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MOSINTER GROUP LIMITED
MOSINTER GROUP LIMITED

China Bortezomib CAS 179324-69-7 VELCADE dpba BORTEZOMIB manufacturer

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Bortezomib CAS 179324-69-7 VELCADE dpba BORTEZOMIB 

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

Model No.: CAS: 179324-69-7
Production Capacity: 1 Ton/Year
Delivery Date: within 7 days
Molecular weight: 384.24
Melting Point: 122-124°C
Stability: Hygroscopic and Moisture Se...
Means of Transport: Ocean,Land,Air
Packing: According to the request of...
Molecular formula: C19H25BN4O4
Density: 1.214
Storage condition: Hygroscopic, -20°C Freezer,...

Bortezomib marketed as Velcade by Millennium Pharmaceuticals and Cytomib by Venus Remedies) is the first therapeutic proteasome inhibitor to be tested

Bortezomib(CAS: 179324-69-7)


Item

Index

Molecular Formula

C19H25BN4O4

Molecular Weight

384.24

Specification

CP/USP/EP

Content

98%min

 

Bortezomib (BAN, INN and USAN. Originally codenamed PS-341; marketed as Velcade by Millennium Pharmaceuticals and Cytomib by Venus Remedies) is the first therapeutic proteasome inhibitor to be tested in humans. It is approved in theU.S.for treating relapsed multiple myeloma and mantle cell lymphoma. In multiple myeloma, complete clinical responses have been obtained in patients with otherwise refractory or rapidly advancing disease.

Pharmacology

Structure

The drug is an N-protected dipeptide and can be written as Pyz-Phe-boroLeu, which stands for pyrazinoic acid,phenylalanine and Leucine with a boronic acid instead of a carboxylic acid. Peptides are written N-terminus to C-terminus, and this convention is used here even though the "C-terminus" is a boronic acid instead of a carboxylic acid.

Mechanism

The boron atom in bortezomib binds the catalytic site of the 26S proteasome with high affinity and specificity. In normal cells, the proteasome regulates protein expression and function by degradation of ubiquitylated proteins, and also cleanses the cell of abnormal or misfolded proteins. Clinical and preclinical data support a role in maintaining the immortal phenotype of myeloma cells, and cell-culture and xenograft data support a similar function in solid tumor cancers. While multiple mechanisms are likely to be involved, proteasome inhibition may prevent degradation of pro-apoptotic factors, permitting activation of programmed cell death in neoplastic cells dependent upon suppression of pro-apoptotic pathways. Recently, it was found that bortezomib caused a rapid and dramatic change in the levels of intracellular peptides that are produced by the proteasome. Some intracellular peptides have been shown to be biologically active, and so the effect of bortezomib on the levels of intracellular peptides may contribute to the biological and/or side effects of the drug.

Pharmacokinetics and pharmacodynamics

Bortezomib is rapidly cleared following intravenous administration. Peak concentrations are reached at about 30 minutes. Drug levels can no longer be measured after an hour. Pharmacodynamicsare measured by measuring proteasome inhibition in peripheral blood mononuclear cells. The much greater sensitivity of myeloma cell lines and mantle cell lines to proteasome inhibition compared with normal peripheral blood mononuclear cells and most other cancer cell lines is poorly understood.

Costs

UK

NICE recommended against Velcade in Oct 2006 due to its cost.

The company proposed a cost reduction for multiple myeloma, and this was taken up in theUK.

Adverse effects

Bortezomib is associated with peripheral neuropathy in 30% of patients; occasionally, it can be painful. This can be worse in patients with pre-existing neuropathy. In addition,myelosuppression causing neutropenia and thrombocytopenia can also occur and be dose-limiting. However, these side effects are usually mild relative to bone marrow transplantation and other treatment options for patients with advanced disease. Bortezomib is associated with a high rate of shingles, although prophylactic acyclovir can reduce the risk of this.

Gastro-intestinal (GI) effects and asthenia are the most common adverse events.

Drug interactions

Green tea extract epigallocatechin gallate (EGCG), which had been expected to have a synergistic effect, was found by Encouse B. Golden, et al. to reduce the effectiveness of bortezomib.

Therapeutic efficacy

Two open-label, phase II trials (SUMMIT and CREST) established the efficacy of bortezomib 1.3 mg/m2 (with or without dexamethasone) administered by intravenous bolus on days 1,4,8, and 11 of a 21-day cycle for a maximum of eight cycles in heavily pretreated patients with relapsed/refractory multiple myeloma.The phase III APEX trial demonstrated the superiority of bortezomib 1.3 mg/m2 over a high-dose dexamethasone regimen (e.g. median TTP 6.2 vs 3.5 months, and 1-year survival 80% vs 66%).


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Company Info

MOSINTER GROUP LIMITED [China (Mainland)]

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

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