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

Abstract

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.

• Authors: T Tada, T Nakajima, Y Onoyama, H Nagasawa, H Hori, S Inayama
• Journal: Nihon Igaku Hoshasen 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
• PMID: 1508643 (Publication Type: English Abstract, Journal Article)

Chemical References

• Hydroxamic Acids
• Nitroimidazoles
• Radiation-Sensitizing Agents
• 2-nitroimidazole-1-methylacetohydroxamate

Topics

• 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)