017.
2. Kerb R., Hoffmeyer S., Brinkmann U. ABC drug transporters: hereditary polymorphisms and pharmacological impact in MDR1, MRP1, and MRP2. Pharmacogenomics. 2:2001;1-14.
3. Litman T., Druley T.E., Stein W.D., Bates S.E. From MDR to MXR: new understanding of multidrug resistance systems, their properties and clinical significance. Cell. Mol. Life Sci. 58:2001;931-958.
4. Gottesman M., Ambudkar S. Overview: ABC transporters and human disease. J. Bioenerg. Biomemb. 33:2001;453-458.
5. Ueda K., Yoshida A., Amachi T. Recent progress in P-glycoprotein research. Anti Cancer Drug Design. 14:1999;115-121.
6. Efferth T., Osieka R. Clinical relevance of the MDR-1 gene and its gene product, P-glycoprotein, for cancer chemotherapy: A meta-analysis. Tumordiagn. u. Ther. 14:1993;238-243.
7. Trock B.J., Leonessa F., Clarke R. Multidrug resistance in breast cancer: a meta-analysis of MDR/GP170 expression and its possible functional significance. J. Natl. Cancer Inst. 89:1997;917-931.
8. Abolhoda A., Wilson A.I., Ross H., Danenberg P.V., Burt M., Scotto K.W. Rapid activiation of MDR1 gene expression in human metastatic sarcoma after in vivo exposure to doxorubicin. Clinical Cancer Res. 5:1999;3352-3356.
9. Cole S.P.C., Bhardwaj G., Gerlach J.H., Macide J.E., Grant C.E., Almquist K.C., Stewart A.J., Kurz E.U., Duncan A.M.V., Deeley R.G. Overexpression of a transporter gene in a multidrug-resistant human lung cancer cell line. Science. 258:1992;1650-1654.
10. Cole S.P.C., Sparks K.E., Fraser K., Loe D.W., Grant C.E., Wilson G.M., Deeley R.G. Pharmacological characterization of multidrug resistant MRP-transfected human tumor cells. Cancer Res. 54:1994;5902-5910.
11. Campling B.G., Young L.C., Baer K.A., Lam Y.M., Deeley R.G., Cole S.P.C., Gerlach J.H. Expression of the MRP and MDR1 multidrug resistance genes in small cell lung cancer. Clin. Cancer Res. 3:1997;115-122.
12. Wright S.R., Boag A.H., Valdimarsson C., Hipfner D.R., Campling B.G., Cole S.P.C., Deeley R.G. Immunohistochernical detection of multidrug resistance protein in human lung cancer and normal lung. Clin. Cancer Res. 4:1998;2279-2289.
13. Young L.C., Campling B., Voskoglou-Nomikos T., Cole S.P.C., Deeley R.G., Gerlach J.H. Expression of multidrug resistance protein-related genes in lung cancer: correlation with drug response. Clin. Cancer Res. 5:1999;673-680.
14. 4 and structurally related conjugates. Vitamins and Hormones. 64:2002;153-184.
15. Loe D.W., Deeley R.G., Cole S.P.C. Characterization of vincristine transport by the M-r 190,000 multi drug resistance protein (MRP): Evidence for cotransport with reduced glutathione. Cancer Research. 58:1998;5130-5136.
16. Renes J., deVries E.G.E., Nienhuis E.F., Jansen P.L.M., Muller M. ATP- and glutathione-dependent transport of ehemotherapeutic drugs by the multidrug resistance protein MRP1. Br. J. Pharmacol. 126:1999;681-688.
17. Zeng H., Liu G., Rea P., Kruh G. Transport of amphipathic anions by human multidrug resistance protein 3. Cancer Res. 60:2000;4479-4484.
18. Kool M., van der Linden M., de Haas M., Scheffer G.L., de Vree J.M.L., Smith A.J., Jansen G., Peters G.J., Ponne N., Scheper R.J., Elferink R., Baas F., Borst P. MRP3, an organic anion transporter able to transport anti-cancer drugs. Proc. Natl. Acad. Sci. USA. 96:1999;6914-6919.
19. Kruh C., Zeng H., Rea P., Liu G., Chen Z., Lee K., Belinsky M. MRP subfamily transporters and resistance to anticancer agents. J. Bioenerg. Biomemb. 33:2001;493-501.
