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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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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.
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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: |
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Targets
Tubulin is the major constituent of microtubules. It binds two moles of GTP, one at an exchangeable site on the beta chain and one at a non-exchangeable site on the alpha-chain
| UniProt ID: | Q71U36 | |||||
|---|---|---|---|---|---|---|
| Gene: | TUBA1A | |||||
| Actions: | adduct | |||||
| References: |
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Tubulin is the major constituent of microtubules. It binds two moles of GTP, one at an exchangeable site on the beta chain and one at a non-exchangeable site on the alpha-chain
| UniProt ID: | P07437 | |||||
|---|---|---|---|---|---|---|
| Gene: | TUBB | |||||
| Actions: | adduct | |||||
| References: |
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In the elongating spermatid it is associated with the manchette, a specialized microtubule system present during reshaping of the sperm head (By similarity)
| UniProt ID: | Q9UJT1 | |||||
|---|---|---|---|---|---|---|
| Gene: | TUBD1 | |||||
| Actions: | adduct | |||||
| References: |
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Tubulin is the major constituent of microtubules. Gamma tubulin is found at microtubule organizing centers (MTOC) such as the spindle poles or the centrosome, suggesting that it is involved in the minus-end nucleation of microtubule assembly
| UniProt ID: | P23258 | |||||
|---|---|---|---|---|---|---|
| Gene: | TUBG1 | |||||
| Actions: | adduct | |||||
| References: |
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| UniProt ID: | Q9UJT0 | |||||
|---|---|---|---|---|---|---|
| Gene: | TUBE1 | |||||
| Actions: | adduct | |||||
| References: |
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Transcription factor that recognizes and binds to the enhancer heptamer motif 5'-TGA[CG]TCA-3'
| UniProt ID: | P05412 | |||||
|---|---|---|---|---|---|---|
| Gene: | JUN | |||||
| Actions: | other/unknown | |||||
| References: |
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Enzymes
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4- hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. The enzyme also hydroxylates etoposide
| UniProt ID: | P08684 | ||
|---|---|---|---|
| Gene: | CYP3A4 | ||
| Actions: | substrate, inhibitor | ||
| References: |
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Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic antidepressants
| UniProt ID: | P10635 | |
|---|---|---|
| Gene: | CYP2D6 | |
| Actions: | substrate, inhibitor | |
| References: |
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Transporters
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells
| UniProt ID: | P08183 | ||||||||||||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Gene: | ABCB1 | ||||||||||||||||||||||||||||||||||||
| Actions: | substrate, inhibitor, inducer | ||||||||||||||||||||||||||||||||||||
| References: |
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May participate directly in the active transport of drugs into subcellular organelles or influence drug distribution indirectly. Confers resistance to anticancer drugs. Transports LTC4. May protect milk against xenobiotics
| UniProt ID: | P33527 | ||||
|---|---|---|---|---|---|
| Gene: | ABCC1 | ||||
| Actions: | substrate, inhibitor, inducer | ||||
| References: |
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Mediates hepatobiliary excretion of numerous organic anions. May function as a cellular cisplatin transporter
| UniProt ID: | Q92887 | |||||
|---|---|---|---|---|---|---|
| Gene: | ABCC2 | |||||
| Actions: | substrate, inhibitor, inducer | |||||
| References: |
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May participate directly in the active transport of drugs into subcellular organelles or influence drug distribution indirectly. Transports glutathione conjugates as leukotriene-c4 (LTC4) and N-ethylmaleimide S-glutathione (NEM-GS)
| UniProt ID: | O95255 | |
|---|---|---|
| Gene: | ABCC6 | |
| Actions: | inhibitor | |
| References: |
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Involved in the ATP-dependent secretion of bile salts into the canaliculus of hepatocytes
| UniProt ID: | O95342 | ||
|---|---|---|---|
| Gene: | ABCB11 | ||
| Actions: | substrate, inhibitor | ||
| References: |
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Mediates tubular uptake of organic compounds from circulation. Mediates the influx of agmatine, dopamine, noradrenaline (norepinephrine), serotonin, choline, famotidine, ranitidine, histamin, creatinine, amantadine, memantine, acriflavine, 4-[4-(dimethylamino)-styryl]-N-methylpyridinium ASP, amiloride, metformin, N-1-methylnicotinamide (NMN), tetraethylammonium (TEA), 1-methyl-4-phenylpyridinium (MPP), cimetidine, cisplatin and oxaliplatin. Cisplatin may develop a nephrotoxic action. Transport of creatinine is inhibited by fluoroquinolones such as DX-619 and LVFX. This transporter is a major determinant of the anticancer activity of oxaliplatin and may contribute to antitumor specificity
| UniProt ID: | O15244 | |
|---|---|---|
| Gene: | SLC22A2 | |
| Actions: | substrate | |
| References: |
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