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Vinorelbine tartrate

Overview Pharmacological effects Clinical evaluation Adverse reactions Chemical properties Application
Vinorelbine tartrate
Vinorelbine tartrate structure
CAS No.
125317-39-7
Chemical Name:
Vinorelbine tartrate
Synonyms
NVB;KW-2307;Eunades;NAVELBINE;Pacilitaxel;VINORELBINE(RG);lbine Ditartrate;butanedioate(1:2);NAVELBINE TARTRATE;Vinorelbin artrate
CBNumber:
CB8761554
Molecular Formula:
C53H66N4O20
Formula Weight:
1079.11
MOL File:
125317-39-7.mol

Vinorelbine tartrate Properties

Melting point:
181-183°C
storage temp. 
2-8°C
solubility 
H2O: 10 mg/mL
form 
powder
color 
off-white
InChIKey
PMDHUNWDGZSEMN-WTUOTUPFSA-N
CAS DataBase Reference
125317-39-7(CAS DataBase Reference)
FDA UNII
253GQW851Q
SAFETY
  • Risk and Safety Statements
Symbol(GHS) 
GHS07,GHS06
Signal word  Danger
Hazard statements  H300-H317
Precautionary statements  P280
Hazard Codes  Xi
Risk Statements  43
Safety Statements  26-36
RIDADR  UN 1544PSN1 6.1 / PGII
WGK Germany  3
HS Code  29339900

Vinorelbine tartrate price More Price(4)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Sigma-Aldrich V2264 Vinorelbine ditartrate salt hydrate ≥98% (HPLC), powder 125317-39-7 5mg $88.5 2018-11-13 Buy
Sigma-Aldrich 1714506 Vinorelbine tartrate 125317-39-7 200mg $3388.35 2019-12-02 Buy
Cayman Chemical 21262 Vinorelbine (tartrate) 125317-39-7 50mg $245 2019-12-02 Buy
Sigma-Aldrich Y0000463 Vinorelbine tartrate European Pharmacopoeia (EP) Reference Standard 125317-39-7 y0000463 $183 2019-12-02 Buy

Vinorelbine tartrate Chemical Properties,Uses,Production

Overview

Vinorelbine belongs to vinblastine derivatives, its action is similar to vincristine. It is first marketed in 1989 in France. The main role is to combine tubulin, consequently, it causes microtubule formation disorder during cells mitosis.
Vinorelbine belongs to cycle specific drugs, it is used clinically in the treatment of non-small cell lung cancer (NSCLC) and breast cancer, ovarian cancer, head and neck squamous cell carcinoma, leukemia. In addition,it also has a strong inhibitory effect on small cell lung cancer, colon cancer, brain tumors, malignant melanoma.

Pharmacological effects

Vinorelbine tartrate is the tartrate form of vinorelbine ,it is a semi-synthetic  vincristine compound, it belongs to M phase specific drugs, mechanism of action is similar to vincristine . Mainly it , by selectively blocking mitotic cell tubulin polymerization to form microtubule and  inducing tubulin depolymerization , impedes spindle microtubules,and it makes cell division stop  in the middle, and it has few effect on the synthetic tubulin in the shaft of nerve cells. Since NVB affinity for axonal microtubules is poor, only when there is a high concentration of it ,it has effect on axonal , so it has the lower neurotoxicity than other vincristine drugs,and it  has a greater therapeutic index. Human pharmacokinetics of vinorelbine show that after intravenous administration there is a three-compartment model, the volume  of distribution is large , PPB is up to 50% to 80%, plasma clearance rate is high, the terminal elimination phase T1/2 is 40 h, it has a rapid tissue distribution, concentration in tissues is significantly higher than vincristine (VCR), vindesine (VDS). Plasma clearance is 0.8 L/(kg • h),it is mainly through biliary secretion, and it is excreted with the feces, urine excretion accounts for 10% to 15%.It has a higher efficacy and less adverse reactions of the nervous system.

Clinical evaluation

Numerous clinical studies have shown that vinorelbine is one of the most effective drugs for the treatment of non-small cell lung cancer and breast cancer, single agent response rate is 14% to 35% and 30% to 60% respectively. And DDP combination chemotherapy in NSCLC and with doxorubicin combination therapy of breast cancer, efficiency is up to 30% to 50% and 50% to 77%, respectively. It has a good effect on ovarian cancer, malignant lymphoma, head and neck cancer, esophageal cancer.

