Vai ai contenuti. | Spostati sulla navigazione | Spostati sulla ricerca | Vai al menu | Contatti | Accessibilità

| Crea un account

Canal, Fabiana (2008) Profarmaci polimerici di farmaci antitumorali. [Tesi di dottorato]

Full text disponibile come:

[img]
Anteprima
Documento PDF
3996Kb

Abstract (inglese)

Anticancer drugs are very active molecules but they present limits that often prevent their success in chemotherapy. Most common problems are low half-life, due to rapid kidney clearance and to rapid inactivation by metabolic enzymes, and low selectivity towards cancer cells that causes severe side effects. The aim of this PhD thesis is to overcome some of the limits of anticancer drugs, especially the low molecular weight ones. In particular, some polymeric conjugates were prepared by linking an anticancer drug to a polymer that acts like a carrier. Poly-(ethylene glycol) was chosen as a carrier and it was linked to two anticancer drugs: gemcitabine, an antimetabolite drug, and epirubicin, an anthracycline. The following conjugates were prepared: mPEG-gemcitabine conjugates, with different molecular weights and shapes, folate-PEG-gemcitabine conjugates, by linking the drug at one side of polymer chain and a targeting moiety at the other side. The stability at different pH values, in plasma and towards the metabolic enzyme, pharmacokinetc behaviour and cytotoxicity were studied. Some epirubicin-PEG-folate conjugates were also prepared, with different number of molecules of folic acid per polymer chain, and were compared to similar ones without folic acid. In this case the cytotoxic activity, the cellular uptake and localization were studied.


Statistiche Download - Aggiungi a RefWorks
Tipo di EPrint:Tesi di dottorato
Relatore:Schiavon, Oddone
Dottorato (corsi e scuole):Ciclo 20 > Scuole per il 20simo ciclo > SCIENZE MOLECOLARI > SCIENZE FARMACEUTICHE
Data di deposito della tesi:31 Gennaio 2008
Anno di Pubblicazione:31 Gennaio 2008
Parole chiave (italiano / inglese):Gemcitabina, epirubicina, PEG, bioconiugazione
Settori scientifico-disciplinari MIUR:Area 03 - Scienze chimiche > CHIM/09 Farmaceutico tecnologico applicativo
Struttura di riferimento:Dipartimenti > Dipartimento di Scienze Farmaceutiche
Codice ID:215
Depositato il:10 Ott 2008
Simple Metadata
Full Metadata
EndNote Format

Bibliografia

I riferimenti della bibliografia possono essere cercati con Cerca la citazione di AIRE, copiando il titolo dell'articolo (o del libro) e la rivista (se presente) nei campi appositi di "Cerca la Citazione di AIRE".
Le url contenute in alcuni riferimenti sono raggiungibili cliccando sul link alla fine della citazione (Vai!) e tramite Google (Ricerca con Google). Il risultato dipende dalla formattazione della citazione.

1. Mason, P., Pharm. J. 260 (1998) 382-385 Cerca con Google

2. Duncan, R., Polymer conjugates for tumor targeting and intracytoplasmatic delivery. The EPR effect as a common gateway? Research focus / Reviews 2 (1999) 441-449 Cerca con Google

3. Thomas, F., Scrip. Magazine May (1998) 42-43 Cerca con Google

4. Folkman, J., Tumour angiogenesis, Adv. Cancer Res. 43 (1985) 175-203 Cerca con Google

5. Lundberg, A.S., Weinberg, R.A., Control of the cell cycle and apoptosis, Eur. J. Cancer 35(4) (1999) 531-539 Cerca con Google

6. Sandhu, J.S., Keating, A., Hozumi, N., Human gene therapy, Crit. Rev. Biotechnol. 17(4) (1997) 307-326 Cerca con Google

7. Robert, K.J., Cheng, Z., Cheng, C.C., Meth. and Find Exp. Clin. Pharmacol. 11 (1989) 439-529 Cerca con Google

8. Allen, T.M., Ligand-targeted therapeutics in anticancer therapy, Nat. Rev. Cancer 2 (2002) 750–763 Cerca con Google

9. Torchilin, V.P., Recent advances with liposomes as pharmaceutical carriers, Nat. Rev. Drug Discov. 4 (2005)145–160 Cerca con Google

10. Damle, N.K., Frost, P., Antibody-targeted chemotherapy with immunoconjugates of calicheamicin, Curr. Opin. Pharmacol. 3 (2003) 386–390 Cerca con Google

11. Harris, J.M, Chess, R.B., Effect of PEGylation on pharmaceuticals, Nat. Rev. Drug Discov. 2 (2003) 214–221 Cerca con Google

12. Veronese, F.M., Pasut, G., Guiotto, A., Protein, peptide and non-peptide drug PEGylation for therapeutic application, Expert Opin. Therap. Patents 14 (2004) 859–894 Cerca con Google

13. Duncan, R., The dawning era of polymer therapeutics, Nat. Rev. Drug Discov. 2 (2003) 347–360 Cerca con Google

14. Duncan, R., Polymer–Drug Conjugates, In: D. Budman et al., Editors, Handbook of Anticancer Drug Development, Lippincott Williams & Wilkins (2003) 239–260 Cerca con Google

