化合物信息

Drug Groups

approved

Description

Antitumor alkaloid isolated from Vinca rosea. (Merck, 11th ed.)

Indication

For treatment of breast cancer, testicular cancer, lymphomas, neuroblastoma, Hodgkin's and non-Hodgkin's lymphomas, mycosis fungoides, histiocytosis, and Kaposi's sarcoma.

Pharmacology

Vinblastine is a vinca alkaloid antineoplastic agent. The vinca alkaloids are structurally similar compounds comprised of 2 multiringed units: vindoline and catharanthine. The vinca alkaloids have become clinically useful since the discovery of their antitumour properties in 1959. Initially, extracts of the periwinkle plant (Catharanthus roseus) were investigated because of putative hypoglycemic properties, but were noted to cause marrow suppression in rats and antileukemic effects in vitro. Vinblastine has some immunosuppressant effect. The vinca alkaloids are considered to be cell cycle phase-specific.

Toxicity

Oral, mouse: LD₅₀ = 423 mg/kg; Oral, rat: LD₅₀ = 305 mg/kg.

Affected Organisms

Biotransformation

Hepatic. Metabolism of vinblastine has been shown to be mediated by hepatic cytochrome P450 3A isoenzymes.

Half Life

Triphasic: 35 min, 53 min, and 19 hours

Protein Binding

98-99%

Elimination

The major route of excretion may be through the biliary system.

References

External Links