药品详细

Vindesine(长春地辛)

基本信息
剂型规格
适应症
药理
临床
理化性质
相互作用
文档
专利
Pathway
文献
序列

化学结构式图

中文名

长春地辛

英文名

Vindesine

分子式

C₄₃H₅₅N₅O₇

化学名

methyl (13S,15S,17S)-13-[(1R,9R,10S,11R,12R,19R)-10-carbamoyl-12-ethyl-10,11-dihydroxy-5-methoxy-8-methyl-8,16-diazapentacyclo[10.6.1.0^{1,9}.0^{2,7}.0^{16,19}]nonadeca-2(7),3,5,13-tetraen-4-yl]-17-ethyl-17-hydroxy-1,11-diazatetracyclo[13.3.1.0^{4,12}.0^{5,10}]nonadeca-4(12),5,7,9-tetraene-13-carboxylate

分子量

Average: 753.9261
Monoisotopic: 753.410149139

CAS号

59917-39-4

ATC分类

L01C 植物碱和其他天然产物

药物类型

small molecule

阶段

approved

商品名

DAVA;Eldesine;Eldisine;

同义名

Desacetylvinblastine Amide Sulfate;Vindesine Sulfate;

基本介绍

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]

生产厂家

封装厂家

参考

Synthesis Reference	Not Available
General Reference	Not Available

剂型

规格

化合物类型

Type	small molecule

Classes

Tryptamines and Derivatives

Substructures

Carbonyl Compounds
Carboxylic Acids and Derivatives
Hydroxy Compounds
Alkanes and Alkenes
Acetates
Indoles and Indole Derivatives
Phenols and Derivatives
Amino Ketones
Aliphatic and Aryl Amines
Pyrroles
Phenylacetates
Pyrrolidines
Ethers
Benzene and Derivatives
Carbamates and Derivatives
Alcohols and Polyols
Phenethylamines
Heterocyclic compounds
Aromatic compounds
Anisoles
Carboxamides and Derivatives
Phenylpropylamines
Tryptamines and Derivatives
Imines
Phenyl Esters
Anilines
Amphetamines
Piperidines
Pyrrolines

适应症

Cancer 癌症;

药理

Indication

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

Pharmacodynamics

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.

Mechanism of action

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

Absorption

Not Available

Volume of distribution

Not Available

Protein binding

65-75%

Metabolism

Hepatic

Important The metabolism module of DrugBank is currently in beta. Questions or suggestions? Please contact us.

Substrate	Enzymes	Product
Vindesine	Cytochrome P450 3A4	Unknown	Details

Route of elimination

Not Available

Half life

24 hours.

Clearance

Not Available

Toxicity

Not Available

Affected organisms

Humans and other mammals

Pathways

Pathway	Name	SMPDB ID
	Vindesine Pathway	SMP00438

理化性质

Properties

State

solid

Experimental Properties

Property	Value	Source
melting point	230-232 °C	Not Available
logP	2.9	Not Available

Predicted Properties

Property	Value	Source
water solubility	7.00e-02 g/l	ALOGPS
logP	3.53	ALOGPS
logP	2.79	ChemAxon
logS	-4	ALOGPS
pKa (strongest acidic)	11.34	ChemAxon
pKa (strongest basic)	8.68	ChemAxon
physiological charge	2	ChemAxon
hydrogen acceptor count	9	ChemAxon
hydrogen donor count	5	ChemAxon
polar surface area	164.82	ChemAxon
rotatable bond count	7	ChemAxon
refractivity	210.32	ChemAxon
polarizability	82.58	ChemAxon

药物相互作用

Drug	Interaction
Mitomycin	Potentially severe lung toxicity
Quinupristin	This combination presents an increased risk of toxicity

食物相互作用

Not Available

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