20. Zelcer N., Saeki T., Reid G., Beijnen J., Borst P. Characterization of drug transport by the human multidrug resistance protein 3 (ABCC3). J. Biol. Chem. 276:2001;46400-46407.
21. Schuetz J.D., Connelly M.C., Sun D.X., Paibir S.G., Flynn P.M., Srinivas R.V., Kumar A., Fridland A. MRP4: A previously unidentified factor in resistance to nucleoside-based antiviral drugs. Nature Medicine. 5:1999;1048-1051.
22. Lai L.Q., Tan T.M. Role of glutathione in the multidrug resistance protein 4 (MRP4/ABCC4)rnediated efflux of cAMP and resistance to purine analogues. Biochem. J. 361:2002;497-503.
23. van Aubel R.A., Smeets P.H., Peters J.G., Bindels R.J., Russel F.G. The MRP4/ABCC4 gene encodes a novel apical organic anion transporter in human kidney proximal tubules: putative efflux pump for urinary cAMP and cGMP. J. Am. Soc. Nephrol. 13:2002;595-603.
24. Jedlitschky C., Burchell B., Keppler D. The multidrug resistance protein 5 functions as an ATP-dependent export pump for cyclic nucleotides. J. Biol. Chem. 275:2000;30069-30074.
25. Maliepaard M., van Gastelen M.A., de Jong L.A., Pluim D., van Waardenburg R.C.A.M., Ruevekamp-Helmers M.C., Hoot B.G.J., Schellens J.H.M. Overexpression of the BCRP/MXR/ABCP gene in a topotecan-selected ovarian tumor cell line. Cancer Res. 59:1999;4559-4563.
26. Volk E.L., Rohde K., Rhee M., McGuire J.J., Doyle L.A., Ross D.D., Schneider F. Methotrexate cross-resistance in a mitoxantrone-selected multidrugresistant MCF7 breast cancer cell line is attributable to enhanced energydependent drug efflux. Cancer Res. 60:2000;3514-3521.
27. Nakatomi K., Yoshikawa M., Oka M., lkegami Y., Hayasaka S., Sano K., Shiozawa K., Kawabata S., Soda H., Ishikawa T., Tanabe S., Kohno S. Transport of 7-ethyl-10-hydroxycamptothecin (SN-38) by breast cancer resistance protein ABCG2 in human lung cancer cells. Biochem. Biophys. Res. Commun. 288:2001;827-832.
28. Honjo Y., Hrycyna C.A., Yan Q.W., Medina-Perez W.Y., Robey R.W., van de Laar A., Litman T., Dean M., Bates S.E. Acquired mutations in the MXR/BCRP/ABCP gene alter substrate specificity in MXR/BCRP/ABCP-overexpressing cells. Cancer Res. 61:2001;6635-6639.
29. Bates S.E., Robey R., Miyake K., Rao K., Ross D.D., Litman T. The role of half-transporters in multidrug resistance. J. Bioenerg. Biomemb. 33:2001;503-511.
30. Matheny C.J., Lamb M.W., Brouwer K.L.R., Pollack G.M. Pharmacokinetic and pharmacodynamic implications of P-glycoprotein modulation. Pharmcotherapy. 21:2001;778-796.
31. Ayrton A., Morgan P. Role of transport proteins in drug absorption, distribution and excretion. Xenobiotica. 31:2001;469-497.
32. van Asperen J., van Tellingen O., Sparreboom A., Schinkel A.H., Borst P., Nooijen W.J., Beijnen J.H. Enhanced oval bioavailability of paclitaxel in mice treated with the P-glycoprotein blocker SDZ PSC 833. Br. J. Cancer. 76:1997;1181-1183.
33. van Asperen J., van Tellingen O., van der Valk M.A., Rozenhart M., Beijnen J.H. Enhanced oral absorption and decreased elimination of paclitaxel in mice cotreated with cyclosporin A. Clin. Cancer Res. 4:1998;2293-2297.
34. Malingre M.M., Ten Bokkel Huinink W.W., Mackay M., Schellens J.H.M., Bcijnen J.H. Pharmacokinetics of oral cyclosporin A when co-administered to enhance the absorption of orally administered docetaxel. Eur. J. Clinical Pharmacol. 57:2001;305-307.
35. Garberg P. In Vitro models of the blood-brain barrier. Atla Alternatives To Laboratory Animals. 26:1998;821-847.
36. van Asperen J., Mayer U., van Tellinger O., Beijnen J.H. The functional role of P-glycoprotein in the blood-brain barrier. Pharm. Sci. 86:1997;881-884.
