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" Pharmacokinetics of 13-cis-retinoic acid in patients with advanced cancer. "
Goodman, G E; Einspahr, J G; Alberts, D S; Davis, T P; Leigh, S A; Chen, H S; Meyskens, F L
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AL
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| Record Number
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910927
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LA9q50g1d7
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| Title & Author
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Pharmacokinetics of 13-cis-retinoic acid in patients with advanced cancer. [Article]\ Goodman, G E; Einspahr, J G; Alberts, D S; Davis, T P; Leigh, S A; Chen, H S; Meyskens, F L
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1982
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| Title of Periodical
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UC Irvine
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| Abstract
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13-cis-Retinoic acid (13-CRA) is a synthetic analog of vitamin A effective reversing preneoplastic lesions in both humans and animals. To study its physiochemical properties and disposition kinetics, we developed a rapid, sensitive, and precise high-performance liquid chromatography assay for 13-CRA in biological samples. This assay system resulted in a clear separation of 13-CRA from all-trans-retinoic acid and retinol and had a detection limit of 20 ng/ml plasma. Recovery was 89 +/- 6% (S.D.) at equivalent physiological concentrations with a precision of 8%. To study the disposition kinetics in humans, 13 patients received a p.o. bolus of 13-CRA and had blood samples collected at timed intervals. For the 10 patients studied on the first day of 13-CRA administration, the mean time to peak plasma concentration was 222 +/- 102 min. Interpatient peak 13-CRA plasma concentrations were found to be variable, suggesting irregular gastrointestinal absorption. Beta-Phase t 1/2 was approximately 25 hr. The prolonged terminal-phase plasma half-life may represent biliary excretion and enterohepatic circulation.
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