15. Duncan, R., N-(2-hydroxypropyl)methacrylamide copolymer conjugates, In: G.S. Kwon, Editor, Polymeric Drug Delivery Systems, Marcel Dekker (2005) 1–92 Cerca con Google

16. Willis, R.C., Good things in small packages. Nanotech advances are producing megaresults in drug delivery, Modern Drug Discov 7 (2004) 30–36 Cerca con Google

17. Vincent, M.J., Duncan, R., Polymer conjugates: nanosized medicines for treating cancer, Trends Biotechnol. 24(1) (2006) 39-47 Cerca con Google

18. Anderson, J.M., Biological responses to materials, Annual Rev. Mat. Res. 31 (2001) 81– 110 Cerca con Google

19. Baldrick, P., Pharmaceutical excipient development: The need for preclinical guidance, Regul. Toxicol. Pharmacol. 32 (2000) 210–218 Cerca con Google

20. Luo, Y., Prestwich, G.D., Cancer-targeted polymeric drugs, Curr. Cancer Drug Targets 2(3) (2002) 209-26 Cerca con Google

21. Arnold, I., Freeman, M.D., Mayhew, E., Targeted drug delivery. Cancer 58 (1986) 573- 583 Cerca con Google

22. Ranade, V.V., Drug delivery systems:3A. Role of polymers in drug delivery. J. Clin. Pharmacol. 30 (1) (1990) 10-23 Cerca con Google

23. Bolla, M., Collette, L., Blank, L., Warde, P., Dubois, J.B., Mirimanoff, R.O., Storme, G., Bernier, J., Kuten, A., Sternberg, C., Mattelaer, J., Lopez Torecilla, J., Pfeffer, J.R., Lino Cutajar, C., Zurlo, A., Pierart, M., Long-term results with immediate androgen suppression and external irradiation in patients with locally advanced prostate cancer (an EORTC study): a phase III randomized trial, Lancet 360 (2002) 103–108 Cerca con Google

24. Guerin, C., Olivi, A., Weingart, J.D., Lawson, H.C., Brem, H., Recent advances in brain tumor therapy: local intracerebral drug delivery by polymers, Invest. New Drugs 22(1) (2004) 27–37 Cerca con Google

25. Hoes, C.J.T., Feijen, J., The application of drug-polymer conjugates in chemotherapy, Drug Carrier Systems (1989) 57-109 Cerca con Google

26. Cavallaro, G., Pitarresi, G., Licciardi, M., Giammona, G., Polymeric prodrug for release of an antitumoral agent by specific enzymes, Bioconjugate Chem. 12(2) (2001) 143-151 Cerca con Google

27. Ringsdorf, H., Structure and properties of pharmacologically active polymers, J. Polym. Sci. Polym. Symp. 51 (1975) 135-153 Cerca con Google

28. Puttnam, D., Kope?ek, J., Polymer conjugates with anticancer activity, Adv. Polym. Sci. 122 (1995) 55-123 Cerca con Google

29. Veronese, F.M., Morpurgo, M., Bioconjugation in pharmaceutical chemistry, Il farmaco 54 (1999) 497-516 Cerca con Google

30. Iver, L., Ratain, M.J., Pharmacogenetics and cancer chemotherapy, Eur. J. Cancer 34(10) (1998) 1493-1499 Cerca con Google

31. Maeda, H., Matsumura, Y., Tumoritropic and lymphotropic principles of macromolecular drugs, CRC Crit. Rev. Ther. Drug Carrier Sys. 6(3) (1989) 193-210 Cerca con Google

32. Maeda, H., Sawa, T., Konno, T., Mechanism of tumor-targeted delivery of macromolecular drugs, including the EPR effect in solid tumor and clinical overview of the prototype polymer drug SMANCS, J. Controlleed Release 74 (2001) 47-61 Cerca con Google

33. Maeda, H., Fang, J., Inutsuka, T., Kitamoto, Y., Vascular permeability enhancement in solid tumor: various factors, mechanisms involved and its implications, International Immunopharmacology 3 (2003) 319-328 Cerca con Google

34. Kope?ek, J., Kope?ková, P., Minko, T., Lu, Z.-R., Peterson, C.M., Water soluble polymers in tumor targeted delivery, J. Controlled Release 74 (2001) 147-158 Cerca con Google

35. Garanger, E., Boturyn, D., Dumy, P., Tumor targeting with RGD peptide ligands-design of new molecular conjugates for imaging and therapy of cancers, Anticancer Agents Med. Chem. 7(5) (2007) 552-558 Cerca con Google

36. Shen, W.C., Ryser, H.J.P., Cys-aconityl spacer between daunomycin and macromolecular carriers: a model of pH-sensitive linkage releasing drug from a lysosomotropic conjugate, Biochem. Biophys. Res. Commun. 102 (1981) 1048-1054 Cerca con Google