37. Schinkel A.H., Wangenaar E., Mol C.A., van Deemter L. P-glycoprotein in the blood-brain barrier of mice influences the brain penetration and pharmacological activity of many drugs. J. Clin. Invest. 97:1996;2517-2524.
38. van Asperen J., van Tellingen O., Schinkel A.H., Beijnen J.H. Comparative pharmacokinetics of vinblastine after a 96-hour continuous infusion in wild-type mice and mice lacking mdrla P-glycoprotein. J. Pharmacol. Exp. Ther. 289:1999;329-333.
39. van Asperen J., van Tellingen O., Tijssen F., Schinkel A.H., Beijnen J.H. Increased accumulation of doxorubicin and doxorubicinol in cardiac tissue of mice lacking mdrla P-glycoprotein. Br. J. Cancer. 79:1999;108-113.
40. van Asperen J., van Tellingen O., Beijnen J.H. The role of mdr1a P-glycoprotein in the biliary and intestinal secretion of doxorubicin and vinblastine in mice. Drug Metab. Dispos. 28:2000;264-267.
41. van Asperen J., Schinkel A.H., Beijnen J.H., Nooijen W.J., Borst P., van Tellingen O. Altered pharmacokinetics of vinblastine in Mdr1a P-glycoprotein-deficient mice. J. Natl. Cancer Inst. 88:1996;994-999.
42. Wijnholds J., Scheffer G.L., van der Valk M., van der Valk P., Beijnen J.H., Scheper R.J., Borst P. Multidrug resistance protein 1 protects the oropharyngeal mucosal layer and the testicular tubules against drug-induced damage. J. Exp. Med. 188:1998;797-808.
43. Rao V.V., Dahlheimer J.L., Bardgett M.E., Snyder A.Z., Finch R.A., Sartorelli A.C., Piwnica Worms D. Choroid plexus epithelial expression of MDR1 P glycoprotein and multidrug resistance-associated protein contribute to the bloodcerebrospinal-fluid drug-permeability barrier. Proc. Natl. Acad. Sci. USA. 96:1999;3900-3905.
44. Buchler M., Konig J., Brom M., Kartenbeck J., Spring H., Hone T., Keppler D. cDNA cloning of the hepatocyte canalicular isoform of the multidrug resistance proein, cMrp, reveals a novel conjugate export pump deficient in hyperbilirubinernic mutant rats. J. Biol. Chem. 271:1996;15091-15098.
45. Uchiumi T., Hinoshita E., Haga S., Nakamura T., Tanaka T., Toh S., Furukawa M., Kawabe T., Wada M., Kagotani K., Okumura K., Kohno K., Akiyama S.-I., Kuwano M. Isolation of a novel human canalicular multispecific organic anion transporter, cMOAT2/MRP3, and its expression in cisplatinresistant cancer cells with decreased ATP-dependent drug transport. Biochem. Biophys. Res. Cornmun. 252:1998;103-110.
46. Paulusma C.C., Bosma P.J., Zaman G.J.R., Bakker C.T.M., Otter M., Scheffer C.L., Scheper R.J., Borst P., Oude Elferink R.P.J. Congenital jaundice in rats with a mutation in a multidrug resistance-associated protein gene. Science. 271:1996;1126-1128.
47. Toh S., Wada M., Uchiumi T., Inokuchi A., Makino Y., Horie Y., Adachi Y., Sakisaka S., Kuwano M. Genomic structure of the canalicular multispecific organic anion-transporter gene (MRP2/cMOAT) and mutations in the ATP-bindingcassette region in Dubin-Johnson syndrome. American Journal Of Human Genetics. 64:1999;739-746.
48. Konig J., Rost D., Cui Y.H., Keppler D. Characterization of the human multidrug resistance protein isoform MRP3 localized to the basolateral hepatocyte membrane. Hepatology. 29:1999;1156-1163.
49. Zeng H., Bain L.J., Belinsky M.G., Kruh G.D. Expression of multidrug resistance protein-3 (multispecific organic anion transporter-D) in human embryonic kidney 293 cells confers resistance to anticancer agents. Cancer Res. 59:1999;5964-5967.
50. Zeng H., Chen Z.-S., Belinsky M.G., Rea P.A., Kruh G.D. Transport of methotrexate (MTX) and folates by multidrug resistance protein (MRP) 3 and MRP1: Effect of polyglutamylation on MTX transport. Cancer Res. 61:2001;7225-7232.
