Vinblastine

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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 stick molecular model
Vinblastine stick molecular model

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.

Contents

[edit] 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.

[edit] 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]

[edit] 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.

[edit] See also

[edit] Footnotes

  1. ^ 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. 
v • d • e
Chemotherapeutic agents/Antineoplastic agents (L01)
Alkylating and alkylating-like agents
Antimetabolites
Spindle poison/mitotic inhibitor
Taxane: (Docetaxel, Larotaxel, Paclitaxel). Vinca: (Vinblastine, Vincristine, Vindesine, Vinorelbine).
Cytotoxic/antitumor antibiotics
Topoisomerase inhibitors
CI monoclonal antibodies
Photosensitizers
Tyrosine kinase inhibitors
Cyclin-dependent kinase inhibitor
Other
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