Carvedilol: A new candidate for reversal of MDR1/P-glycoprotein-mediated multidrug resistance

Anti-Cancer Drugs

Volumn 15, Issue 4, 2004, Pages 303-309

  Takara, Kohji ^a,b   Sakaeda, Toshiyuki ^a   Okumura, Katsuhiko ^a  

^a KOBE UNIVERSITY   (Japan)

^b KYOTO PHARMACEUTICAL UNIVERSITY   (Japan)

Author keywords

adrenoceptor antagonist; Antioxidant; Carvedilol; CYP3A4; MDR1 P glycoprotein; Multidrug resistance

Indexed keywords

ATENOLOL; BIRICODAR; CARVEDILOL; DAUNORUBICIN; DEXVERAPAMIL; DOXORUBICIN; FLUOROURACIL; GLYCOPROTEIN P; METOPROLOL; MULTIDRUG RESISTANCE PROTEIN 1; PROPRANOLOL; TARIQUIDAR; VALSPODAR; VERAPAMIL; VINBLASTINE; ZOSUQUIDAR;

CLINICAL TRIAL; CORONARY ARTERY DISEASE; DRUG ACTIVITY; DRUG EFFICACY; DRUG POTENCY; DRUG SAFETY; DRUG SELECTIVITY; HEART LEFT VENTRICLE FAILURE; HUMAN; HYPERTENSION; OVARY CARCINOMA; PRIORITY JOURNAL; REVIEW;

ADRENERGIC BETA-ANTAGONISTS; ARYL HYDROCARBON HYDROXYLASES; CARBAZOLES; CLINICAL TRIALS; CYTOCHROME P-450 CYP3A; DRUG RESISTANCE, MULTIPLE; DRUG RESISTANCE, NEOPLASM; HUMANS; NEOPLASMS; OXIDOREDUCTASES, N-DEMETHYLATING; P-GLYCOPROTEIN; PROPANOLAMINES; RECEPTORS, ADRENERGIC, BETA; SUBSTRATE SPECIFICITY;

EID: 1942421254     PISSN: 09594973     EISSN: None     Source Type: Journal    
DOI: 10.1097/00001813-200404000-00001     Document Type: Review

References (87)