51. Maliepaard M., Scheffer G.L., Faneyte I.F., van Gastelen M.A., Pijnenborg A.C., Schinkel A.H., van De Vijver M.J., Scheper R.J., Schellens J.H. Subcellular localization and distribution of the breast cancer resistance protein transporter in normal human tissues. Cancer Res. 61:2001;3458-3464.
52. Ford J.M., Hait W.N. Pharmacology of drugs that alter multidrug resistance in cancer. Pharmacol. Reviews. 42:1990;155-199.
53. Avendano C., Menendez J.C. Inhibitors of multidrug resistance to antitumor agents (MDR). Cur. Med. Chem. 9:2002;159-193.
54. Cottesman M.M., Fojo T., Bates S.F. Multidrug resistance in cancer: Role of ATP-dependent transporters. Nature Rev. Cancer. 2:2002;48-58.
55. Raderer M., Scheithauer W. Clinical trials of agents that reverse multidrug resistance. Cancer. 72:1993;3553-3563.
56. Germann U.A., Ford P.J., Shlyakhter D., Mason V.S., Harding M.W. Chemosensitization and drug accumulation effects of VX710, verapamil, cyclosporin A, MS-209 and GF120918 in multidrug resistant HL60/ADR cells expressing the multidrug resistance-associated MRP. Anti-Cancer Drugs. 8:1997;141-155.
57. Bohme M., Büchler M., Müller M., Keppler D. Differential inhibition by cyclosporins of primary-active ATP-dependent transporters in the hepatocyte canalicular membrane. FEBS Lett. 333:1993;193-196.
58. Childs S., Yeh R.L., Hui D., Ling V. Taxol resistance mediated by transfection of the liver-specific sister gcne of P-glyeoprotein. Cancer Res. 58:1998;4160-4167.
59. Hyafil F., Vergely C., Du Vignaud P., Grand-Perret T. In vitro and in vivo reversal of multidrug resistance by GF120918, an acnidonecarboxamide derivative. Cancer Res. 53:1993;4595-4602.
60. Allen J.D., Brinkhuis R.F., Wijnholds J., Schinkel A.H. The mouse Bcrp1/Mxr/Abcp gene: Amplification and overexpression in cell lincs selectcd for resistance to topotecan, mitoxantrone, or doxorubicin. Cancer Res. 59:1999;4237-4241.
61. Evers R., Kool M., Smith A.J., van Deemter L., de Haas M., Borst P. Inhibitory effect of the reversal agents V-104, GF120918 and Pluronic L61 on MDR1 Pgp-, MRP1- and MRP2-mediated transport. Br. J. Cancer. 83:2000;366-374.
62. Maliepaard M., van Gastelen M.A., Tohgo A., Hausheer F.H., van Waardenburg R.C., de Jong L.A., Pluim D., Beijnen H.H., Schellens J.H.M. Circumvention of breast cancer resistance protein (BCRP)-mediated resistance to camptothecins in vitro using non-substrate drugs or the BCRP inhibitor GF120918. Clinical Cancer Res. 7:2001;935-941.
63. Martin C., Berridge G., Mistry P., Higgins C., Charlton P., Callaghan R. The molecular interaction of the high affinity reversal agent XR9576 with Pglycoprotein. Br. J. Pharmacol. 128:1999;403-411.
64. Mistry P., Stewart A.J., Dangerfield W., Okiji S., Liddle C., Bootle D., Plumb J.A., Templeton D., Charlton P. In vitro and in vivo reversal of P-glycoproteinmediated multidrug resistance by a novel potent modulator, XR9576. Cancer Res. 61:2001;749-758.
65. Newman M.J., Rodarte J.C., Benbatoul K.D., Romano S.J., Zhang C., Krane S., Moran E.J., Uyeda R.T., Dixon R., Cuns E.S., Mayer L.D. Discovery and characterization of OC144-093, a novel inhibitor of P-glycoprotein-mediated multidrug resistance. Cancer Res. 60:2000;2964-2972.
66. Dantzig A.H., Shepard R.L., Law K.L., Tabas L., Pratt S., Gillespie J.S., Binkley S.N., Kuhfeld M.T., Starling J.J., Wrighton S.A. Selectivity of the multidrug resistance modulator, LY335979, for P-glycoprotein and effect on cytochrome P450 activities. JPET. 290:1999;854-890.
