The pharmacokinetics in mice and dogs of nitroimidazole radiosensitizers and chemosensitizers more lipophilic than misonidazole
The pharmacokinetic properties of nitroimidazole radiosensitizers and chemosensitizers more lipophilic than misonidazole (MISO) were examined. In dogs, 2 analogues showed comparable peak plasma concentrations with considerable shorter half-lives (t1/2) and reduced areas under curves (AUC). Benznidazole (R0 07-1051) had a much longer t1/2, a higher AUC, and somewhat higher peak concentrations. In mice tumor/plasma, brain/plasma, and tumor/brain ratios were generally similar to MISO, as was penetration of brain and peripheral nerve by benznidazole in dogs. Selection of lipophilic analogues with appropriate pharmacokinetic properties may facilitate accommodation of the potentially different requirements for improved radiosensitization or chemosensitization.
- Research Organization:
- Dept. of Clinical Veterinary Medicine, Cambridge, England
- OSTI ID:
- 6722315
- Journal Information:
- Int. J. Radiat. Oncol., Biol. Phys.; (United States), Journal Name: Int. J. Radiat. Oncol., Biol. Phys.; (United States) Vol. 8:3/4; ISSN IOBPD
- Country of Publication:
- United States
- Language:
- English
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63 RADIATION, THERMAL, AND OTHER ENVIRON. POLLUTANT EFFECTS ON LIVING ORGS. AND BIOL. MAT.
ANIMALS
ANTINEOPLASTIC DRUGS
AZOLES
BIOLOGICAL HALF-LIFE
BIOLOGICAL MATERIALS
BLOOD
BLOOD PLASMA
BODY
BODY FLUIDS
BRAIN
CENTRAL NERVOUS SYSTEM
DISEASES
DOGS
DRUGS
HETEROCYCLIC COMPOUNDS
IMIDAZOLES
KINETICS
MAMMALS
MATERIALS
MICE
MISONIDAZOLE
NEOPLASMS
NERVOUS SYSTEM
NITRO COMPOUNDS
ORGANIC COMPOUNDS
ORGANIC NITROGEN COMPOUNDS
ORGANS
PHARMACOLOGY
RADIOSENSITIZERS
RODENTS
VERTEBRATES