Tesmilifene may enhance breast cancer chemotherapy by killing a clone of aggressive, multi-drug resistant cells through its action on the p-glycoprotein pump

Medical Hypotheses

Volumn 66, Issue 4, 2006, Pages 715-731

  Vincent, Mark ^a  

^a LONDON REGIONAL CANCER PROGRAM   (Canada)

Author keywords

[No Author keywords available]

Indexed keywords

ANTHRACYCLINE; CISPLATIN; CYCLOPHOSPHAMIDE; CYTOCHROME P450 1A1; CYTOCHROME P450 2D6; CYTOCHROME P450 3A4; DAUNORUBICIN; DOCETAXEL; DOXORUBICIN; EPIRUBICIN; ESTROGEN; ESTROGEN RECEPTOR; FLUOROURACIL; GLYCOPROTEIN P; METHANE; MITOXANTRONE; PACLITAXEL; PREDNISONE; REACTIVE OXYGEN METABOLITE; RHODAMINE; TAXANE DERIVATIVE; TESMILIFENE; TRASTUZUMAB; VERAPAMIL;

ARTICLE; ATAXIA; BREAST CANCER; CANCER CELL; CANCER CHEMOTHERAPY; CANCER GROWTH; CANCER SURVIVAL; CARDIOTOXICITY; CLINICAL TRIAL; ELECTRON TRANSPORT; HALLUCINATION; HUMAN; MOTION SICKNESS; MULTIDRUG RESISTANCE; PRIORITY JOURNAL; PROSTATE CANCER; RECURRENT DISEASE; SURVIVAL RATE;

ANTINEOPLASTIC COMBINED CHEMOTHERAPY PROTOCOLS; ATP-BINDING CASSETTE TRANSPORTERS; BREAST NEOPLASMS; CLINICAL TRIALS; DRUG RESISTANCE, MULTIPLE; DRUG RESISTANCE, NEOPLASM; FEMALE; HUMANS; PHENYL ETHERS;

ATAXIA;

EID: 31844444483     PISSN: 03069877     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.mehy.2005.11.005     Document Type: Article

References (96)