67. R.L. Shepard, J. Cao, J.J. Starling, A.H. Dantzig, Effect of P-glycoprotein inhibitor, LY335979 on P-glycoprotein, MRP1 and BCRP-mediated resistance. Int. J. Cancer 103 (in press).
68. Wacher V.J., Wu C.Y., Benet L.Z. Overlapping substrate specificities and tissue distribution of cytochrome P450 3A and P-glycoprotein: implications for drug delivery and activity in cancer chemotherapy. Mol. Carcinog. 13:1995;129-134.
69. Kim R.B., Wandel C., Leake B., Cvetkovic M., Frornm M.F., Dempsey P.J., Roden M.M., Belas F., Chaudhary A.K., Roden D.M., Wood A.J.J., Wilkinson G.R. Interrelationship between substrates and inhibitors of human CYP3A and P-glycoprotein. Pharm. Res. 16:1999;408-414.
70. Schuetz E.G., Beck W.T., Schuetz J.D. Modulators and substrates of Pglycoprotein and cytochrome P4503A coordinately up-regulate these proteins in human colon carcinoma cells. Mol. Pharmacol. 49:1996;311-318.
71. Tateishi T., Nakura H., Asoh M., Watanabe M., Tanaka M., Kumai T., Kobayashi S. Multiple cytochrome P-450 subfamilies are co-induced with P-glycoprotein by both phenothiazine and 2-acetylaminofluorene in rats. Cancer Letters. 138:1999;73-79.
72. Schuetz E.G. Induction of cytochromes P450. Curt. Drug Metab. 2:2001;139-147.
73. Kostrubsky V.E., Lewis L.D., Strom S.C., Wood S.C., Schuetz E.G., Schuetz J.D., Sinclair P.R., Wrighton S.A., Sinclair J.F. Induction of cytochrome P4503A by taxol in primary cultures of human hepatocytes. Arch. Biochem. Biophys. 355:1998;131-136.
74. Synold T.W., Dussault I., Forman B.M. The orphan nuclear receptor SXR coordinately regulates drug metabolism and efflux. Nat. Med. 7:2001;584-590.
75. Waridel C., Kim R.B., Kajiji S., Guengerich F.P., Wilkinson G.R., Wood A.J.J. P-glycoprotein and cytochronie P-450 3A inkiibition: Dissociation of inhibitory potencies. Cancer Res. 59:1999;3944-3948.
76. Benet L.A., Wu C.-Y., Hebert M.F., Wacher V.J. Intestinal drug metabolism and antitransport processes: A potential paradigm shift in oral drug delivery. J. Control. Release. 39:1996;139-143.
77. Fischer V., Rodriquez-Cascon A., Heitz F., Tynes R., Hauck C., Cohen D., Vickers A.E.M. The multidrug resistance modulator vaispodar (PSC 833) is metabolizcd by human cytochrome P450 3A. Implications for drug-drug Interactions and pharmacological activity of the main metabolite. Drug Met. Disp. 26:1998;802-811.
78. Sikic B.I., Fisher G.A., Lum B.L., Halsey J., Beketie-Oreskovic L., Chen G. Modulation and prevention of multidrug resistance by inhibitors of Pglycoprotein. Cancer Chem. Pharmacol. 40:1997;S13-S19.
79. Chico I., Kang M.H., Bergan R., Abraham J., Bakke S., Meadows B., Rutt A., Robey R., Coyke P., Merino M., Coldspiel B., Smith T., Steinberg S., Figg W.D., Fojo T., Bates S. Phase I study of infusional paclitaxel in combination with the P-glycoprotein antagonist PSC 833. J. Clin. Oncol. 19:2001;832-842.
80. Rowinsky E.K., Smith L., Wang Y.-M., Chaturvedi P., Villalona M., Campbell E., Aylesworth C., Eckhardt S.G., Hammond L., Kraynak M., Drengler R., Stephenson J.J., Harding M.W., von Hoff D.D. Phase I and pharmacokinetic study of paclitaxel in combination with biricodar, a novel agent that reverses multidrug resistance conferred by overexpression of both MDR1 and MRP. J. Clin. Oncol. 16:1998;2964-2976.
81. Schellens J.H.M., Kruytzer M.F., Vasey P.A., Harris A.L., Deplanque G., Burgess M., deAlwis D., &Callaghan M., Kaye S.B., Beijnen J.H. Phase I and pharmacokinetics study of the P-glycoprotein inhibitor LY335979 and paclitaxel in patients with solid tumors. Am. Assoc. Cancer Res. 42:2001;535.