1. Sponer G, Bartsch W, Strain K, Muller-Beckmann B, Bohm E Pharmacological profile of carvedilol as a beta-blocking agent with vasodilating and hypotensive properties. J Cardiovasc Pharmacol 1987; 9:317-327.
2. McTavish D, Campoli-Richards D, Sorkin EM. Carvedilol. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy. Drugs 1993; 45:232-258.
3. Dunn CJ, Lea AP, Wagstaff AJ. Carvedilol. A reappraisal of its pharmacological properties and therapeutic use in cardiovascular disorders. Drugs 1997; 54:161-185.
4. Batlouni M, de Albuquerque DC. Beta-adrenergic blocking agents in heart failure. Arq Bras Cardiol 2000; 75:339-360.
5. Bristow MR. Beta-adrenergic receptor blockade in chronic heart failure. Circulation 2000; 101:558-569.
6. Fowler M. Beta-adrenergic blocking drugs in severe heart failure. Rev Cardiovasc Med 2002; 3(suppl 3):S20-S26.
7. Yue TL, Cheng HY, Lysko PG, et al. Carvedilol, a new vasodilator and beta adrenoceptor antagonist, is an antioxidant and free radical scavenger. J Pharmacol Exp Ther 1992; 263:92-98.
8. Cheng J, Kamiya K, Kodama I. Carvedilol: molecular and cellular basis for its multifaceted therapeutic potential. Cardiovasc Drug Rev 2001; 19:152-171.
9. Nakamura K, Kusano K, Nakamura Y, et al. Carvedilol decreases elevated oxidative stress in human failing myocardium. Circulation 2002; 105:2867-2871.
10. Yue TL, McKenna PJ, Lysko PG, Ruffolo Jr RR, Feuerstein GZ. Carvedilol, a new antihypertensive, prevents oxidation of human low density lipoprotein by macrophages and copper. Atherosclerosis 1992; 97:209-216.
11. Yue TL, Mckenna PJ, Lysko PG, et al. SB 211475, a metabolite of carvedilol, a novel antihypertensive agent, is a potent antioxidant. Eur J Pharmacol 1994; 251:237-243.
12. Constant J. A review of why and how we may use beta-blockers in congestive heart failure. Chest 1998; 113:800-808.
13. Neugebauer G, Akpan W, von Wollendorff E, Neubert P, Reiff K. Pharmacokinetics and disposition of carvedilol in humans. J Cardiovasc Pharmacol 1987; 10(suppl 11):S85-S88.
14. von Mollendorff E, Reiff K, Neugebauer G. Pharmacokinetics and bioavailability of carvedilol, a vasodilating beta-blocker. Eur J Clin Pharmacol 1987; 33:511-513.
15. Oldham HG, Clarke SE. In vitro identification of the human cytochrome P450 enzymes involved in the metabolism of R(+)-and S(-)-carvedilol. Drug Metab Dispos 1997; 25:970-977.
16. Cubeddu LX, Fuenmayor N, Varin F, Villagra VG, Colindres RE, Powell JR. Clinical pharmacology of carvedilol in normal volunteers. Clin Pharmacol Ther 1987; 41:31-44.
17. McPhillips JJ, Schwemer GT, Scott DI, Zinny M, Patterson D. Effects of carvedilol on blood pressure in patients with mild to moderate hypertension. A dose response study. Drugs 1988; 36(suppl 6):82-91.
18. Abraham WT, Scarpinato L Higher expectations for management of heart failure: current recommendations. J Am Board Fam Pract 2002; 15:39-49.
19. Cesario DA, Fonarow GC. Beta-blocker therapy for heart failure: the standard of care. Rev Cardiovasc Med 2002; 3:14-21.
20. Jonsson O, Behnam-Motlagh P, Persson M, Henriksson R, Grankvist K. Increase in doxorubicin cytotoxicity by carvedilol inhibition of P-glycoprotein activity. Biochem Pharmacol 1999; 58:1801-1806.
21. Kakumoto M, Sakaeda T, Takara K, et al. Effects of carvedilol on MDR1-mediated multidrug resistance: comparison with verapamil. Cancer Sci 2003; 94:81-86.
22. Geney R, Ungureanu M, Li D, Ojima I. Overcoming multidrug resistance in taxane chemotherapy. Clin Chem Lab Med 2002; 40:918-925.
23. Goldman B. Multidrug resistance: can new drugs help chemotherapy score against cancer? J Natl Cancer Inst 2003; 95:255-257.
24. Mattern J. Drug resistance in cancer: a multifactorial problem. Anticancer Res 2003; 23:1769-1772.