1. L. Reyno, L. Seymour, and D. Tu Phase III study of N,N-diethyl-2-[4- (phenylmethyl)phenoxy] ethanamine (BMS-217380-01) combined with doxorubicin versus doxorubicin alone in metastatic/recurrent breast cancer: National Cancer Institute of Canada Clinical Trials Group Study MA. 19 J Clin Oncol 22 2004 269 276
2. M. Marty, F. Cognetti, and D. Maraninchi Randomized phase II trial of the efficacy and safety of trastuzumab combined with docetaxel in patients with human epidermal growth factor receptor 2-positive metastatic breast cancer administered as first-line treatment: the M77001 study group J Clin Oncol 23 2005 4265 4274
3. D.J. Slamon, B. Leyland-Jones, and S. Shak Randomized phase II trial of the efficacy and safety of trastuzumab combined with docetaxel in patients with human epidermal growth factor receptor 2-positive metastatic breast cancer administered as first-line treatment: the M77001 study group J Clin Oncol 23 2005 4265 4274
4. Y. Yamaguchi, K. Hironaka, and M. Okawaki HER2-specific cytotoxic activity of lymphokine-activated killer cells in the presence of trastuzumab Anticancer Res 25 2A 2005 827 832
5. J.A. Menendez, L. Vellon, and R. Lupu Targeting fatty acid synthase-driven lipid rafts: a novel strategy to overcome trastuzumab resistance in breast cancer cells Med Hypoth 64 2005 997 1001
6. C.T. Chan, M.Z. Metz, and S.E.I. Kane Differential sensitivities of trastuzumab (Herceptin)-resistant human breast cancer cells to phosphoinositide-3 kinase (P1-3K) and epidermal growth factor receptor (EGFR-kinase inhibitors Br Cancer Res Treat 91 2005 187 201
7. K.E. Longva, N.M. Pedersen, and C. Haslekas Herceptin-induced inhibition of ErbB2 signaling involves reduced phosphorylation of Akt but not endocytic down-regulation of ErbB2 Int J Cancer 116 2005 359 367
8. M. Vincent, P. Keane, H. Chen, and K. Pritchard Subgroup analysis of a phase III trial of doxorubicin plus tesmilifene in advanced breast cancer (ABC): Tesmilifene survival benefit focused on patients with more aggressive disease Proc ASCO 23 S16 I 2005 #756 p 67s.
9. Brandes LJ. Personal communication, 2005.
10. E.A. Kroeger, and L.J. Brandes Evidence that tamoxifen is a histamine antagonist Biochem Biophys Res Commun 131 1985 750 751
11. L.J. Brandes, F.S. LaBella, and R.C. Warrington Increased therapeutic index of antineoplastic drugs in combination with intracellular histamine antagonists JNCI 83 1991 1326 1329
12. A.T. Menendez, C. Raventos-Suarex, and C. Fairchild Mechanism of action of DPPE, a chemosensitizing agent Proc Am Assoc Cancer Res 39 1998 3462 (abstr)
13. K. Kudoh, and Y. Kikuchi Enhancement of antitumour activity of cisplatin by N,N-diethyl-2-[4-(phenylmethyl)phenoxy] ethanamine-HCl in human ovarian cancer cells with intrinsic or acquired resistance to cisplatin Eur J Cancer 33 1997 122 128
14. Ferguson P., et al. Data in-house. YM Biosciences, 2004.
15. J.A. Jones, K.D. Albright, R.D. Christen, S.B. Howell, and E.F. McClay Synergy between tamoxifen and cisplatin in human melanoma cells is dependent on the presence of antiestorgen-binding sites Cancer Res 57 1997 2657 2660
16. L.J. Brandes A diphenylmethane derivative selective for the anti-estrogen binding site may help define its biological role Biochem Biophys Res Commun 124 1989 244 249
17. L.J. Brandes, and M.W. Hermanouet A diphenylmethane derivative specific for the antiestrogen binding site found in rat liver microsomes Biochem Biophys Res Commun 123 1984 724 728
18. L.J. Brandes, G.M. Queen, and F.S. LaBella N,N-diethyl-2-[4- (phenylmethyl] ethanamine (DPPE), a chemopotentiating and cytoprotective agent in clinical trials: interaction with histamine at cytoprotective agent in clinical trials: interaction with histamine at cytochrome P450 3A4 and other isozymes that metabolize antineoplastic drugs Cancer Chemother Pharmacol 45 2000 298 304