82. H. Thomas, J.A. Steiner, G.P. Mould, G. Mellows, A.J. Stewart, D.B. Norris, J.F. Waterfall, Abstract #288. A Phase IIA pharmacokinetic study of the P-glycoprotein inhibitor, XR9576 in combination with paclitaxel in patients with ovarian cancer. in Am. Soc. Clin. Oncol., 2001.
83. Monsarrat B., Alvinerie P., Wright M., Dubois J., Gueritte-Voegelein F., Guenard D., Donehower R.C., Rowinsky E.K. Hepatic metabolism and biliary excretion of taxol in rats and humans. J. Natl. Cancer Inst. Monogr. 15:1993;39-46.
84. Waite T., Walle U.K., Kumar G.N., Bhalla K.N. Taxol metabolism and disposition in cancer patients. Drug Metab Dispos. 23:1995;506-512.
85. M.J. Moore, L.L. Siu, A. Oza, M. MacLean, B. Fisher, C. Jordan, C. Slapak, L. Seymour, A phase I study of vinorelbine plus multidrug resistance (MDR) inhibitor LY 335979 in patients with advanced solid tumors. in Proc. of 11th NCI EORTC AACR Symposium on New Drugs in Cancer Therapy, 2000.
86. Leveque D., JehI F. Clinical pharmacokinetics of vinorelbine. Clin. Pharmacokinetics. 31:1996;184-197.
87. Sparreboom A., Planting A.S., Jewell R.C., van der Burg M.E., van der Gaast A., de Bruijn P., Loos W.J., Nooter K., Chandler L., Paul E.M., Wissel P.S., Verweij J. Clinical pharmacokinetics of doxorubicin in combination with GF120918, a potent inhibitor of MDRI P-glycoprotein. Anticancer Drugs. 10:1999;719-728.
88. Allen J.D., Brinkhuis R.F., van Deemter L., Wijnholds J., Schinkel A.H. Extensive contribution of the multidrug transporters P-glycoprotein and MRP1 to basal drug resistance. Cancer Res. 60:2000;5761-5766.
89. Borst P., Evers R., Kool M., Wijnholds J. A family of drug transporters: the multidrug resistance-associated proteins. J. Natl. Cancer Inst. 92:2000;1295-1302.
90. Riggs C.E.J., Benjamin R.S., Serpick A.A., Bachur N.R. Bilary disposition of adriamycin. Clin. Pharmacol. Ther. 22:1977;234-241.
91. Benjamin R., Riggs C.J., Bachur N. Plasma pharmacokinetics of adriamycin and its metabolites in humans with normal hepatic and renal function. Cancer Res. 37:1977;1416-1420.
92. Giaccone C., Linn S.C., Welink J., Catimel C., Stieltjcs H., van der Vijgh W.J., Eeltink C., Vermorken J.B., Pinedo H.M. A dose-finding and pharmacokinetic study of reversal of multidrug resistance with SDZ PSC 833 in combination with doxorubicin in patients with solid tumors. Clin. Cancer Res. 3:1997;2005-2015.
93. Sonneveld P., Marie J., Huisman C. Reversal of multidrug resistance by SDZPSC833, combined with VAD (vincristine, doxorubicin, dexamethasone) in refractory multiple myeloma. A phase I study. Leukemia. 10:1996;1741-1750.
94. Massart C., Gibassier J., Raoul M., Pourquier P., Leclech C., Robert J. Cyclosporin A, verapamil, and S9788 reverse doxorubicin resistance in human medullary thyroid carcinoma cell line. Anticancer Drugs. 6:1995;135-146.
95. Ferry D., Price L., Atsmon J., Moshe I., Merimsy O., van Tellingen O., Steiner J., Mellows G., Norris D.B., Waterfall J. A Phase IIA pharmacokinetic and pharmacodynamic study of the P-glycoprotein inhibitor, XR9576 in patients with doxorubicin chemotherapy. Proc. Am. Assoc. Cancer Res. 42:2001;950.
96. S. Callies, D.P. de Alwis, J.G. Wright, A. Sandier, M. Burgess, L. Aarons, A population pharmacokinetic model for doxorubucin and doxorubucinol in the presence of a novel MDR thodulator, Zosuquidar Trihydrochioride (LY335979). Cancer Chemother. Pharmacol. (in press).
