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  • Title: Lack of dose proportional pharmacokinetics for CI-937, an anthrapyrazole DNA intercalator, in mice.
    Author: Wong B, Nordblom G, Chang T, Whitfield L.
    Journal: Res Commun Chem Pathol Pharmacol; 1989 Nov; 66(2):191-202. PubMed ID: 2602655.
    Abstract:
    The time course of CI-937, an anthrapyrazole DNA intercalator, was studied in plasma of mice after single intravenous doses of 1.2, 8, 12, and 15 mg/kg (1/10 the LD10, 2/3 the LD10, LD10, and LD50). CI-937 concentrations in plasma were determined by a sensitive radioimmunoassay capable of quantifying 0.1 ng/ml. Area under the plasma concentration-time curve increased less than proportionally to dose. Time-averaged plasma clearance was dose-dependent, increasing from 31.1 to 63.6 ml/min/kg over the 1.2 to 12 mg/kg dose range. Terminal half-life in plasma ranged from 11 to 25 days. Fraction plasma protein bound was 69 to 76% from 10 to 10,000 ng/ml, which suggests the nonlinear behavior was not due to saturable protein binding. Potential mechanisms include autoinduction of metabolism and dose-dependent reabsorption from the gastrointestinal tract or kidneys.
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