19. Bristol Myers Squibb/YM Biosciences data in-house, 1997.
20. Wang JC, Liu XY, Lu WL., et al. Pharmacokinetics of intravenously administered stealth liposomal doxorubicin modulated with verapamil in rats. Eur J Pharm Biopharm 2005; Aug 26: [Epub ahead of print].
21. Darvais R, Baronjerdi M. Cancer Chemother Pharmacol 2005; June 4 [Epub ahead of print].
22. A. Sandler, M. Gordon, and D.P. De Alwis A phase I trial of a potent p-glycoprotein inhibitor, zosuquidar trihydrochloride (LY335979), administered intravenously in combination with doxorubicin in patients with advanced malignancy Clin Cancer Res 10 2004 3265 3272
23. S.E. Bates, W.H. Wilson, and A.T. Foju Clinical reversal of multidrug resistance The Oncologist 1 1996 269 275
24. B.I. Sikic, G.A. Fishe, and B.L. Lum Modulation and prevention of multidrug resistance by inhibitors of P-glycoprotein Cancer Chemother Pharmacol 40 Suppl. 1997 S13 S19
25. B. Kedjouar, P. de Dedina, and M. Oulad-Abdelghani Molecular characterization of the microsomal tamoxifen binding site J Biol Chem 279 2004 34048 34061
26. P.J. Ferguson, and M.D. Vincent Enhancement of docetaxel cytotoxicity in multidrug resistant variant cell lines of human head and neck squamous cell carcinoma HN-5a and promyelocytic leukemia HL-60 by N,N-diethyl-2-[4- phenylmethyl)phenoxyl]ethanamine (DPPE; Tesmilifene) Proc Am Asso Cancer Res 46 2005 127 abstract
27. L.J. Brandes, K.J. Simons, S.P. Bracken, and R.C. Warrington Results of a clinical trial in humans with refractory cancer of the intracellular histamine antagonist, N,N-diethyl-2-[4-(phenylmethyl) phenoxy]ethanamine-HCI, in combination with various single antineoplastic agents J Clin Oncol 12 6 1994 1281 1290
28. G.B. Glavin, and J.M. Gerrard Characterization of the gastroprotective effects of N,N-diethyl-2-[4-(phenylmethyl)phenoxy]-ethanamine hydrochloride, a non-H1/non-H2 histamine antagonist Digestion 47 1990 143 148
29. L.J. Brandes, K.A. McDonald, and S.P. Bracken Results of a human pilot study testing the hypothesis that the intracellular histamine antagonist DPPE increases the therapeutic index of doxorubicin Adv Biosci 89 1993 375 401
30. L. Brandes, and S. Bracken The intracellular histamine antagonist, N,N-diethyl-2-[4-(phenylmethyl)phenoxy] ethanamine. HCl, may potentiate doxorubicin in the treatment of metastatic breast cancer: Results of a pilot study Br Cancer Res Treat 49 1998 61 68
31. K. Khoo, L. Brandes, and L. Reyno Phase II trial of N,N-diethyl-2-[4- (phenylmethyl)phenoxy]ethanamine. HCl and doxorubicin chemotherapy in metastatic breast cancer: A National Cancer Institute of Canada clinical trials group study J Clin Oncol 17 1999 3431 3437
32. Santome L, Tabernero J, Riofrio M, et al. Continuing improvement of efficacy with single-agent paclitaxel (T) after discontinuation of doxorubicin (A) in patients (pts) with metastatic or locally advanced breast cancer (ABC) treated with that combination. In: Proc ASCO 2001:20; abstract 1994.
33. L.J. Brandes, S.P. Bracken, and E.W. Ramsey N,N-diethyl-2-[4- (phenylmethyl)phenoxy]ethanamine in combination with cyclophosphamide: an active, low-toxicity regimen for metastatic hormonally unresponsive prostate cancer J Clin Oncol 1995 1398 1403
34. L.J. Brandes, D. Raghaven, and K. Klapp Apparently increased anticancer efect in phase II trial of mitoxantrone-DPPE for symptomatic hormone-refractory prostate cancer (Cap) Proc ASCO 19 2000 378a abstract 1496A
