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MOSINTER GROUP LIMITED
MOSINTER GROUP LIMITED

China Vandetanib CAS 443913-73-3 Vandetanib base manufacturer

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Vandetanib CAS 443913-73-3 Vandetanib base 

Payment Terms: T/T,L/C,WU 
Place of Origin: Shandong, China (Mainland) 
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Product Detail

Model No.: C22H24BrFN4O2
Production Capacity: 150kg/year
Delivery Date: ithin 7 days
Molecular Weight: 475.35
Content: 95%min
Density: 1.406g/cm3
Flashing point: 279.306°C
Alias: Vandetanib base
Means of Transport: Ocean,Land,Air
Packing: s per request of clients
Molecular Formula: C22H24BrFN4O2
Specification: CP/USP/EP
Brand: MOSINTER
Boiling point: 538.22°C at 760 mmHg
Name: Vandetanib

Vandetanib is an anti-cancer drug that is used for the treatment of certain tumours of the thyroid gland.

Vandetanib ( CAS: 443913-73-3)


Item

Index

Molecular Formula

C22H24BrFN4O2

Molecular Weight

475.35

Specification

CP/USP/EP

Content

95%min

Vandetanib (INN, trade name Caprelsa) is an anti-cancer drug that is used for the treatment of certain tumours of the thyroid gland. It acts as akinase inhibitor of a number of cell receptors, mainly the vascular endothelial growth factor receptor (VEGFR), the epidermal growth factor receptor (EGFR), and the RET-tyrosine kinase. The drug was developed by AstraZeneca.

Approvals and indications

Vandetanib was the first drug to be approved by FDA (April 2011) for treatment of late-stage (metastatic) medullary thyroid cancer in adult patients who are ineligible for surgery.Vandetanib was first initially marketed without a trade name, and is being marketed under the trade name Caprelsa since August 2011.

Contraindications

In patients with moderate and severe hepatic impairment, no dosage for vandetanib has been recommended, as its safety and efficacy has not been established yet.Vandetanib is contraindicated in patients with congenital long QT syndrome.

Adverse effects

Common side effects include abdominal pain and diarrhoea, rashes, prolonged QT interval, hypertension, headache, and fatigue.

Interactions

Vandetanib has been reported as a substrate for the OATP-1B1 and OATP-1B3 transporter. Interaction of vandetanib with OATP-1B1 and OATP-1B3 may alter its hepatic disposition and can lead to transporter mediated drug-drug interactions. Also, Vandetanib is an inhibitor of OATP-1B3 transporter but not for OATP-1B1.

Other drugs that prolong the QT interval can possibly add to this side effect of vandetanib. As the drug is partly metabolised via the liver enzymeCYP3A4, strong inducers of this enzyme can decrease its blood plasma concentrations. CYP3A4 inhibitors do not significantly increase vandetanib concentrations, presumably because it is also metabolised by flavin containing monooxygenase 1 (FMO1) and 3.

Pharmacokinetics

Vandetanib is well absorbed from the gut, reaches peak blood plasma concentrations 4 to 10 hours after application, and has a half-life of 19 days on average. It has to be taken for about three months to achieve a steady-state concentration. In the blood, it is almost completely (90–96%) bound to plasma proteins such as albumin. It is metabolised to N-desmethylvandetanib via CYP3A4 and to vandetanib-N-oxide via FMO1 and 3. Both of these are active metabolites. Vandetanib is excreted via the faeces (44%) and the urine (25%) in form of the unchanged drug and the metabolites.

Metabolites of vandetanib (top left): N-desmethylvandetanib (bottom left, via CYP3A4), vandetanib-N-oxide (bottom right, viaFMO1 and FMO3), both pharmacologically active, and a minor amount of a glucuronide.

Clinical trials

Non-small cell lung cancer

The drug underwent clinical trials as a potential targeted treatment for non-small-cell lung cancer. There have been some promising results from a phase III trial with docetaxel.There have also been ambivalent results when used with pemetrexed. Another trial with docetaxel was recruiting in July 2009.

AstraZeneca withdrew EU regulatory submissions for vandetanib (under the proposed trade name Zactima) in October 2009 after trials showed no benefit when the drug was administered alongside chemotherapy.

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Company Info

MOSINTER GROUP LIMITED [China (Mainland)]

sgs ico Offline Showroom in USA

Business Type:Manufacturer, Trading Company
City: Ningbo
Province/State: Zhejiang
Country/Region: China (Mainland)

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