37. Soyez, H., Schacht, E., Vanderkerken, S., The crucial role of spacer groups in macromolecular prodrug design, Adv. Drug Del. Rev. 21 (1996) 81-106 Cerca con Google

38. Duncan, R., Hume, I.C., Yardley, H.J., Flanagan, A., Ulbrich, K., Subr, U., Strohalm, J., Macromolecular prodrugs for use in target cancer chemotherapy: melphalan covalently coupled to N-(2-Hydroxypropyl)methacrylamide copolymers, J. Controlled Release 16 (1991) 121-136 Cerca con Google

39. Vercauren, R., Bruneeld, D., Schacht, E., Effect of the medical modification of dextran on the degradation by dextranases. J. Bioactive Comp. Polym. 5 (1990) 4-15 Cerca con Google

40. Rihova, B., Riha, I., Immunological problems of polymer bound drugs, CRC Crit. Rev. Therap. Drug Carrier Sys. 1 (1985) 311-374 Cerca con Google

41. Renglesen, W., Anionic dyes, heparin and heparinoids-the rediscovery of polyanionic antitumor agents, J. Natl. Cancer Inst. 81 (1989) 1920-1930 Cerca con Google

42. Trouet, A., Deprez-Decampeneere, D., De Duve, C., Chemotherapy trough lysosomes with a DNA-daunorubicin complex, Nature New Biology 239 (1972) 110-112 Cerca con Google

43. Trouet, A., Jollés, A., Targeting of daunorubicin by association with DNA or proteins: a review, Seminars in Oncology 11 (1984) 64-72 Cerca con Google

44. De Duve, C., De Barsy, T., Poole, B., Trouet, A., Tulkens, P., Van Hoof, Lysosomotropic agents, Biochem. Pharmacol. 23 (1974) 2495-2531 Cerca con Google

45. Larsen, C., Dextran prodrugs-structure and stability in relation to therapeutic activity, Adv. Drug Deliv. Rev. 3 (1989) 103-154 Cerca con Google

46. Sezaky, H., Hashida, M., Macromolecular-drug conjugates in targeted cancer chemotherapy, CRC Crit. Rev. Ther. Drug Carrier Syst. 1 (1983) 1-38 Cerca con Google

47. Maeda, H., SMANCS and polymer conjugated macromolecular drugs: advantages in cancer chemotherapy, Adv. Drug Delivery Rev. 6 (1991) 181-202 Cerca con Google

48. Duncan, R., Spreafico, F., Polymer conjugates: pharmacokinetic considerations for design and development, Clin. Pharmacokinet. 27(4) (1994) 290-306 Cerca con Google

49. Seymour, L.W., Duncan, R., Strohalm, J., Kopecek, J., Effect of molecular weight of N- (2-hydroxypropyl)methacrylamide copolymers on body distributions and rate of excretion after subcutaneous intraperitoneal and intravenous administration to rats, J. Biomed. Mater. Res. 21(11) (1987) 1341-1358 Cerca con Google

50. Vasey, P.A., Duncan, R., Kaye, S.B., Cassidy, J., Clinical Phase I trial (HPMA copolymer doxorubicin), Eur. J. Cancer 31A (1995) S193 Cerca con Google

51. Bailey, J.F.E., Koleske, J.V., Poly(etylene-oxide), Academic Press New York, (1976) 52. Dreborg, S., Akerblom, E.B., Immunotherapy with monomethoxypolyethylene glycol modified allergens, Crit. Rev. Ther. Drug Carrier Syst. 6(4) (1990) 315-365 Cerca con Google

52. Dreborg, S., Akerblom, E.B., Immunotherapy with monomethoxypolyethylene glycol modified allergens, Crit. Rev. Ther. Drug Carrier Syst. 6(4) (1990) 315-365 Cerca con Google

53. Powell, G.M., Polyethylene glycol, Handbook of water soluble gums and resins (R.L. Davidson, Ed.), pp 18-1-18-31, McGraw-Hill, New York, 1980. Cerca con Google

54. Mutter, M., Bayer, E., The peptides Academic Press, New York (1979) 285-332 Cerca con Google

55. Yamaoka,T., Tabata, Y., Ikada, Y., Distribution and tissue uptake of poly(ethylene glycol) with different molecular weights after intravenous administration to mice, J. Pharm. Sci. 83(4) (1994) 601-606 Cerca con Google

56. Delgado, C., Francis, G.E., Fisher, D., The uses and properties of PEG-linked proteins, Crit. Rev. Ther. Drug Carrier Syst. 9 (1992) 249-304 Cerca con Google

57. Roberts, M.J., Bentley, M.D., Harris, J.M., Chemistry for peptide and protein PEGylation, Adv. Drug Deliv. Rev. 54 (2002) 459-476 Cerca con Google

58. Bhadra, D., Bhadra, S., Jain, P., Jain, N.K., Pegnology: a review of PEG-ylated systems, Pharmazie 57 (2002) 5-29 Cerca con Google

59. Davis, F.F., The origin of PEGnology, Adv. Drug Deliv. Rev. 54 (1992), 457-458 Cerca con Google

60. Veronese, F.M., Peptide and protein PEGylation: a review of problems and solutions, Biomaterials 22 (2001) 405-417 Cerca con Google