35. I.F. Tannock, D. Osoba, and M.R. Stockler Chemotherapy with mitoxantrone plus prednisone or prednisone alone for symptomatic hormone-resistant prostate cancer: a Canadian randomized trial with palliative end points J Clin Oncol 14 1996 1756 1764
36. J.F. Bishop, J. Dewar, and G.C. Toner Initial paclitaxel improves outcome compared with CMFP combination chemotherapy as front-line therapy in untreated metastatic breast cancer J Clin Oncol 17 1999 2355 2364
37. M.J. Moore, D. Goldstein, and J. Hamm Erlotinib plus gemcitabine compared to gemcitabine alone in patients with advanced pancreatic cancer. A phase III trial of the National Cancer Institute of Canada Clinical Trials Group (NCIC-CTG Proc ASCO 24 2005 abstract
38. Chintamani, J.P. Singh, and M.K. Mittal Role of p-glycoprotein expression in predicting response to neoadjuvant chemotherapy in breast cancer - a prospective clinical study World J Surg Oncol 3 2005 61
39. M. Greaves Cancer. The evolutionary legacy 2000 Oxford University Press Oxford 35 41
40. K. Albain Adjuvant chemo hormonal therapy for primary breast cancer should be sequential instead of concurrent: Initial results from Intergroup trial 0100/SWOG-8814 Proc ASCO 21 2002 37a abstract 143
41. J.R. Waddle, R.L. Fine, and B.C. Case Phase I and pharmocokinetic analysis of high-dose tamoxifen and chemotherapy in normal and tumor-bearing dogs Cancer Chemother Pharm 44 1999 74 80
42. L.J. Brandes, G.M. Queen, and F.S. LaBella Potent interaction of histamine and polyamines at microsomal cytochrome P450, nuclei, and chromatin from rat hepatocytes J Cell Biochem 69 1998 233 243
43. M. Baumhakel, D. Kasel, and R.A. Rao-Schymanski Screening for inhibitory effects of antineoplastic agents on CYP3A4 in human liver microsomes Int J Clin Pharmacol Ther 39 2001 517 528
44. E.G. Schuetz, W.T. Beck, and J.D. Schuetz Modulators and substrates of P-glycoprotein and cytochrome P4503A coordinately up-regulate these proteins in human colon carcinoma cells Mol Pharmacol 49 1996 311 318
45. V.J. Wacher, C.-Y. Wu, and L.Z. Benet Overlapping substrate specificities and tissue distribution of cytochrome P450 3A and P-glycoprotein: implications for drug delivery and activity in cancer chemotherapy Mol Carcinogen 13 1995 129 134
46. O. Polgar, and S.E. Bates ABC transporters in the balance: is there a role in multidrug resistance? Biochem Soc Trans 33 Pt 1 2005 241 245
47. L. Puszlai, P. Wagner, and N. Ibrahim Phase II study of tariquidar, a selective P-glycoprotein inhibitor, in patients with chemotherapy-resistant, advanced breast carcinoma Cancer 104 2005 682 692
48. K. Garber Energy boost: the Warburg effect returns in a new theory of cancer JNCI 96 2004 1805 1806
49. O. Warburg Ist die aerobe glykolyse spezifisch fuer die Tumoren Biochem 2 204 1929 482 483
50. O. Warburg On the origin of cancer cells Science 123 1956 309 314
51. P. Manders, P. Bult, C.G. Sweep, V.C. Tjan-Heinjnen, and L.V. Beex The prognostic value of the mitotic activity index in patients with primary breast cancer who were not treated with adjuvant systemic therapy Breast Cancer Res Treat 77 2003 77 84
52. S.C. Linn, G. Ciacone, and P.J. van Diest Prognostic relevance of P-glycoprotein expression in breast cancer Ann Oncol 6 1995 679 685
53. M. Banerjee, J. George, and E.Y. Song Tree based model for breast cancer prognostication J Clin Oncol 22 2004 2567 2575
54. M. Filipts, G. Pohl, and M. Rudas Clinical role of multidrug resistance protein 1 expression in chemotherapy resistance in early-stage breast cancer: The Austrian Breast and Colorectal Cancer Study Group J Clin Oncol 23 2005 1161 1168
55. A. Larkin, L. O'Driscoll, and S. Kennedy Investigation of MRP-1 protein and MDR-1 P-glycoprotein expression in invasive breast cancer: A prognostic study Int J Cancer 112 2004 286 294
