Vinblastine drug data and news

Vinblastine drug data, resources, and news articles (when available). Onconews.org provides news on cancer research. This section, which includes profiles on medicines that may or not be cancer-related is in beta form. If things run smoothly we will be releasing a new format late in the summer of 2006.

Generic name Vinblastine
Brand Names/Synonyms AIDS-002673; AIDS002673; Indole Alkaloid; NSC49842; Nincaluicolflastine; Rozevin; Velban; Velbe; Vinblastin; Vinblastina [Dcit]; Vinblastine; Vinblastine Sulfate; Vinblastinum [Inn-Latin]; Vincaleucoblastin; Vincaleucoblastine; Vincaleukoblastine; Vincoblastine
Indication For treatment of breast cancer, testicular cancer, lymphomas, neuroblastoma, Hodgkin's and non-Hodgkin's lymphomas, mycosis fungoides, histiocytosis, and Kaposi's sarcoma.
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Description Not Available
Pharmacology Vinblastine is a vinca alkaloid antineoplastic agent. The vinca alkaloids are structurally similar compounds comprised of 2 multiringed units: vindoline and catharanthine. The vinca alkaloids have become clinically useful since the discovery of their antitumour properties in 1959. Initially, extracts of the periwinkle plant (Catharanthus roseus) were investigated because of putative hypoglycemic properties, but were noted to cause marrow suppression in rats and antileukemic effects in vitro. Vinblastine has some immunosuppressant effect. The vinca alkaloids are considered to be cell cycle phase-specific.
Mechanism Of Action The antitumor activity of vinblastine is thought to be due primarily to inhibition of mitosis at metaphase through its interaction with tubulin. Vinblastine binds to the microtubular proteins of the mitotic spindle, leading to crystallization of the microtubule and mitotic arrest or cell death.
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Dosage Forms LIQUID; POWDER FOR SOLUTION; SOLUTION
Drug_Category Antineoplastic Agents, Phytogenic; ATC:L01CA01
Absorption Not Available
Interactions Interactions for Vinblastine:

Vinblastine sulfate should not be diluted with solvents that raise or lower the pH of the resulting solution from between 3.5 and 5. Solutions should be made with normal saline (with or without preservative) and should not be combined in the same container with any other chemical. Unused portions of the remaining solutions that do not contain preservatives should be discarded immediately.

The simultaneous oral or intravenous administration of phenytoin and antineoplastic chemotherapy combinations that included vinblastine sulfate has been reported to have reduced blood levels of the anticonvulsant and to have increased seizure activity. Dosage adjustment should be based on serial blood level monitoring. The contribution of vinblastine sulfate to this interaction is not certain. The interaction may result from either reduced absorption of phenytoin or an increase in the rate of its metabolism and elimination.

Caution should be exercised in patients concurrently taking drugs known to inhibit drug metabolism by hepatic cytochrome P450 isoenzymes in the CYP 3A subfamily, or in patients with hepatic dysfunction. Concurrent administration of vinblastine sulfate with an inhibitor of this metabolic pathway (such as erythromycin, doxorubicin, or etoposide) may cause an earlier onset and/or an increased severity of side effects.

Toxicity Oral, mouse: LD50 = 423 mg/kg; Oral, rat: LD50 = 305 mg/kg.
Organisms Affected Humans and other mammals
Chemical IUPAC Name Not Available
Chemical Formula C46H58N4O9
Molecular Weight 810.974 g/mol
Smiles String CCC1(CC2CC(C3=C(CCN(C2)C1)C4=CC=CC=C4N3)(C5=C(C=C6C(=C5)C78CCN9C7C(C=CC9)(C(C(C8N6C)(C(=O)OC)O)OC(=O)C)CC)OC)C(=O)OC)O
Melting Point 267 oC
Water Solubility Negligible
State Solid (crystalline powder)
LogP/Hphobicity 5.587
Isoelectric Point Not Available
Biotransformation Hepatic. Metabolism of vinblastine has been shown to be mediated by hepatic cytochrome P450 3A isoenzymes.
Half Life Triphasic: 35 min, 53 min, and 19 hours
Protein Binding [%] 98-99%
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Drug Reference http://www.drugs.com/cons/Vinblastine.html
http://www.rxlist.com/cgi/generic3/vinblastine.htm
Drug Type Approved Drug
Accession No APRD00708
CAS Registry Number 865-21-4
KEGG Compound ID C07201
PubChem ID SID:156698
PharmGKB ID PA451877
SwissProt ID Not Available
GenBank ID Not Available
Drug ID Number [DIN] 2183056

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