[Radiosensitizing effect of a 2-nitroimidazole hydroxamate (KIN-804) to murine tumors].

We studied the toxicity, pharmacokinesis and radiosensitizing effect of a newly developed 2-nitroimidazole-1-methylacetohydroxamate (KIN-804) in C3H/He mice bearing SCC-VII tumor. They were compared with misonidazole. LD50/7 of KIN-804 and misonidazole were 3200 and 2000 mg/kg. The concentration of KIN-804 in the brain and sciatic nerve was at a very low level and its clearance from the sciatic nerve was rapid. Enhancement ratios calculated using the growth delay method were 1.50 for KIN-804 and 1.36 for misonidazole respectively when they were administered by intraperitoneal injection with a dose of 100 mg/kg. KIN-804 was considered to be a promising radiosensitizer because it obtained less toxicity and a higher radiosensitizing activity than misonidazole.
AuthorsT Tada, T Nakajima, Y Onoyama, H Nagasawa, H Hori, S Inayama
JournalNihon Igaku Hò„shasen Gakkai zasshi. Nippon acta radiologica (Nihon Igaku Hoshasen Gakkai Zasshi) Vol. 52 Issue 5 Pg. 688-90 (May 25 1992) ISSN: 0048-0428 [Print] JAPAN
PMID1508643 (Publication Type: English Abstract, Journal Article)
Chemical References
  • Hydroxamic Acids
  • Nitroimidazoles
  • Radiation-Sensitizing Agents
  • 2-nitroimidazole-1-methylacetohydroxamate
  • Animals
  • Hydroxamic Acids (pharmacokinetics, pharmacology, toxicity)
  • Lethal Dose 50
  • Male
  • Mice
  • Mice, Inbred C3H
  • Neoplasms, Experimental (metabolism, pathology, radiotherapy)
  • Nitroimidazoles (pharmacokinetics, pharmacology, toxicity)
  • Radiation-Sensitizing Agents (pharmacokinetics, pharmacology, toxicity)

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