56. B. Punyammalee, S. Manoromana, and W. Purisa Association of mdr1 gene expression with other prognostic factors and clinical outcome in human breast cancer J Med Assoc Thai 80 Suppl. 1 1997 S162 S173
57. F. Tsukamoto, E. Shiba, and T. Taguchi Immunohistochemical detection of P-glycoprotein in breast cancer and its significance as a prognostic factor Breast Cancer 4 1997 259 263
58. B.J. Trock, F. Leonessa, and R. Clarke Multidrug resistance in breast cancer: a meta-analysis of MDR1/gp170 expression and its possible functional significance JNCI 89 1997 917 931
59. T. Litman, T. Zeuthen, T. Skovsgaard, and W.D. Stein Structure-activity relationships of P-glycoprotein interacting drugs: kinetic characterization of their effects on ATPase activity Biochem Biophys Acta 1361 1997 159 168
60. A. Ramu, and N. Ramu Reversal of multidrug resistance by phenothiazines and structurally related compounds Cancer Chemother Pharmacol 30 1992 165 173
61. J. Karwatsky, M.C. Lincoln, and E. Georges A mechanism for p-glycoprotein-mediated apoptosis as revealed by verapamil hypersensitivity Biochemistry 42 2003 12163 12173
62. N.T. Bech-Hansen Pleiotropic phenotype of colchicine-resistant CHO cells: cross-resistance and collateral sensitivity J Cell Physiol 88 1976 31 32
63. D.R. Cano-Gauci, and J.R. Riordan Action of calcium antagonists on multidrug resistant cells. Specific cytotoxicity independent of increased cancer drug accumulation Biochem Pharmacol 36 1987 2115 2123
64. J.R. Warr, M. Anderson, and J. Fergusson Properties of verapamil-hypersensitive multidrug-resistant Chinese hamster ovary cells Cancer Res 48 1988 4477 4483
65. M. Barancik, P. Docolomansky, J. Slezak, and A. Breier Overcoming of vincristine resistance in L1210/VCR cells by several corticosteroids. Collateral sensitivity of resistant cells Neoplasma 40 1993 21 25
66. H. Riehm, and J.L. Biedler Potentiation of drug effect by Tween 80 in Chinese hamster cells resistant to actinomycin D and daunomycin Cancer Res 32 1972 1195 1200
67. T.W. Loo, M.C. Bartlerr, and D.M. Clarke Methanethiosulfonate derivatives of rhodamine and verapamil activate human p-glycoprotein at different sites J Biol Chem 278 2003 50136 50141
68. G.D. Eyton, R. Regev, and Y.G. Assaraf Functional reconstitution of p-glycoprotein reveals an apparent near stoichiometric drug transport to ATP hydrolysis J Biol Chem 271 1996 3172 3178
69. R.E. Daoud, and R.L. Juliano Modulation of doxorubicin resistance by valinomycin (NSC 122023) and liposomal valinomycin in Chinese hamster ovary cells Cancer Res 49 1989 2661 2667
70. R. Xu, H. Pelicano, and Y. Zhou Inhibition of glycolysis in cancer cells: A novel strategy to overcome drug resistance associated with mitochondrial respiratory defect and hypoxia Cancer Res 65 2005 613 621
71. X.L. Zu, and M. Guppy Cancer metabolism: facts, fantasy and fiction Biochem Biophys Res Commun 313 2004 459 465
72. J.S. Carew, and P. Huang Mitochondrial defects in cancer Mol Cancer 9 2002 1 12
73. A. Unruh, A. Ressel, and E. Mohamed The hypoxia-inducible factor-1 alpha is a negative factor for tumor therapy Oncogene 22 2003 3213 3220
74. G. Maschek, N. Savaraj, and W. Priebe 2-deoxy-d-glucose increases the efficacy of adriamycin and paclitaxel in human osteosarcoma and non-small cell lung cancers in vivo Cancer Res 64 2004 31 34
75. I.F. Rabey, A.D. Lien, and S.J. Welsh Hypoxia-inducible factor-1 alpha and the glycolytic phenotype in tumors Neoplasia 7 2005 324 330
76. L. Hlavata, H. Aguilaniu, A. Pichova, and T. Nystrom The oncogenic RAS2 (val19) mutation locks respiration, independently of PKA, in a mode prone to generate ROS EMBO J 22 2003 3337 3345
