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Comparison of tumor growth inhibitory and toxic effects of a new fluorouracil--nitrosourea derivative (B-3839).

Abstract
The toxic effect and anti-tumor activity of B-3839, a new molecular combination of pyrimidine antimetabolite 5-fluorouracil (5-FU) with the alkylating agent N-Chloroethyl-N-nitrosourea (BCNU), was compared to that of BCNU and 5-FU given alone and in physical combination. The tumor inhibitory effect of B-3839 was similar to that of BCNU given alone or combined with a low dose of 5-FU in the i.m. Walker tumor model. Furthermore, the bone marrow toxicity of BCNU was not significantly altered by either form of combination with 5-FU. The intestinal side effects, evaluated by measuring the decrease of marker enzyme (thymidine kinase, xanthine oxidase, alkaline phosphatase, sucrase, maltase) activities in isolated enterocytes, were dose-dependent and moderate. A significant, more than 30%, decrease occurred only if BCNU and 5-FU were given simultaneously or as B-3839. The molecular combination of the two drugs does not provide any additional advantage over their physical combination.
AuthorsN Prajda, J Kralovánszky, S Somfai-Relle, F Gál, S Kerpel-Fronius
JournalIn vivo (Athens, Greece) (In Vivo) 1988 Mar-Apr Vol. 2 Issue 2 Pg. 151-4 ISSN: 0258-851X [Print] Greece
PMID2979832 (Publication Type: Comparative Study, Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • Antineoplastic Agents
  • Nitrosourea Compounds
  • B 3839
  • Fluorouracil
  • Carmustine
Topics
  • Animals
  • Antineoplastic Agents (therapeutic use)
  • Carcinoma 256, Walker (drug therapy)
  • Carmustine (therapeutic use, toxicity)
  • Digestive System (drug effects, pathology)
  • Fluorouracil (analogs & derivatives, therapeutic use, toxicity)
  • Male
  • Nitrosourea Compounds (therapeutic use, toxicity)
  • Rats
  • Rats, Inbred Strains

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