Clinical testing of Ro-03-8799 - pharmacokinetics, toxicology, tissue and tumor concentrations

Journal Article · Sat Sep 01 04:00:00 EDT 1984 · Int. J. Radiat. Oncol., Biol. Phys.; (United States)

DOI:https://doi.org/10.1016/0360-3016(84)90544-3· OSTI ID:6003683

Saunders, M I; Anderson, P J; Bennett, M H; Dische, S; Minchinton, A; Stratford, M R.L.; Tothill, M

Ro-03-8799, a lipophilic nitroimidazole with a basic side chain, has now been administered intravenously to 69 patients. The elimination half-life in plasma was 5.1 hr and the plasma concentration at 30 min was 14.8 ..mu..g/ml standardized to a dose of 1 g per square meter of surface area. Immediate symptoms of malaise, heat, sweating and disorientation limit the amount of the drug which may be given on any one occasion. However, a dose of 750 mg per square meter of surface area may be given combined with daily radiotherapy. The data suggest that when given with a 20 fraction course of radiotherapy, sensitization of hypoxic cells may be achieved equal to a 10-fold increase in the dose of misonidazole above that presently permitted.

• Research Organization: Mount Vernon Hospital, Northwood, England
• OSTI ID: 6003683
• Journal Information: Int. J. Radiat. Oncol., Biol. Phys.; (United States), Journal Name: Int. J. Radiat. Oncol., Biol. Phys.; (United States) Vol. 10:9; ISSN IOBPD
• Country of Publication: United States
• Language: English

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62 RADIOLOGY AND NUCLEAR MEDICINE
63 RADIATION, THERMAL, AND OTHER ENVIRON. POLLUTANT EFFECTS ON LIVING ORGS. AND BIOL. MAT.
AZOLES
BIOLOGICAL HALF-LIFE
BIOLOGICAL MATERIALS
BLOOD
BLOOD PLASMA
BODY FLUIDS
HETEROCYCLIC COMPOUNDS
IMIDAZOLES
MATERIALS
MEDICINE
NITRO COMPOUNDS
NUCLEAR MEDICINE
ORGANIC COMPOUNDS
ORGANIC NITROGEN COMPOUNDS
PATIENTS
PHARMACOLOGY
RADIOLOGY
RADIOSENSITIVITY EFFECTS
RADIOTHERAPY
THERAPY
TOXICITY