Drug/Small Molecule:
vindesine

Overview

Generic Names: Desacetylvinblastine Amide Sulfate; Vindesine Sulfate
Trade Names: DAVA; Eldesine; Eldisine
PharmGKB Accession Id: PA10232

Description

Vinblastine derivative with antineoplastic activity against cancer. Major side effects are myelosuppression and neurotoxicity. Vindesine is used extensively in chemotherapy protocols (antineoplastic combined chemotherapy protocols). [PubChem]

Indication

For the treatment of acute leukaemia, malignant lymphoma, Hodgkin's disease, acute erythraemia and acute panmyelosis

ATC Therapeutic Category

  • L01CA:Vinca alkaloids and analogues

Pharmacology and Interactions

Mechanism Of Action

Vindesine acts by causing the arrest of cells in metaphase mitosis through its interaction with tubulin. The drug is cell-cycle specific for the S phase.

Pharmacology

Vindesine is indicated for the treatment of acute lymphocytic leukemia of childhood that is resistant to vincristine and non-oat cell lung cancer.Vindesine causes the arrest of cells in metaphase mitosis. It is three times more potent than vincristine and nearly 10 times more potent than vinblastine in causing mitotic arrest in in vitro studies at doses designed to arrest from 10 to 15% of the cells in mitosis. Vindesine and vincristine are approximately equipotent at dose levels that arrest 40 to 50% of the cells in mitosis. Unlike vinblastine, vindesine produces very few postmetaphase cells. Vindesine has demonstrated activity in patients who have relapsed while receiving multiple-agent treatment that included vincristine.

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

Hepatic

Protein Binding

65-75%

Half Life

24 hours.

Chemical Properties

Chemical Formula:

C43H55N5O7

SMILES Code:

CC[C@@]1(C[C@@H]2C[C@@](C3=C(CCN(C2)C1)C4=CC=CC=C4N3)(C5=C(C=C6C(=C5)[C@]78CC[N@@]9[C@H]7[C@@](C=CC9
)([C@H]([C@@]([C@@H]8N6C)(C(=O)N)O)O)CC)OC)C(=O)OC)O

(Format: OpenEye Isomeric)

Molecular Weight ( average / monoisotopic )

753.9261 / 753.4101

Curated Information

The following genes are in curated knowledge about this drug.

  Gene Relationship Evidence
Phenotype data available Genotype Data Available Literature annotations available Has annotations
ABCB1
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Pathways
No phenotype data Genotype Data Available Literature annotations available Not annotated
ABCB11
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Pathways
No phenotype data Genotype Data Available Literature annotations available Not annotated
ABCB4
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Pathways
Phenotype data available Genotype Data Available Literature annotations available Not annotated
ABCC1
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Pathways
No phenotype data Genotype Data Available Literature annotations available Not annotated
ABCC10
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Pathways
Phenotype data available Genotype Data Available Literature annotations available Not annotated
ABCC2
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Pathways
Phenotype data available Genotype Data Available Literature annotations available Has annotations
CYP3A4
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Pathways
Phenotype data available Genotype Data Available Literature annotations available Has annotations
CYP3A5
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Pathways
Phenotype data available Genotype Data Available Literature annotations available Not annotated
RALBP1
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Pathways

Non-Curated Information

A list of non-curated publications that mention this drug along with other genes is available.

Metabolizing Enzymes

Drug Targets

PharmGKB Curated Pathways

Non-Curated Information

A list of non-curated publications that mention this drug along with other drugs is available.

Curated Information

The following diseases are in curated knowledge about this drug.

  Disease Relationship Evidence
No phenotype data No genotype data Literature annotations available Not annotated
Hodgkin Disease
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Pathways
No phenotype data No genotype data Literature annotations available Not annotated
Lymphoma, Non-Hodgkin
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Pathways
No phenotype data No genotype data Literature annotations available Not annotated
Multiple Myeloma
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Pathways
Phenotype data available Genotype Data Available Literature annotations available Not annotated
Precursor Cell Lymphoblastic Leukemia-Lymphoma
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  • PK
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Pathways

Non-Curated Information

A list of non-curated publications that mention this drug along with other diseases is available.

LinkOuts

Web Resource:
Wikipedia
DrugBank:
DB00309
KEGG Drug ID:
D01769
PubChem Compound ID:
40839
PubChem Substance ID:
181645

Common Searches

Search PubMed
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Non-Curated Publications

A list of non-curated publications that mention this drug is available.

PharmGKB integrates drug information from different sources: DrugBank, Open Eye Scientific Software.
The PharmGKB is financially supported by the NIH/ NIGMS and is managed at Stanford University (U01GM61374).
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