25. Shen D, Pastan I, Gottesman MM. Cross-resistance to methotrexate and metals in human cisplatin-resistant cell lines results from a pleiotropic defect in accumulation of these compounds associated with reduced plasma membrane binding proteins. Cancer Res 1998; 58:268-275.
26. Persidis A. Cancer multidrug resistance. Nat Biotechnol 1999; 17:94-95.
27. Ueda K, Yoshida A, Amachi T. Recent progress in P-glycoprotein research. Anticancer Drug Des 1999; 14:115-121.
28. Bush JA, Li G. Cancer chemoresistance: the relationship between p53 and multidrug transporters. Int J Cancer 2002; 98:323-330.
29. Liem AA, Chamberlain MP, Wolf CR, Thompson AM. The role of signal transduction in cancer treatment and drug resistance. Eur J Surg Oncol 2002; 28:679-684.
30. Tsuruo T, Naito M, Tomida A, et al. Molecular targeting therapy of cancer: drug resistance, apoptosis and survival signal. Cancer Sci 2003; 94:15-21.
31. Ejendal KF, Hrycyna CA. Multidrug resistance and cancer: the role of the human ABC transporter ABCG2. Curr Protein Pept Sci 2002; 3:503-511.
32. Gottesman MM, Fojo T, Bates SE. Multidrug resistance in cancer: role of ATP-dependent transporters. Nat Rev Cancer 2002; 2:48-58.
33. Stein WD. Reversers of the multidrug resistance transporter P-glycoprotein. Curr Opin Invest Drugs 2002; 3:812-817.
34. Sharma R, Awasthi YC, Yang Y, Sharma A, Singhal SS, Awasthi S. Energy dependent transport of xenobiotics and its relevance to multidrug resistance. Curr Cancer Drug Targets 2003; 3:89-107.
35. Sparreboom A, Danesi R, Ando Y, Chan J, Figg WD. Pharmacogenomics of ABC transporters and its role in cancer chemotherapy. Drug Resist Update 2003; 6:71-84.
36. Juliano RL, Ling V. A surface glycoprotein modulating drug permeability in Chinese hamster ovary cell mutants. Biochim Biophys Acta 1976; 455:152-162.
37. Sakaeda T, Nakamura T, Okumura K. Pharmacogenetics of MDR1 and its impact on the pharmacokinetics and pharmacodynamics of drugs. Pharmacogenomics 2003; 4:397-410.
38. Tsuruo T, Iida H, Tsukagoshi S, Sakurai Y. Overcoming of vincristine resistance in P388 leukemia in vivo and in vitro through enhanced cytotoxicity of vincristine and vinblastine by verapamil. Cancer Res 1981; 41:1967-1972.
39. Rogan AM, Hamilton TC, Young RC, Klecker Jr RW, Ozols RF. Reversal of adriamycin resistance by verapamil in human ovarian cancer. Science 1984; 224:994-996.
40. Watanabe T, Tsuge H, Oh-Hara T, Naito M, Tsuruo T. Comparative study on reversal efficacy of SDZ PSC 833, cyclosporin A and verapamil on multidrug resistance in vitro and in vivo. Acta Oncol 1995; 34:235-241.
41. Germann UA, Shlyakhter D, Mason VS, et al. Cellular and biochemical characterization of VX-710 as a chemosensitizer: reversal of P-glycoprotein-mediated multidrug resistance in vitro. Anticancer Drugs 1997; 8:125-140.
42. Rowinsky EK, Smith L, Wang YM, et al. 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 1998; 16:2964-2976.
43. Thomas H, Coley HM. Overcoming multidrug resistance in cancer: an update on the clinical strategy of inhibiting P-glycoprotein. Cancer Control 2003; 10:159-165.
44. Fischer V, Rodriguez-Gascon A, Heitz F, et al. The multidrug resistance modulator valspodar (PSC 833) is metabolized by human cytochrome P450 3A. Implications for drug-drug interactions and pharmacological activity of the main metabolite. Drug Metab Dispos 1998; 26:802-811.
45. Achira M, Suzuki H, Ito K, Sugiyama Y. Comparative studies to determine the selective inhibitors for P-glycoprotein and cytochrome P4503A4. AAPS PharmSci 1999; 1:E18.
46. Wacher VJ, Wu CY, Benet LZ. Overlapping substrate specificities and tissue distribution of cytochrome P450 3A and P-glycoprotein: implications for drug delivery and activity in cancer chemotherapy. Mol Carcinogen 1995; 13:129-134.
47. Wacher VJ, Silverman JA, Zhang Y, Benet LZ. Role of P-glycoprotein and cytochrome P450 3A in limiting oral absorption of peptides and peptidomimetics. J Pharm Sci 1998; 87:1322-1330.
