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A phase I study of vinblastine tryptophan ester


Vinblastine tryptophan ester (VTrpE) is a new vinca alkaloid derivative that achieves antitumor activity in a large variety of animal models. In this phase I study the drug was given as an i. v. injection over 5 min, once a week or once every 2 weeks. Twenty patients with advanced cancer were entered in this trial. The doses ranged from 2.5 mg/m2 to 35 mg/m2. Myelosuppression is the dose-limiting toxicity, with the risk of leukopenia being more serious than that of thrombocytopenia, but the myelosuppression is always reversible. Neurotoxicity, well documented when other vinca alkaloid derivatives are used, is insignificant. Two cases of disease stabilization have been observed in patients with non-small cell lung cancer. For VTrpE, a dose schedule of 30 mg/m2 per week may be recommended for phase II studies in non-small cell lung cancer.

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  1. 1.

    Barnett CJ, Culligan GJ, Gerzonk K, Hoying RC, Jones WE, Newlon WM, Poore GA, Robison RL, Sweeney MJ, Todd GC (1978) Structure activity relationships of dimeric catharanthus alkaloids: I. Deacetyl vinblastine amide (vindesine) sulfate. J Med Chem 21: 88

  2. 2.

    Bhushana Rao KSP, Collard MP, Trouet A (1983) Vinblastine-23-oyl amino acid derivatives, chemistry and antitumor activities. 13th International Congress of Chemotherapy, Vienna, August 28 to Sept. 2, SE 12 4 11/A

  3. 3.

    Bhushana Rao KSP, Collard MP, Trouet A, De Bruyn A, Verzele M, Noiret A, De Jonghe JP, Hannart J (1985) On the amidation of 17-deacetyl vinblastine with the ethyl esters of some amino acids. Bull Soc Chim Belg 94: 133

  4. 4.

    Bhushana Rao KSP, Collard MP, Atassi G, De Jonghe JP, Hannart J, Trouet A (1985) Vinblastine 23-oyl-amino acid derivatives: chemistry, physicochemical data, toxicity and antitumor activities against P388 and L1210 leukemias. J Med Chem 28: 1079

  5. 5.

    Bhushana Rao KSP, Collard MP, Trouet A (1985) Vinca 23-oyl amino acid derivatives as new anticancer agents. (Review). Anticancer Res 5: 374

  6. 6.

    Cooperative Study (1965) Neoplastic disease: Treatment with vinblastine. Arch Intern Med 116: 846

  7. 7.

    Gralla R, Raphael B, Golbey R, Young CW (1979) Phase II evaluation of vindesine in patients with non-small cell carcinoma of the lung. Cancer Treat Rep 63: 1343

  8. 8.

    Holland JF, Scharlan C, Gailani S, Krant MJ, Olson KB, Horton J, Shnider BI, Lynch JJ, Owers A, Carbone PP, Colsky J, Grob D, Miller SP, Hall TC (1973) Vincristine treatment of advanced cancer; a cooperative study of 393 cases. Cancer Res 33: 1258

  9. 9.

    Johnson IS, Armstrong JG, Gorman M, Burnett JP Jr (1963) The vinca alkaloids: a new class of oncolytic agents. Cancer Res 23: 1390

  10. 10.

    Kaplan RS, Wiernik PH (1979) Neurotoxicity of antineoplastic drugs. Semin Oncol 9: 103

  11. 11.

    Neus N, Gorman M, Hargrove W, Cone NJ, Biemann K, Buchi G, Manning RE (1964) Vinca alkaloids: XXI. The structures of the oncolytic alkaloids vinblastine (VBL) and vincristine (VCR). J Am Chem Soc 86: 1140

  12. 12.

    Noble RL (1964) Catharanthus roseus (vinca rosea). The importance and value of chance observation. Lloydia 2: 280

  13. 13.

    Sandler SG, Tobin W, Henderson ES (1969) Vincristine induced neuropathy. A clinical study of 50 leukemic patients. Neurology 19: 367

  14. 14.

    Sohier WD, Wong RK, Aisenberg AC (1968) Vinblastine in the treatment of advanced Hodgkin's diseases Cancer 22: 467

  15. 15.

    Weiss HD, Walker MD, WiernikPH (1974) Neurotoxicity of commonly used antineoplastic agents. N Engl J Med 291: 75 and 127

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Correspondence to F. Ceulemans.

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Ceulemans, F., Humblet, Y., Bosly, A. et al. A phase I study of vinblastine tryptophan ester. Cancer Chemother. Pharmacol. 18, 44–46 (1986).

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  • Ester
  • Lung Cancer
  • Animal Model
  • Cancer Research
  • Tryptophan