61. Greewald, R.B., PEG drugs: an overview, J. Controlled Release 74 (2001) 159-171 Cerca con Google

62. Greewald, R.B., Choe, Y.H., McGuire, J., Conover, C.D., Effective drug delivery by PEGylated drug conjugates, Adv. Drug Deliv. Rev. 55 (2003) 217-250 Cerca con Google

63. Herman, S., Hooftman, G., Schacht, E., Poly(ethylene glycol) with reactive endgroups: I. Modification of proteins, Journal of bioactive and biocompatible polymers 10 (1995)145- 187 Cerca con Google

64. Woghiren, C., Sharma, B., Stein, S. Protected thiol-polyethylene glycol: a new activated polymer for reversible protein modification, Bioconjug. Chem. 4 (1993) 314-318 Cerca con Google

65. Morpurgo, M., Veronese F.M., Kanchesky, D., Harris, J.M., Preparation and characterization of poly(ethylene glycol) vinyl sulfone, Bioconjug. Chem. 7 (1996) 363- 368 Cerca con Google

66. Catalogo Shearwater Polymers, Inc. 2005 Cerca con Google

67. Molineux, G., Pegylation: engineering improved pharmaceuticals for enhanced therapy, Cancer Treat. Rev. 28 (Suppl.A) (2002) 13-16 Cerca con Google

68. Caliceti, P., Veronese, F.M., Pharmacokinetic and biodistribution properties of poly(ethylene glycol)-protein conjugates, Adv. Drug Deliv. Rev. 55 (2003) 1261-1277 Cerca con Google

69. Zalipsky, S., Functionalized poly(ethylene glycol) for preparation of biologically relevant conjugates, Bioconjugate Chem. 6 (1995) 150-165 Cerca con Google

70. Gotesman, M.M., The role of proteases in cancer, Semin. Cancer Biol. 1 (1990) 97-160 Cerca con Google

71. Abuchowski, A., Devis, F.F., Devis, F., Immunosuppressive properties and circulatory life of acromobacter glutaminase-asparaginase covalently attached to poly(ethylene glycol) in man, Cancer Treat. Rep. 65 (1981) 1077-1081 Cerca con Google

72. Abuchowski, A., Kazo, G.M., Verhoest, C.R., Van Es, T., Kafkewitz, D., Nucci, M.L., Viau, A.T., Davis, F.F., Cancer therapy with chemically modified enzymes. I. Antitumor properties of polyethylene glycol-asparaginase conjugates, Cancer Biochem. Biopys. 7 (1984) 175–186 Cerca con Google

73. Carl, P.L., Chakravarty, P.K., Katzenellenbogen, J.A. A novel connector linkage applicable in prodrug design, J. Med. Chem. 24 (1981) 479–480 Cerca con Google

74. Zalipsky S., Chemistry of polyethylene glycol conjugates with biologically active molecules, Adv. Drug Del. Rev. 16 (1995) 157-182 Cerca con Google

75. Poiani, G.J., Riley, D.J., Fox, J.D., Kemnizer, J.E., Gean, K.F., Kohn, J., Conjugates of cis-4-hydroxy- -proline and poly(PEG-Lys), a water soluble poly(ether urethane): Synthesis and evaluation of antifibrotic effects in vitro and in vivo, Bioconj. Chem. 5 (1994) 621–630 Cerca con Google

76. Tomlinson R., et al. Pendent chain functionalized polyacetals that display pH-dependent degradation: a platform for the development of novel polymer therapeutics, Macromolecules 35 (2002) 473–480 Cerca con Google

77. Hreczuk-Hirst D., Chicco, D., German, L., Duncan, R., Dextrins as potential carriers for drug targeting: tailored rates of dextrin degradation by introduction of pendant groups, Int. J. Pharm. 230 (2001) 57–66 Cerca con Google

78. Mero, A., Coniugati polimerici di interesse farmaceutico, Tesi di dottorato di ricerca (2006) Cerca con Google

79. Malik N., Evangorou, E.G., Duncan, R., Dendrimer–platinate: a novel approach to cancer chemotherapy, Anticancer Drugs 10 (1999) 767–776 Cerca con Google

80. Kobayashi, H., Kawamoto, S., Sakai, Y., Choyke, P.L., Star, R.A., Brechbiel, M.W., Sato, N., Tagaya, Y., Morris, J.C., Waldmann, T.A., Lymphatic drainage imaging of breast cancer in mice by micro-magnetic resonance lymphangiography using a nano-size paramagnetic contrast agent, J. Natl. Cancer Inst. 96 (2004) 703–708 Cerca con Google

81. Baker J.R., et al. The synthesis and testing of anticancer therapeutic nanodevices, Biomedical Microdevices 3 (2001) 61–69 Cerca con Google

82. Shukla, S., Wu, G., Chatterjee, M., Yang, W., Sekido, M., Diop, L.A., Müller, R., Sudimack, J.J., Lee, R.J., Barth, R.F., Tjarks, W., Synthesis and biological evaluation of folate receptor-targeted boronated PAMAM dendrimers as potential agents for neutron capture therapy, Bioconjug. Chem. 14 (2003) 158–167 Cerca con Google

