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Vinblastine



Vinblastine
Systematic (IUPAC) name
 ?
Identifiers
CAS number 865-21-4
ATC code L01CA01
PubChem 8935
DrugBank APRD00708
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.

D(AU) D(US)

Legal status

POM(UK) -only(US)

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.

Additional recommended knowledge

Contents

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

 
This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Vinblastine". A list of authors is available in Wikipedia.
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