Adverse reactions

Chemical properties

White or almost white powder or crystalline powder, odorless.

Application

Antineoplastic agents

Chemical Properties

Pale Yellow Powder

Uses

An antineoplastic

Definition

ChEBI: The L-(+)-tartrate salt of vinorelbine.

brand name

Navelbine (Pierre).

General Description

Vinorelbine ditartrate is available in 1- and 5-mL vials at aconcentration of 10 mg/mL for IV use. It is FDA approvedfor the treatment of NSCLC. The agent has also been usedin treating metastatic breast cancer, cervical cancer, uterinecancer, and lung cancer especially in older patients or thosewith physical difficulties. Vinorelbine is the most lipophilicof the vinca alkaloids because of modifications of thecatharanthine ring system and dehydration of the piperidinering. This allows the agent to be quickly taken up into cellsincluding lung tissue where concentrations are 300-foldhigher than plasma concentrations. This is 3 to 13 timeshigher than the lung concentrations seen with vincristine.The agent is highly protein bound (80%–91%) and metabolizedby CYP3A. The major metabolite seen is the 4-Odesacetylderivative, which is equally active with the parentbut only formed in small quantities. The agent is eliminatedprimarily (33%–88%) in the bile with some appearing inthe urine (16%–30%). The elimination half-life is 27 to43 hours. The toxicities seen for vinorelbine includemyelosuppression, which is dose limiting but ceases upondiscontinuation of drug. This is most commonly seen as aneutropenia, and patient’s neutrophil count should be monitoredprior to and during therapy to decrease the chanceof infection. Additional toxicities include nausea/vomiting,elevation of liver function tests, alopecia, generalized fatigue,and inappropriate secretion of antidiuretic hormone.Neurotoxicity is seen with vinorelbine but occurs to a lesserdegree compared with other vinca alkaloids because of itsdecreased affinity for axonal microtubules.

Biological Activity

Selective mitotic microtubule antagonist that exhibits > 20 fold selectivity over axonal microtubules. Inhibits proliferation of multiple human tumor cell lines (IC 50 = 1.25 nM in HeLa cells) and blocks metaphase/anaphase transition by suppression of microtubule dynamics (IC 50 = 3.8 nM). Reduces spindle length by 29% and inhibits microtubule polymerization at micromolar concentrations.

Vinorelbine tartrate Preparation Products And Raw materials

Raw materials

Preparation Products


Vinorelbine tartrate Suppliers

Global( 320)Suppliers
Supplier Tel Fax Email Country ProdList Advantage
Hainan Xiyuan Chemical Technology Co., Ltd.
+86-15008981366
15008981366@163.com CHINA 9 58
Henan DaKen Chemical CO.,LTD.
+86-371-55531817
info@dakenchem.com CHINA 21829 58
Henan Tianfu Chemical Co.,Ltd.
0371-55170693
0371-55170693 info@tianfuchem.com CHINA 22626 55
Nanjing Finetech Chemical Co., Ltd.
025-85710122 17714198479
025-85710122 sales@fine-chemtech.com CHINA 890 55
Hebei Chisure Biotechnology Co., Ltd.
+8613292890173
0311 66567340 luna@speedgainpharma.com CHINA 1011 58
Shanghai Zheyan Biotech Co., Ltd.
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career henan chemical co
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Chengdu GLP Biotech Co., Ltd
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Biochempartner
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Shenzhen Nexconn Pharmatechs Ltd
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View Lastest Price from Vinorelbine tartrate manufacturers

Image Release date Product Price Min. Order Purity Supply Ability Manufacturer
2019-07-05 Vinorelbine tartrate
125317-39-7
US $10.00 / KG 1KG 99% 10 mt Hebei Guanlang Biotechnology Co., Ltd.
2019-11-12 Vinorelbine Tartrate
125317-39-7
US $0.00 / mg 5mg ≥98%(HPLC) 10 g Shanghai Standard Technology Co., Ltd.
2020-04-30 Vinorelbine tartrate
125317-39-7
US $0.00-0.00 / 公斤 1公斤 99.0% 800 ton Shaanxi Dideu Medichem Co. Ltd

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