83. Gao C., Xu, Y., Yan, D., Chen, W., Water-soluble degradable hyperbranched polyesters: novel candidates for drug delivery?, Biomacromolecules 4 (2003), pp. 704–712. Cerca con Google

84. Schlaad, H., Antonietti, M., Block copolymers with amino acid sequences: molecular chimeras of polypeptides and synthetic polymers, Eur. Phys. J. E 10 (2003) 17–23 Cerca con Google

85. Jelinkova, M., Strohalm, J., Etrych, T., Ulbrich, K., Rihova, B., Star-like vs. classic macromolecular prodrugs: two different antibody-targeted HPMA copolymers of doxorubicin studied in vitro and in vivo as potential anticancer drugs, Pharm. Res. 20 (2003) 1558–1564 Cerca con Google

86. Shaunak, S., Thomas, S., Gianasi, E., Godwin, A., Jones, E., Teo, I., Mireskandari, K., Luthert, P., Duncan, R., Patterson, S., Khaw, P., Brocchini, S., Polyvalent dendrimer glucosamine conjugates prevent scar tissue formation, Nat. Biotechnol. 22 (2004) 977– 984 Cerca con Google

87. Kwon, G., Suwa, S., Yokoyama, M., Okano, T., Sakurai Y., Kataoka, K., Enhanced tumor accumulation and prolonged circulation times of micelle-forming poly(ethylene oxide-aspartate) block copolymer-adriamycin conjugates, J. Controlled Rel. 29 (1994) 17–23 Cerca con Google

88. Noble, S., Goa, K.L., Gemcitabine. A review of its pharmacology and clinical potential in N-small cell lung cancer and pancreatic cancer, Drugs 54(3) (1997) 447-472 Cerca con Google

89. Hertel, L.W., Kroin, J.S., Misner, J.W., Tustin, J.M., Synthesis of 2-deoxy-2,2-difluoro- D-ribose and 2-Deoxy-2,2-difluoro-D-ribofuranosyl nucleosides, J. Org. Chem. 53 (1988) 2406-2409 Cerca con Google

90. Storniolo, A.M., Allerheiligen, S.R.B., Pearce, H.L., Preclinical, pharmacologic and phase I studies of gemcitabine, Seminars in Oncology 24 (2, Suppl.7) (1997) S7-2-S7-7 Cerca con Google

91. Abbruzzese, J.L., Grunewald, R., Weeks, E.A., Gravel, D., Adams, T., Nowak, B., Mineishi, S., Tarassoff, P., Satterlee, W., Raber, M.N., Plunkett, W., A phase I clinical, plasma, and cellular pharmacology study of gemcitabine, J. Clin. Oncol. 9(3) (1991) 491- 498 Cerca con Google

92. Hertel, L.W., Boder, G.B., Kroin, J.S., Rinzel, S.M., Poore, G.A.,Todd, G.C., Grindey, G.B., Evaluation of the antitumor activity of gemcitabine (2’,2’-difluoro-2’- deoxycytidine), Cancer Research 50 (1990) 417-4422 Cerca con Google

93. Heinemann, V., Hertel, L.W., Grindey, G.B., Plunkett, W., Comparison of the cellular pharmacokinetics and toxicity of 2’,2’-difluodeoxycytidine and 1- ß-Darabinofuranosylcytosine, Cancer Research 48 (1988) 4024-4031 Cerca con Google

94. Plunkett, W., Huang, P., Xu, Y.-Z., Heinemann, V., Grunewald, R., Gandhi, V., Gemcitabine: metabolism, mechanisms of action, and self-potentiation, Seminars in Oncology 22(4 Suppl.11) (1995) 3-10 Cerca con Google

95. Kedzierski, P., Solaski, W.A., Cheng, H., Mitchell, J., Leszczynski, J., DFT study of the reaction proceeding in the cytidine deaminase, Chemical Physics Letter 381 (2003) 660- 665 Cerca con Google

96. Heinemann, V., Xu, Y.-Z., Chubb, S., Sen, A., Hertel, L.W., Grindey, G.B., Cellular elimination of 2’,2’-difluorodeoxycytidine 5’-triphosphate: a mechanism of selfpotentiation, Cancer Research 52 (1992) 533-539 Cerca con Google

97. FDA Revised Label-Version 082598, Gemzar® for injection. Cerca con Google

98. Huang, P., Chubb, S., Hertel, L.W., Grindey, G.B., Plunkett, W., Action of 2’,2’- difluorodeoxycytidine on DNA synthesis, Cancer Res. 51 (1991) 6110-6117 Cerca con Google

99. Heinemann, V., Xu, Y.-Z., Chubb, S., Sen, A., Hertel, L.W., Grindey, G.B., Plunkett, W., Inhibition of ribonucleotide reduction in CCRF-CEM cells by 2’,2’- dufluorodeoxycytidine, Molec. Pharmacol. 38(4) (1990) 567-572 Cerca con Google

