The anti-tumour effects of the prodrugs N-1-leucyl-doxorubicin and vinblastine-isoleucinate in human ovarian cancer xenografts

E. Boven, H. R. Hendriks, C. A M Erkelens, H. M. Pinedo

Research output: Contribution to journalArticle

Abstract

N-1-leucyl-doxorubicin and vinblastine-isoleucinate can be considered as relatively non-toxic prodrugs from doxorubicin and vinblastine, respectively. A comparative analysis was carried out of the anti-tumour activity of the four compounds as well as vintriptol in four human ovarian cancer xenografts different in histology, growth rate and chemosensitivity. Injections were given i.v. weekly twice into mice bearing well-established s.c. tumours. At equitoxic doses, the amount of drug administered for N-1-leucyldoxorubicin and vinblastine-isoleucinate was respectively 3-fold and 2-fold higher than the doses of the parent compound. N-1-leucyl-doxorubicin induced a growth inhibition > 50% in three out of four human ovarian cancer lines. The anti-tumour effects obtained were significantly better (P <0.01) than in the case of doxorubicin. Vinblastine-isoleucinate studied in two of these lines could induce a growth inhibition of > 50%. This prodrug appeared slightly less effective than vinblastine. Insignificant growth inhibition (<50%) was obtained by vintriptol.

Original languageEnglish (US)
Pages (from-to)1044-1047
Number of pages4
JournalBritish Journal of Cancer
Volume66
Issue number6
StatePublished - 1992
Externally publishedYes

ASJC Scopus subject areas

  • Cancer Research
  • Oncology

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