PHARMACOKINETICS AND METABOLISM OF VINBLASTINE IN HUMANS

  • 1 January 1977
    • journal article
    • research article
    • Vol. 37  (8) , 2597-2602
Abstract
The pharmacokinetics of the antitumor agent vinblastine in humans was examined using a radioimmunoassay specific for the Vinca alkaloids and aromatic ring [3H]vinblastine. The data were consistent with a 3 compartment open model system with the following values: .alpha. phase: T1/2 = 3.90 .+-. 1.46 min; Vc = 16.8 .+-. 7.1 l. .beta. phase: t1/2 = 53.0 .+-. 13.0 min; V.beta. = 79.0 .+-. 52.0 l; .gamma. phase: t1/2 = 1173.0 .+-. 65.0 min; V.gamma. = 1656.0 .+-. 717.0 l. Most significant was the finding that vinblastine is metabolized to deacetylvinblastine and this compound is more biologically active on a weight basis than the parent. No other biologically active metabolites appeared to be present in urine or stool.

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