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QuickView for Vinblastine (compound)


PubChem
Name: Vinblastine
PubChem Compound ID: 11957719
Description: Antitumor alkaloid isolated from Vinca rosea. (Merck, 11th ed.)
Molecular formula: C46H60N4O13S
Molecular weight: 909.054 g/mol
Synonyms:
EU-0101227
DrugBank
Identification
Name: Vinblastine
Name (isomeric): DB00570
Drug Type: small molecule
Description: Antitumor alkaloid isolated from Vinca rosea. (Merck, 11th ed.)
Brand: Vincaleucoblastine, Vinblastin, Velbe, Velban, Vincaleucoblastin, Rozevin, Vincaleukoblastine, Vinblastina [Dcit], Nincaluicolflastine, Vinblastine Sulfate, Vincoblastine, Vinblastinum [INN-Latin]
Category: Tubulin Modulators, Antineoplastic Agents, Phytogenic
CAS number: 865-21-4
Pharmacology
Indication: For treatment of breast cancer, testicular cancer, lymphomas, neuroblastoma, Hodgkin's and non-Hodgkin's lymphomas, mycosis fungoides, histiocytosis, and Kaposi's sarcoma.
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<...
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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.
Protein binding: 98-99%
Biotransformation: Hepatic. Metabolism of vinblastine has been shown to be mediated by hepatic cytochrome P450 3A isoenzymes.
Route of elimination: The major route of excretion may be through the biliary system.
Half Life: Triphasic: 35 min, 53 min, and 19 hours
Toxicity: Oral, mouse: LD50 = 423 mg/kg; Oral, rat: LD50 = 305 mg/kg.
Affected organisms: Humans and other mammals
Interactions
Drug interaction:
AprepitantAprepitant may change levels of the chemotherapy agent, vinblastine.
NatalizumabConcomitant Vinblastine and Natalizumab therapy may increase the risk of infection. Concurrent therapy should be avoided.
IndinavirIndinavir, a strong CYP3A4 inhibitor, may decrease the metabolism of Vinblastine. Consider alternate therapy to avoid Vinblastine toxicity. Monitor for changes in the therapeutic/adverse effects of Vinblastine if Indinavir is initiated, discontinued or dose changed.
ConivaptanConivaptan, a strong CYP3A4 inhibitor, may decrease the metabolism of Vinblastine. Consider alternate therapy to avoid Vinblastine toxicity. Monitor for changes in the therapeutic/adverse effects of Vinblastine if Conivaptan is initiated, discontinued or dose changed.
ImatinibImatinib, a strong CYP3A4 inhibitor, may decrease the metabolism of Vinblastine. Consider alternate therapy to avoid Vinblastine toxicity. Monitor for changes in the therapeutic/adverse effects of Vinblastine if Imatinib is initiated, discontinued or dose changed.
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