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 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.

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.

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.