97. Nabholtz J.-M., Senn H.J., Bezwoda W.R., Melnychuk D., Deschenes L., Douma J., Vandenberg T.A., Rapoport B., Rosso R., Trillet-Lenoir V., Drbal J., Molino A., Nortier J.W.R., Richel D.J., Nagykalnai T., Siedlecki P., Wilking N., Genot J.Y., Hupperets P.S.G.J., Pannuti F., Skarlos D., Tomiak E.M., Murawsky M., Alakl M., Riva A., Aapro M. Prospective randomized trial of docetaxel versus mitomycin plus vinbiastine in patients with metastatic breast cancer progressing despite previous anthracycline-containing chemotherapy. 304 Study Group. J. Clin. Oncol. 17:1999;1413-1424.
98. Kim R.B., Fromm M.F., Wandel C., Leaker B. AJ.J. Wood, D.M. Roden, C.R. Wilkinson, The drug transporter P-glycoprotein limits oral absorption and brain entry of HIV-1protease inhibitors. J. Clin. Invest. 101:1998;289-294.
99. Gutmann H., Fricker C., Drewe J., Toeroek M., Miller D.S. Interactions of HIV protease inhibitors with ATP-dependent drug export proteins. Mol. Pharmacol. 56:1999;383-389.
100. Sadeque A.J., Wandel C., He H., Shah S., Wood A.J. Increased drug delivery to the brain by P-glycoprotein inhibition. Clin. Pharmacol. Ther. 68:2000;231-237.
101. Von Hoff D.D., Layard M.W., Basa P., Davis H.L.J., Von Hoff A.L., Rozencweig M., Muggia F.M. Risk factors for doxorubicin-induced congestive heart failure. Ann. Intern. Med. 91:1979;710-717.
102. Witherspoon S.M., Emerson D.L., Ken B.M., Lloyd T.L., Dalton W.S., Wissel P.S. Flow cytometric assay of modulation of P-glycoprotein fucntion in whole blood by the multidrug resistance inhibitor GG918. Clin. Cancer Res. 2:1996;7-12.
103. Robey R., Bakke S., Stein W., Meadows B., Litman T., Patil S., Smith T., Fojo T., Bates S. Efflux of rhodamine from CD56(+) cells as a surrogate marker for teversal of P-glycoprotein-mediated thug efflux by PSC 833. Blood. 93:1999;306-314.
104. Green L.J., Marder P., Slapak C.A. Modulation by LY335979 of P-glycoprotein function in multidrug-resistant cell lines and human natural killer cells. Biochem. Pharmacol. 61:2001;1393-1399.
105. Hendrikse N.H., Franssen E.J., van der Graaf W.T.A., Vaalburg W., deVries E.G.E. Visualization of multidrug resistance in vivo. European Journal Of Nuclear Medicine. 26:1999;283-293.
106. Fracasso P.M., Westerveldt P., Fears C.A., Rosen D.M., Zuhowski E.G., Cazenave L.A., Litchman M., Egorin M.J. Phase I study of paclitaxel in combination with a multidrug resistance modulator, PSC 833 (valspodar), in refractory malignancies. J. Clin. Oncol. 18:(valspodar):2000;1124-1134.
107. Fracasso P.M., Brady M.F., Moore D.H., Walker J.L., Rose P.G., Letvak L., Grogan T.M., McGuire W.P. Phase II study of paclitaxel and valspodar (PSC 833) in refractory ovarian carcinoma: a gynecologic oncology group study. J. Clin. Oncol. 19:2001;2975-2982.
108. Budman D.R., Berry D.A., Cirrincione C.T., Henderson I.C., Wood W.C., Weiss R.B., Ferree C.R., Muss H.B., Green M.R., Norton L., Frei E. Dose and dose intensity as determinants of outcome in the adjuvant treatment of breast cancer. The Cancer and Leukemia Group B. J. Natl. Cancer Inst. 90:1998;1205-1211.
109. Chang J. Chemotherapy dose reduction and delay in clinical practice. Evaluating the risk to patient outcomein adjuvant chemotherapy for breast cancer. Eur. J. Cancer. 36:2000;S11-S14.
110. Evans D.L., Tilby M., Dive C. Differential sensitivity to the induction of apoptosis by cisplatin in proliferating and quiescent immature rat thymocytes is independent of the levels of drug accumulation and DNA adduct formation. Cancer Res. 54:1994;1596-1603.
