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Vinblastine
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| Systematic (IUPAC) name | |
| ? | |
| Identifiers | |
| CAS number | |
| ATC code | L01 |
| PubChem | |
| DrugBank | |
| Chemical data | |
| Formula | C46H58N4O9 |
| Mol. mass | 810.974 g/mol |
| Pharmacokinetic data | |
| Bioavailability | n/a |
| Metabolism | Hepatic (CYP3A4-mediated) |
| Half life | 24.8 hours (terminal) |
| Excretion | Biliary and renal |
| Therapeutic considerations | |
| Pregnancy cat. | |
| Legal status | |
| Routes | Exclusively intravenous |
Vinblastine is an anti-mitotic drug used to treat certain kinds of cancer, including Hodgkin's lymphoma, non-small cell lung cancer, breast cancer and testicular cancer.
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History
Vinblastine was first isolated by Robert Noble and Charles Thomas Beer from the Madagascar periwinkle plant. Vinblastine's utility as a chemotherapeutic agent was first discovered when it was crushed into a tea. Consumption of the tea led to a decreased number of white blood cells; therefore, it was hypothesized that vinblastine might be effective against cancers of the white blood cells such as lymphoma.
Pharmacology
Vinblastine is a vinca alkaloid and a chemical analogue of vincristine. It binds tubulin, thereby inhibiting the assembly of microtubules. It is M phase cell cycle specific since microtubules are a component of the mitotic spindle and the kinetochore which are necessary for the separation of chromosomes during anaphase of mitosis. Toxicities include bone marrow suppression (which is dose-limiting), gastrointestinal toxicity, potent vesicant (blister-forming) activity, and extravasation injury (forms deep ulcers).
Vinblastine paracrystals may be comprised of tightly-packed unpolymerized tubulin or microtubules.[1]
Indications
Vinblastine is a component of a number of chemotherapy regimens, including ABVD for Hodgkin lymphoma. It is also used to treat histiocytosis according to the established protocols of the Histiocytosis Association of America.
See also
Footnotes
- ^ Starling D (1976). "Two ultrastructurally distinct tubulin paracrystals induced in sea-urchin eggs by vinblastine sulphate.". J Cell Sci 20 (1): 79–89. PMID 942954.
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- This page was last modified on 27 May 2008, at 18:32.
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