48. Wandel C, Kim RB, Kajiji S, Guengerich P, Wilkinson GR, Wood AJ. P-glycoprotein and cytochrome P-450 3A inhibition: dissociation of inhibitory potencies. Cancer Res 1999; 59:3944-3948.
49. Kim RB, Wandel C, Leake B, et al. Interrelationship between substrates and inhibitors of human CYP3A and P-glycoprotein. Pharm Res 1999; 16:408-414.
50. Tran CD, Timmins P, Conway BR, Irwin WJ. Investigation of the coordinated functional activities of cytochrome P450 3A4 and P-glycoprotein in limiting the absorption of xenobiotics in Caco-2 cells. J Pharm Sci 2002; 91:117-128.
51. Yasuda K, Lan LB, Sanglard D, Furuya K, Schuetz JD, Schuetz EG. Interaction of cytochrome P450 3A inhibitors with P-glycoprotein. J Pharmacol Exp Ther 2002; 303:323-332.
52. Dantzig AH, Shepard RL, Cao J, et al. Reversal of P-glycoprotein-mediated multidrug resistance by a potent cyclopropyldibenzosuberane modulator, LY335979. Cancer Res 1996; 56:4171-4179.
53. van Zuylen L, Sparreboom A, van der Gaast A, et al. The orally administered P-glycoprotein inhibitor R101933 does not alter the plasma pharmacokinetics of docetaxel. Clin Cancer Res 2000; 6:1365-1371.
54. Mistry P, Stewart AJ, Dangerfield W, et al. In vitro and in vivo reversal of P-glycoprotein-mediated multidrug resistance by a novel potent modulator, XR9576. Cancer Res 2001; 61:749-758.
55. van Zuylen L, Sparreboom A, van der Gaast A, et al. Disposition of docetaxel in the presence of P-glycoprotein inhibition by intravenous administration of R101933. Eur J Cancer 2002; 38:1090-1099.
56. Mistry P, Folkes A. ONT-093 (Ontogen). Curr Opin Invest Drugs 2002; 3:1666-1671.
57. Thiebaut F, Tsuruo T, Hamada H, Gottesman MM, Pastan I, Willingham MC. Cellular localization of the multidrug-resistance gene product P-glycoprotein in normal human tissues. Proc Natl Acad Sci USA 1987; 84:7735-7738.
58. Benet LZ, Izumi T, Zhang Y, Silverman JA, Wacher VJ. Intestinal MDR transport proteins and P-450 enzymes as barriers to oral drug delivery. J Control Release 1999; 62:25-31.
59. Zhang Y, Benet LZ. The gut as a barrier to drug absorption: combined role of cytochrome P450 3A and P-glycoprotein. Clin Pharmacokinet 2001; 40:159-168.
60. Fromm MF. The influence of MDR1 polymorphisms on P-glycoprotein expression and function in humans. Adv Drug Deliv Rev 2002; 54:1295-1310.
61. Zhang Y, Guo X, Lin ET, Benet LZ. Overlapping substrate specificities of cytochrome P450 3A and P-glycoprotein for a novel cysteine protease inhibitor. Drug Metab Dispos 1998; 26:360-366.
62. Zhou-Pan XR, Seree E, Zhou XJ, et al. Involvement of human liver cytochrome P450 3A in vinblastine metabolism: drug interactions. Cancer Res 1993; 53:5121-5126.
63. Zhou XJ, Zhou-Pan XR, Gauthier T, Placidi M, Maurel P, Rahmani R. Human liver microsomal cytochrome P450 3A isozymes mediated vindesine biotransformation. Metabolic drug interactions. Biochem Pharmacol 1993; 45:853-861.
64. Relling MV, Nemec J, Schuetz EG, Schuetz JD, Gonzalez FJ, Korzekwa KR. O-demethylation of epipodophyllotoxins is catalyzed by human cytochrome P450 3A4. Mol Pharmacol 1994; 45:352-358.
65. Achira M, Suzuki H, Ito K, Sugiyama Y. Comparative studies to determine the selective inhibitors for P-glycoprotein and cytochrome P4503A4. AAPS PharmSci 1999; 1:E18.
66. Takara K, Kakumoto M, Tanigawara Y, Funakoshi J, Sakaeda T, Okumura K. Interaction of digoxin with antihypertensive drugs via MDR1. Life Sci 2002; 70:1491-1500.
67. Westphal K, Weinbrenner A, Zschiesche M, et al. Induction of P-glycoprotein by rifampin increases intestinal secretion of talinolol in human beings: a new type of drug/drug interaction. Clin Pharmacol Ther 2000; 68:345-355.
68. Karisson J, Kuo SM, Ziemniak J, Artursson P. Transport of celiprolol across human intestinal epithelial (Caco-2) cells: mediation of secretion by multiple transporters including P-glycoprotein. Br J Pharmacol 1993; 110:1009-1016.
