Vinblastine

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Vinblastine
Systematic (IUPAC) name
?
Identifiers
CAS number	865-21-4
ATC code	L01 CA01
PubChem	8935
DrugBank	APRD00708
Chemical data
Formula	C₄₆H₅₈N₄O₉
Mol. weight	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 a drug used to treat certain kinds of cancer, including Hodgkin's lymphoma, non-small cell lung cancer, breast cancer and testicular cancer.

1 History
2 Pharmacology
3 Indications
4 See also
5 Footnotes

[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 estabilished protocols of the Histiocytosis Association of America.

[edit] See also

[edit] 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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Chemotherapeutic agents/Antineoplastic agents (L01) edit - Chemotherapy regimens
Alkylating agents:	Nitrogen mustards: ( Chlorambucil, Chlormethine, Cyclophosphamide, Ifosfamide, Melphalan). Nitrosoureas: ( Carmustine, Fotemustine, Lomustine, Streptozocin). Platinum: ( Carboplatin, Cisplatin, Oxaliplatin, BBR3464). Busulfan, Dacarbazine, Mechlorethamine, Procarbazine, Temozolomide, ThioTEPA, Uramustine
Antimetabolites:	Folic acid: ( Methotrexate, Pemetrexed, Raltitrexed). Purine: ( Cladribine, Clofarabine, Fludarabine, Mercaptopurine, Tioguanine). Pyrimidine: ( Capecitabine). Cytarabine, Fluorouracil, Gemcitabine
Plant alkaloids:	Taxane: ( Docetaxel, Paclitaxel). Vinca: ( Vinblastine, Vincristine, Vindesine, Vinorelbine).
Cytotoxic/antitumor antibiotics:	Anthracycline family: (Daunorubicin, Doxorubicin, Epirubicin, Idarubicin, Mitoxantrone, Valrubicin). Bleomycin, Hydroxyurea, Mitomycin
Topoisomerase inhibitors:	Topotecan, Irinotecan, Podophyllum: ( Etoposide, Teniposide).
Monoclonal antibodies:	Alemtuzumab, Bevacizumab, Cetuximab, Gemtuzumab, Panitumumab, Rituximab, Trastuzumab
Photosensitizers:	Aminolevulinic acid, Methyl aminolevulinate, Porfimer sodium, Verteporfin
Kinase inhibitors:	Dasatinib, Erlotinib, Gefitinib, Imatinib, Lapatinib, Nilotinib, Sorafenib, Sunitinib, Vandetanib (ZD6474)
Other:	Alitretinoin, Altretamine, Amsacrine, Anagrelide, Arsenic trioxide, Asparaginase, Bexarotene, Bortezomib, Denileukin diftitox, Estramustine, Hydroxycarbamide, Pentostatin, Masoprocol, Mitotane, Pegaspargase, Tretinoin