77. M. Board, S. Humm, and E.A. Newsholme Maximum activities of key enzymes of glycolysis, glutaminolysis, pentose phosphate pathway and tricarboxylic acid cycle in normal, neoplastic and suppressed cells Biochem J 265 1990 503 509
78. P. Newsholme, S. Gordon, and E.A. Newsholme Rates of utilization and fates of glucose, glutamine, pyruvate, fatty acids and ketone bodies by mouse macrophages Biochem J 242 1987 631 636
79. Isidoro A, Casado E, Redondo A, et al. Breast carcinomas ful fill the Warburg hypothesis and provide metabolic markers of cancer prognosis. Carcinogenesis, 2005 July 20 [Epub ahead of print].
80. H. Pelicano, D. Carney, and P. Huang ROS stress in cancer cells and therapeutic implications Drug Res Updates 7 2004 97 110
81. J.S. Modica-Napolitano, and K.K. Singh Mitochondrial dysfunction in cancer Mitochondrion 4 2004 755 762 Epub 2004, Oct 1
82. Y. Shidara, K. Yamagata, and T. Kanamori Positive contribution of pathogenic mutations in the mitochondrial genome to the promotion of cancer by prevention from apoptosis Cancer Res 65 2005 1655 1663
83. E. McClay, K. Albright, J. Jones, R. Christen, and S. Howell N,N-diethyl-2-[4-phenylmethyl)-phenoxyl]-ethanaminHCL (DPPE) is synergistic with cisplatin (DDP) in human melanoma cell lines Proc Am Assoc Cancer Res 34 1993 402 (abstr)
84. H. Hiramatsu, Y. Kikuchi, and K. Kudoh Growth-inhibitory effects of N,N-diethyl-2-[4-(phenylmethyl)phenoxy]-ethanamine-HCl combined with cisplatin on human ovarian cancer cells innoculated into nude mice Jpn J Cancer Res 88 1997 1003 1008
85. Y. Huang, P. Anderle, and K.J. Bussey Membrane transporters and channels: role of the transportome in cancer chemosensitivity and chemoresistance Cancer Res 64 2004 4230 4294
86. B. van Triest, H.M. Pinedo, and F. Telleman Cross-resistance to antifolates in multidrug resistant cell lines with P-glycoprotein or multidrug resistance protein expression Biochem Pharmacol 53 1997 1855 1866
87. Q. Mao, and J.D. Unadket Role of the breast cancer resistance protein (ABCG2) in drug transport AAPS J 7 2005 E118 E133
88. K. Yasui, S. Mihara, and C. Zhao Alteration in copy numbers of genes as a mechanism for acquired drug resistance Cancer Res 64 2004 1403 1410
89. M. Nomura, R. Matsunami, and K. Kobayashi Involvement of ABC transporters in chemosensitivity of human renal cell carcinoma, and regulation of MRP2 expression by conjugated bilirubin Anticancer Res 4 2005 2729 2735
90. K. Nakayama, A. Kanzaki, and K. Terada Prognostic value of the Cu-transporting ATPase in ovarian carcinoma patients receiving cisplatin-based chemotherapy Clin Cancer Res 10 8 2004 2804 2811
91. T. Suzuki, K. Nishio, and S. Tanabe The MRP family and anticancer drug metabolism Curr Drug Metab 2 4 2001 367 377
92. B. Savas, G. Arslan, T. Karpuzoglu, and C. Ozkaynak Multidrug resistant malignant melanoma with intracranial metastasis responding to immunotherapy Anticancer Res 19 5 1999 3313 3320
93. Ravi D, Muniyappa H, Das KC. Endogenous thioredoxin is required for redox-cycling of anthracyclines and p53+ dependent apoptosis in cancer cells. J Biol Chem, 2005 Sept 13: [Epub ahead of print].
94. S. Raguz, M.T. De Bella, and G. Tripuraneni Activation of the MDR1 upstream promoter in breast carcinoma as a surrogate for metastatic invasion Clin Cancer Res 10 2004 2776 2783
95. H. Burger, J.A. Foekens, and M.P. Look RNA expression of breast cancer resistance protein, lung resistance-related protein, multidrug resistance-associated proteins 1 and 2, and multidrug resistance gene 1 in breast cancer: Correlation with chemotherapeutic response Clin Cancer Res 9 2003 827 836
96. Keane P. Personal communication, 2004.