Combination of the new minor groove alkylator tallimustine and melphalan

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Abstract

The benzoyl nitrogen mustard derivative of distamycin A, tallimustine, belongs to a new class of alkylating agents, known as DNA minor groove alkylating agents. It alkylates adenine N3 with high sequence specificity, causing no alkylation of guanine N7, the main site of alkylation of clinically used nitrogen mustards such as L-PAM. The present study investigated the in vivo antitumour activity of a combination of tallimustine and melphalan (L-PAM). Two murine tumours were used: i.p. (intraperitoneally) transplanted L1210 leukaemia and i.m. (intramuscularly) transplanted M5076 ovarian reticulum cell sarcoma (M5). In L1210, which is only marginally sensitive to tallimustine, the combination of tallimustine 3 mg/kg i.p. with L-PAM 10 mg/kg i.p. was as effective as 20 mg/kg L-PAM, which is the maximum tolerated dose. In M5, which is sensitive to both drugs, the combination Was superior to either drug alone. The results suggest that the combination of tallimustine and L-PAM - or possibly in general, minor groove alkylators and major groove alkylators - may be therapeutically advantageous and therefore should be investigated clinically.

Original languageEnglish
Pages (from-to)284-287
Number of pages4
JournalEuropean Journal of Cancer
Volume33
Issue number2
DOIs
Publication statusPublished - 1997

Keywords

  • Alkylating drug
  • Antineoplastic agent
  • In vivo
  • Melphalan
  • Mouse tumours
  • Tallimustine

ASJC Scopus subject areas

  • Cancer Research
  • Hematology
  • Oncology

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