100. Gandhi, V., Plunkett, W., Modulatory activity of 2’,2’-difluorodeoxycytidine on the phosphorylation and cytotoxicity of arabinosyl nucleosides, Cancer Res. 50(12) (1990) 3675-3680 Cerca con Google

101. Ruiz van Haperen V.M.T., Veerman, G., van Moorsel, C.T.A., Peters, G.J., Induction of in vivo resistance against gemcitabine, Adv. Exp. Med. Biol. 431 (1998) 637- 640 Cerca con Google

102. Goan, Y.-G., Zhou, B., Hu, E., Mi, S., Y, Y., Overexpression of ribonucleotide reductase as a mechanism of resistance to 2,2-difluorodeoxycytidine in the human KB cancer cell line, Cancer Research 59 (1999) 4204-4207 Cerca con Google

103. Hui, Y.F., Reitz, J., Gemcitabine. A cytydine analogue active against solid tumors, Am. J. Health-Syst. Pharm. 54 (1997) 162-170 Cerca con Google

104. Eli Lilly and Company, Summary of product characteristics: Gemcitabine. UK prescribing information. Eli Lilly (1997) Cerca con Google

105. Grunewald, R., Kantarjian, H., Du, M., Faucher, K., Tarassoff, P., Plunkett, W., Gemcitabine in leukemia: a phase I clinical, plasma, and cellular pharmacology study, J. Clin. Oncol. 10(3) (1992) 406-413 Cerca con Google

106. Barton-Burke, M., Gemcitabine: A pharmacologic and clinical overview, Cancer Nursing 22(2) (1999) 176-183 Cerca con Google

107. Guchelaar, H.-J., Richel, D.J., van Knapen, A., Clinical, toxicological and pharmacological aspects of gemcitabine, Cancer Treat. Rev. 22 (1996) 15-31 Cerca con Google

108. Levitt, M.L., Kassem, B., Gooding, W.E., Miketic, L.M., Landreneau, R.J., Ferson, P.F., Keenan, R., Yousem, S.A., Lindberg, C.A., Trenn, M.R., Ponas, R.S., Tarasoff, P., Sabatine, J.M., Friberg, D., Whiteside, T.L., Phase I study of gemcitabine given weekly as a short infusion for non-small cell lung cancer: results and possible immune system-related mechanisms, Lung Cancer (2003) 1-10 Cerca con Google

109. Abratt, R.P., Bezwoda, W.R., Falkson, G., Goedhals, L., Hacking, D., Rugg, T.A., Efficacy and safety profile of gemcitabine in non-small cell lung cancer: a phase II study, J. Clin. Oncol. 12(8) (1994) 1535-1540 Cerca con Google

110. Crinò, L., Calandri, C., Gemzar platinum combinations: phase III trials in nonsmall cell lung cancer, Lung Cancer 38 (2002) S9-S12 Cerca con Google

111. Hoang, T., Kim, K.M., Jalowski, A., Koch, P., Beatty, P., McGovern, J., Quisumbing, M., Shapiro, G., Witte, R., Schiller, J.H., Phase II study of second-line gemcitabine in sensitive or refractory small cell lung cancer, Lung Cancer 42 (2003) 97- 102 Cerca con Google

112. Cormier, Y., Eisenhauer, E., Muldal, A., Gregg, R., Ayoub, J., Goss, G., Stewart, D., Tarsoff, P., Wong, D., Gemcitabine is an active new agent in previously untreated extensive small cell lung cancer (SCLC), Annals of Oncology 5 (1994) 283-285 Cerca con Google

113. Heinemann, V., Gemcitabine-based combination treatment of pancreatic cancer, Seminars in Oncology 28(1 Suppl.3) (2002) 25-35 Cerca con Google

114. Rothenberg, M.L., Moore, M.J., Cripps, M.C., Andersen, J.S., Portenoy, R.K., Burris III, H.A., Green, M.R., Tarssoff, P.G., Brown, T.D., Casper, E.S., Storniolo, A.M., Von Hoff, D.D., A phase II trial of gemcitabine in patients with 5-FU-refractory pancreas cancer, Annals of Oncology 7 (1996) 347-353 Cerca con Google

115. Carmichael, J., Fink, U., Russell, R.C.G., Spittle, M.F., Harris, A.L., Spiessi, G., Blatter, J., Phase II study of gemcitabine in patients with advanced pancreatic cancer, Br. J. Cancer 73 (1996) 101-105 Cerca con Google

116. Fruscella, E., Gallo, D., Ferrandina, G., D’Agostino, G., Scambia, G., Gemcitabine: current role and future options in the treatment of ovarian cancer, Critical Reviews in Oncology/Hematology 48 (2003) 81-88 Cerca con Google

117. Fowler Jr., W.C., Van Le, L., Gemcitabine as a single-agent treatment for ovarian cancer, Gynecologic Oncology 90 (2003) S21-S23 Cerca con Google

118. Mutch, D.G., Gemcitabine combination chemotherapy of ovarian cancer, Gynecologic Oncology 90 (2003) S16-S20 Cerca con Google

