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MedKoo product information:

 

Gefitinib

 

Gefitinib is an anilinoquinazoline with antineoplastic activity. Gefitinib inhibits the catalytic activity of numerous tyrosine kinases including the epidermal growth factor receptor (EGFR), which may result in inhibition of tyrosine kinase-dependent tumor growth. Specifically, this agent competes with the binding of ATP to the tyrosine kinase domain of EGFR, thereby inhibiting receptor autophosphorylation and resulting in inhibition of signal transduction. Gefitinib may also induce cell cycle arrest and inhibit angiogenesis. Gefitinib (INN) (Iressa) is a drug used in the treatment of certain types of cancer. Gefitinib is an EGFR inhibitor, like erlotinib, which interrupts a growth factor in cancer cells. It is marketed by AstraZeneca and Teva. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).

 

  

MedKoo Code#:  100140

Name:  Gefitinib

CAS#:  184475-35-2

 

Synonym:  US brand name: Iressa. Code name: ZD 1839.

 

IUPAC/Chemical name:

N-(3-chloro-4-fluorophenyl)-7-methoxy-6-(3-morpholinopropoxy)quinazolin-4-amine

 

Chemical structure:

Theoretical analysis :

  

 

 

MedKoo Code#: 100140
Name:  Gefitinib
CAS#:  184475-35-2

Chemical Formula: C22H24ClFN4O3

Exact Mass: 446.15210

Molecular Weight: 446.90

Elemental Analysis: C, 59.13; H, 5.41; Cl, 7.93; F, 4.25; N, 12.54; O, 10.74

 

 

Availability and price:

 

Gefitinib (98%) is in stock.

100 mg / $190.00

500 mg / $350.00

1 g / $450.00

 

For quotation, question, and order, please send email to sales@medkoo.com to describe your needs. A representative will respond your email shortly. We offer big discount for orders of bulk quantities.

 

Quality control data:

Product will be shipped with supporting analytical data.

 

 

Information about this agent

 

According to http://en.wikipedia.org/wiki/Gefitinib, Gefitinib is the first selective inhibitor of epidermal growth factor receptor's (EGFR) tyrosine kinase domain. Thus gefitinib is an EGFR inhibitor. The target protein (EGFR) is also sometimes referred to as Her1 or ErbB-1 depending on the literature source. EGFR is overexpressed in the cells of certain types of human carcinomas - for example in lung and breast cancers. This leads to inappropriate activation of the anti-apoptotic Ras signalling cascade, eventually leading to uncontrolled cell proliferation. Research on gefitinib-sensitive non-small cell lung cancers has shown that a mutation in the EGFR tyrosine kinase domain is responsible for activating anti-apoptotic pathways.  These mutations tend to confer increased sensitivity to tyrosine kinase inhibitors such as gefitinib and erlotinib. Of the types of non-small cell lung cancer histologies, adenocarcinoma is the type that most often harbors these mutations. These mutations are more commonly seen in Asians, women, and non-smokers (who also tend to more often have adenocarcinoma). Gefitinib inhibits EGFR tyrosine kinase by binding to the adenosine triphosphate (ATP)-binding site of the enzyme. Thus the function of the EGFR tyrosine kinase in activating the Ras signal transduction cascade is inhibited, and malignant cells are inhibited.

 

Gefitinib is currently only indicated for the treatment of locally advanced or metastatic non-small cell lung cancer (NSCLC) in patients who have previously received chemotherapy. While gefitinib has yet to be proven to be effective in other cancers, there is potential for its use in the treatment of other cancers where EGFR overexpression is involved.  In 2004, AstraZeneca informed the United States Food and Drug Administration (FDA) that a large randomized study failed to demonstrate a survival advantage for gefitinib in the treatment of non-small cell lung cancer (NSCLC). Whether progression-free survival is prolonged is not clear from this statement. AstraZeneca also withdrew their application to market gefitinib in Europe shortly after this announcement.

Erlotinib is another EGFR tyrosine kinase inhibitor that works in the same way as gefitinib. Given the lack of survival advantage for gefitinib and the positive results for erlotinib, erlotinib has replaced gefitinib in the United States (except in patients where gefitinib has had a proven response).

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