69. Neuhoff S, Langguth P, Dressier C, Andersson TB, Regardh CG, Spahn-Langguth H. Affinities at the verapamil binding site of MDR1 -encoded P-glycoprotein: drugs and analogs, stereoisomers and metabolites. Int J Clin Pharmacol Ther 2000; 38:168-179.
70. Lilja JJ, Backman JT, Laitila J, Luurila H, Neuvonen PJ. Itraconazole increases but grapefruit juice greatly decreases plasma concentrations of celiprolol. Clin Pharmacol Ther 2003; 73:192-198.
71. Hirsch-Ernst KI, Ziemann C, Foth H, Kozian D, Schmitz-Salue C, Kahl GF. Induction of mdr1b mRNA and P-glycoprotein expression by tumor necrosis factor alpha in primary rat hepatocyte cultures. J Cell Physiol 1998; 176:506-515.
72. Ziemann C, Burkle A, Kahl GF, Hirsch-Ernst KI. Reactive oxygen species participate in mdr1b mRNA and P-glycoprotein overexpression in primary rat hepatocyte cultures. Carcinogenesis 1999; 20:407-414.
73. Thevenod F, Friedmann JM, Katsen AD, Hauser IA. Up-regulation of multidrug resistance P-glycoprotein via nuclear factor-kappaB activation protects kidney proximal tubule cells from cadmium-and reactive oxygen species-induced apoptosis. J Biol Chem 2000; 275:1887-1896.
74. Liu YW, Sakaeda T, Takara K, et al. Effects of reactive oxygen species on cell proliferation and death in HeLa cells and its MDR1 -overexpressing derivative cell Line. Biol Pharm Bull 2003; 26:278-281.
75. Brouillard F, Tondelier D, Edelman A, Baudouin-Legros M. Drug resistance induced by ouabain via the stimulation of MDR1 gene expression in human carcinomatous pulmonary cells. Cancer Res 2001; 61:1693-1698.
76. Takara K, Tsujimoto M, Ohnishi N, Yokoyama T. Digoxin up-regulates MDR1 in human colon carcinoma Caco-2 cells. Biochem Biophys Res Commun 2002; 292:190-194.
77. Asghar A, Gorski JC, Haehner-Daniels B, Hall SD. Induction of multidrug resistance-1 and cytochrome P450 mRNAs in human mononuclear cells by rifampin. Drug Metab Dispos 2002; 30:20-26.
78. Dresser GK, Schwarz UI, Wilkinson GR, Kim RB. Coordinate induction of both cytochrome P4503A and MDR1 by St John's wort in healthy subjects. Clin Pharmacol Ther 2003; 73:41-50.
79. Synold TW, Dussault I, Forman BM. The orphan nuclear receptor SXR coordinately regulates drug metabolism and efflux. Nat Med 2001; 7:584-590.
80. Labialle S, Gayet L, Marthinet E, Rigal D, Baggetto LG. Transcriptional regulators of the human multidrug resistance 1 gene: recent views. Biochem Pharmacol 2002; 64:943-948.
81. Labialle S, Gayet L, Marthinet E, Rigal D, Baggetto LG. Transcriptional regulation of the human MDR1 gene at the level of the inverted MED-1 promoter region. Ann NY Acad Sci 2002; 973:468-471.
82. Dussault I, Lin M, Hollister K, Wang EH, Synold TW, Forman BM. Peptide mimetic HIV protease inhibitors are ligands for the orphan receptor SXR. J Biol Chem 2001; 276:33309-33312.
83. Ekins S, Erickson JA. A pharmacophore for human pregnane X receptor ligands. Drug Metab Dispos 2002; 30:96-99.
84. Takara K, Takagi K, Tsujimoto M, Ohnishi N, Yokoyama T. Digoxin up-regulates multidrug resistance transporter (MDR1) mRNA and simultaneously down-regulates steroid xenobiotic receptor mRNA. Biochem Biophys Res Commun 2003; 306:116-120.
85. Yague E, Armesilla AL, Harrison G, et al. P-glycoprotein (MDR1) expression in leukemic cells is regulated at two distinct steps, mRNA stabilization and translational initiation. J Biol Chem 2003; 278:10344-10352.
86. Jenkins RR, Del Signore CM, Sauer P, Skelly C. The effect of beta blocking drugs on lipid peroxidation in rat heart in vitro. Lipids 1992; 27:539-542.
87. Gao F, Chen J, Lopez BL, et al. Comparison of bisoprolol and carvedilol cardioprotection in a rabbit ischemia and reperfusion model. Eur J Pharmacol 2000; 406:109-116.