119. Carmichael, J., Possinger, K., Phillip, P., Beykirch, M., Kerr, H., Walling, J., Harris, A.L., Advanced breast cancer: a phase II trial with gemcitabine, J. Clin. Oncol. 13(11) (1995) 2731-2736 Cerca con Google

120. Morabito, A., Filippelli, G., Palmeri, S., Cascinu, S., Ferraù, F., Zagonel, V., Gattuso, D., Catalano, V., Capaccetti, B., Franciosi, V., Accurso, V., Scinto, F., Gasparini, G., The combination of gemcitabine and vinorelbine is an active regimen as second-line therapy in patients with metastatic breast cancer pretreated with taxanes and/or anthracyclines: a phase I-II study, Breast cancer Research and Treatment, 78 (2003) 29-36 Cerca con Google

121. Smorenburg, C.H., Bontenbal, M., Seynaeve, C., van Zuylen, C., de Heus, G., Verweij, J., de Wit, R., Phase II study of weekly gemcitabine in patients with metastatic breast cancer relapsing or failing both an anthracycline and a taxane, Breast Cancer research and Treatment 66 (2001) 83-87 Cerca con Google

122. Sternberg, C.N., Gemcitabine in bladder cancer, Seminars in Oncology 27(1 Suppl. 2) (2000) 31-39 Cerca con Google

123. Laufer, M., Ramalingam, S., Schoenberg, M.P., Haisfield-Wolf, M.E., Zuhowski, E.G., Trueheart, I.N., Eisenberg, M.A., Nativ, O., Egorin, M.J., Intravesical gemcitabine therapy for superficial transitional cell carcinoma of the bladder: a phase I and pharmacokinetic study, J Clin. Oncol. 21(4) (2003) 697-703 Cerca con Google

124. Vogelzang, N.J., Future directions for gemcitabine in the treatment of genitourinary cancer, Semin. Oncol. 29(3) (2002) 40-45 Cerca con Google

125. Kindler, H.L., van Meerbeeck, J.P., The role of gemcitabine in the treatment of malignant mesothelioma, Semin. Oncol. 29 (2002) 70-76 Cerca con Google

126. Fung, M.C., Storniolo, A.M., Nguyen, B., Arning, M., Brookfield, W., Vigil, J., A review of Hemolytic Uremic Syndrome in patients treated with gemcitabine therapy, Cancer 85(9) (1999) 2023-2032 Cerca con Google

127. Epirubicin official FDA information, side effects and usesù Cerca con Google

128. Plosker, G.L., Faulds, D., Epirubicin. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic use in cancer chemotherapy, Drugs 45 (1993) 788-856 Cerca con Google

129. Robert, J., Clinical Pharmacokinetics of epirubicin, Clin. Phermacokinet. 26 (1994) 428-438 Cerca con Google

130. Zagotto, G., Gatto, B., Moro, S., Sissi, C., Palumbo, M., Anthracyclines: recent development in their separation and quantitation, J. Chromatogr. B 764 (2001) 161-171 Cerca con Google

131. Lopez, M., Anthracyclines in the adjuvant treatment of breast carcinoma: thirty years later, Clin. Ter. 157(2) (2006) 165-177 Cerca con Google

132. Glück, S., Adjuvant chemotherapy for early breast cancer: optimal use of epirubicin, Oncologist 10(10) (2005) 780-791 Cerca con Google

133. Pronzato, P., Vigani, A., Tognoni, A., Vaira, F., Canessa, P., Anthracyclines in non-small cell lung cancer, Lung Cancer 34 (2001) S57-59 Cerca con Google

134. Gabizon, A., Horowitz, A.T., Goren, D., Tzemach, D., Mandelbaum-Shavit, F., Qazen, M.M., Zalipsky, S., Targeting folate receptor with folate linked to extremities of poly(ethylene glycol)-grafted liposomes: in vitro studies, Bioconjug. Chem. 10(2) (1999) 289-298 Cerca con Google

135. Lu, Y., Low, P.S., Folate-mediated delivery of macromolecular anticancer therapeutic agents, Adv. Drug Del. Rev. 54 (2002) 675-693 Cerca con Google

136. Sudimack, J., Lee, R.J., Targeted drug delivery via the folate receptor, Advanced Drug Del. Rev. 41 (2) (2000) 147-162 Cerca con Google

137. Weitman, S.D., Lark, R.H., Coney, L.R., Fort, D.W., Frasca, V., Zurawski, V.R.Jr., Kamen, B.A., Distribution of the folate receptor GP38 in normal and malignant cell lines and tissues, Cancer Res. 52 (1992) 3396-3401 Cerca con Google

138. Campbell, I.G., Jones, T.A., Foulkes, W.D., Trowsdale, J., Folate-binding protein is a marker for ovarian cancer, Cancer Res. 51 (1991) 5329-5338 Cerca con Google

139. Garin-Chese, P., Campbell, I., Saigo, P.E., Lewis, J.L.Jr., Old, L.J., Retting, W.J., Trophoblast and ovarian cancer antigen LK26. Sensitivity and specificity in immunopathology and molecular identification as a folate-binding protein, Am. J. Pat. 142 (1993) 557-567 Cerca con Google