111. van Tellingen O., Kemper M., Beijnen J.H. P-glycoprotein inhibition in tumors by PSC 833: Impact of dose adjustments on the efficacy doxorubicin chemotherapy. AACR. 42:2001;950.
112. Beijnen J.H., Huizing M.T., ten Bokkel Huinink W.W., Veenhof C.H., Vermorken J.B., Giaccone C., Pinedo H.M. Bioanalysis, pharmacokinetics, and pharmacodynamics of the novel anticancer drug paclitaxel (Taxol). Sem. Oncol. 21:1994;53-62.
113. Leith C.P., Kopecky K.J., Chen I.M., Eijdems L., Slovak M.L., McConnell T.S., Head D.R., Weick J., Grever M.R., Appelbaum F.R., Willman C.L. Frequency and clinical significance of the expression of the multidrug resistance proteins MDR1/P-glycoprotein, MRP1, and LRP in acute myeloid leukemia: a Southwest Oncology Group Study. Blood. 94:1999;1086-1099.
114. L.D. Cripe, M. Tailman, C. Karanes,A.F. List, P.A. Kinney, M.F. Burgess, C.A. Slapak, Abstract # 2492. A phase II trial of Zosuquidar (LY335979), a modulator of P-glycopro!ein (PgP) activity, plus daunorubicin and high-dose cytarabine in patients with newly-diagnosed secondary acute myeloid leukemia (AML), refractory anemia with excess blasts in transformation (RAEB-t) or relapsed/refractory AML. in Proc. Am. Soc. Haematol. Orlando, FL, 2001.
115. Don R., Karanes C., Spier C., Crogan T., Greer J., Moore J., Weinberger B., Schiller G., Pearce T., Litchman M., Dalton W., Roe D., List A. Phase I/II study of the P-glycoprotein modulator PSC 833 in patients with acute myeloid leukemia. J. Clin. Oncol. 19:2001;1589-1599.
116. List A.F., Kopecky K.J., Willman C.L., Head D.R., Persons D.L., Slovak M.L., Dorr R., Karanes C., Hynes H.E., Doroshow J., Shurafa M., Appelbaum F.R. Benefit of cyclosporinc modulation of drug resistance in patients with poor-risk acute myeloid leukemia: a Southwest Oncology Group study. Blood. 98:2001;3212-3220.
117. J.E. Kolitz, S.L. George, R.K. Dodge, E. Hoke, D.D. Hurd, L.P. Bayard, E. Velez-Garcia, M.A. Caligiuri, J.O. Moore, J.W. Vardiman, C.D. Bloomfield, R.A. Larson, [Abstract #1928] Dose escalation studies of ara-C (A), daunorubicin (D) and etoposide (E) with and without multidrug resistance (MDR) modulation with PSC-833 (P) in untreated adults with acute myeloid leukemia (AML) <60 Years: Final induction results of CALGB 9621. in Am. Soc. of Hematology. Orlando, FL, 2001.
118. Norman B.H., Gruber J.M., Hollinshead S.P., Wilson J.W., Starling J.J., Law K.L., Self T.D., Tabas L.B., Williams D.C., Paul D.C., Wagner M.M., Dantzig A.H. Tricyclic isoxazoles are novel inhibitors of the multidrug resistance protein (MRP1). Bioorg. Med. Chem. Lett. 12:2002;883-886.
119. Jansen W.J.M., Hulscher T.M., van Ark-Otte J., Giaccone G., Pinedo H.M., Boven E. CPT-11 sensitivity in relation to the expression of P170-glycoprotein and multidrug resistance-associated protein. Br. J. Cancer. 77:1998;359-365.
120. Mahon F.X., Deininger M.W.N., Schultheis B., Chabrol J., Reiffers J., Goldman J.M., Melo J.V. Selection and characterization of BCR-ABL positive cell lines with differential sensitivity to the tyrosine kinase inhibitor STI571: diverse mechanisms of resistance. Blood. 96:2000;1070-1079.
121. Sandor V., Fojo T., Bates S.E. Future perspectives for the development of Pglycoprotein modulators. Drug Resistance Updates. 1:1998;190-200.
122. de Jong M.C., Slootstra J.W., Scheffer G.L., Schroeijers A.B., Puijk W.C., Dinkelberg R., Icool M., Broxterman H.J., Meloen R.H., Scheper R.J. Peptide transport by the multidrug resistance protein MRP1. Cancer Res. 61:2001;2552-2557.