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Pharmacokinetics and Metabolism of Vinblastine in Humans¹

Oncology Center, The Johns Hopkins University School of Medicine, Baltimore, Maryland 21205

The pharmacokinetics of vinblastine in humans was examined using a radioimmunoassay specific for both the Vinca alkaloids and aromatic ring [³H]vinblastine. The data were consistent with a three-compartment open model system with the following values. phase: t_1/2 = 3.90 ± 1.46 min; V_c = 16.8 ± 7.1 liters. ß phase: t_1/2 = 53.0 ± 13.0 min; V_ß = 79.0 ± 52.0 liters; phase: t_1/2 = 1173.0 ± 65.0 min; V = 1656.0 ± 717.0 liters. Most significant was the finding that vinblastine is metabolized to deacetylvinblastine and that 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 in stool.

¹ This research was supported in part by USPHS Grant CA-16157 from the National Cancer Institute, NIH, and in part by The Eli Lilly and Co., Indianapolis, Ind.

² To whom requests for reprints should be addressed, at The Johns Hopkins Oncology Center, 601 North Broadway, Baltimore, Md. 21205.

Received 11/30/76. Accepted 4/22/77.