140. Jhaveri, M.S., Rait, A.S., Chung, K.N., Trepel, J.B., Chang, E.H., Antisense oligonucleotides targeted to the human folate receptor inhibit breast cancer growth and sensitize the cell to doxorubicin treatment, Mol. Cancer Ther. 3(12) (2004) 1505-12 Cerca con Google

141. Rijnboutt, S., Jansen, G., Postuma, G., Hynes, J.B., Schornagel, J.H., Strous, G.J., Endocytosis of GPI-linked membrane folate receptor-a, J. Cell Biol. 132 (1-2) (1999) 35- 47 Cerca con Google

142. Rothberg, B.A., Ying, Y., Kolhouse, J.F., Kamen, B.A., Anderson, R.G.W., The Glycophospholipid-linked folate receptor internalizes folate without entering the clatrincoated pit endocytic pathway, J. Cell Biol. 110 (1990) 637-649 Cerca con Google

143. Anderson, R.G.W., Kamen, B.A., Rothberg, K.G., Lacey, S.W., Potocytosis: sequestration and transport of small molecules by caveolae, Science 255 (1992) 410-411 Cerca con Google

144. Stella, B., Arpicco, S., Peracchia, M.T., Desmaele, D., Hoebeke, J., Renoir, M., D’Angelo, J., Cattel, L., Couvreur, P., Design of folic acid-conjugated nanoparticles for drug targeting, J. Pharm. Sciences 89 (2000) 1452-1464 Cerca con Google

145. Wang, S., Lee, J.R., Mathias, J.C., Green, A.M., Low, S.P., Synthesis, purification and tumor cell uptake of Ga-Deferoxamine-folate, a potential radiopharmaceutical for tumor imaging, Bioconj. Chem. 7 (1996) 56-62 Cerca con Google

146. Snyder, S.L., Sobocinski, P.Z., An improved 2,4,6-trinitrobenzenesulfonic acid method for the determination of amines, Anal. Biochem. 64(1) (1975) 284-288 Cerca con Google

147. Sims, G.E.C., Snape, T.J., A method for the estimation of polyethylene glycol in plasma protein fractions, Anal. Biochem. 107(1) (1980) 60-63 Cerca con Google

148. Lee, R.J., Low, P.S., Delivery of liposomes into cultured KB cells via folate receptor-mediated endocytosis, J. Biological Chem. 5(4) (1994) 3198-3204 Cerca con Google

149. Vicentini, M., Coniugati polimerici di gemcitabina: studi preliminari per un targeting antitumorale, Tesi di laurea (2005) Cerca con Google

150. Alexander, R.L., Morris-Natschke, S.L., Ishaq, K.S., Fleming, R.A., Kucera, G.L., Synthesis and cytotoxic activity of two novel 1-dodecylthio-2-decyloxypropyl-3- phosphatidic acid conjugates with gemcitabine and cytosine arabinoside, J. Med. Chem. 46 (2003) 4205-4208 Cerca con Google

151. Schneider, R., Schmitt, F., Frochot, C., Fort, Y., Lourette, N., Guillemin, F., Müller, J-F., Barberi-Heyob, M., Design, synthesis and biological evaluation of folic acid targeted tetraphenylporphyrin as novel photosensitizers for selective photodynamic therapy, Bioorg. Med. Chem. 13 (2005) 2799-2808 Cerca con Google

152. Zhang, Q., Xiang, G., Zhang, Y., Yang, K., Fan,W., Lin, J., Zeng, F., Wu, J., Increase of doxorubicin sensitività for folate receptor positive cells when given as the prodrug N-(phenylacetyl)doxorubicin in combination with folate-conjugated PGA, J. Pharm. Sci. 10 (2006) 2266-2075 Cerca con Google

153. Yoo, H.S., Park, T.G., Folate-receptor-targeted delivery of doxorubicin nanoaggregates stabilized by doxorubicin-PEG-folate conjugate, J. Controlled Rel. 100 (2004) 247-256 Cerca con Google

154. Chattopadhyay, S., Wang, Y., Zhao, R., Goldman, I.D., Lack of impact of the loss of constitutive folate receptor _ expression, achieved by RNA interference, on the activity of the new generation antifolate pemetrexed in HeLa cells, Clin. Cancer Res. 10 (2004) 7986-7993 Cerca con Google

155. Fang, J., Deng, D., Nakamura, H., Akuta, T., Qin, H., Iyer, A.K., Greish, K., Maeda, H., Oxystress inducing antitumor therapeutics via tumor-targeted delivery of PEG-conjugated D-amino acid oxidase, Int. J. Cancer 122(5) (2008) 1135-1144 Cerca con Google

156. Schiavon, O., Pasut, G., Moro, S., Orsolini, P., Guiotto, A., Veronese, F.M., PEGAra- C conjugates for controlled release, Eur. J. Med. Chem. 39(2) (2004) 123-133 Cerca con Google

Download statistics

Solo per lo Staff dell Archivio: Modifica questo record