CAS 184475-35-2 Cancer Treatment Steroids , Antineoplastic Agents Gefitinib ZD -1839
Storage: Store at RT
Purity: ≥98% (HPLC)
CAS Number: 184475-35-2
PubChem ID: 123631
InChI Key: XGALLCVXEZPNRQ-UHFFFAOYSA-N
Solubility: DMSO (44.69), ethanol (4.47)
Appearance: white powder
Gefitinib (ZD1839) (INN, , trade name Iressa, marketed by AstraZeneca and Teva), is a drug used for certain breast, lung and other cancers. Gefitinib is an EGFR inhibitor, like erlotinib, which interrupts signaling through the epidermal growth factor receptor (EGFR) in target cells. Therefore, it is only effective in cancers with mutated and overactive EGFR. However, meta-analyses have not shown any improvement in overall survival, that is, it does not extend life.
Gefitinib is used to treat non-small cell lung cancer that has spread to other parts of the body in people with certain types of tumors. Gefitinib is in a class of medications called kinase inhibitors. It works by blocking the action of a certain naturally occurring substance that may be needed to help cancer cells multiply.
Items of analysis
White to off-white powder
Loss on drying
Residue on ignition
Max Single Impurity
≤ 0.10 %
Mechanism of action:
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 a member of a family of receptors (ErbB) which includes Her1(EGFR), Her2(erb-B2), Her3(erb-B3) and Her4 (Erb-B4). 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 anti-apoptotic Ras signal transduction cascade is inhibited, and malignant cells are inhibited.
How to use Gefitinib Tablet:
Take gefitinib by mouth once daily, with or without food, or as directed.
Medications which reduce or completely block stomach acid (e.g., proton pump inhibitors/PPIs, H2 blockers, antacids) may decrease the absorption of gefitinib. This could decrease the effectiveness of gefitinib. Consult your doctor or pharmacist if you are taking any of these medications.
Use this medication regularly in order to get the most benefit from it. To help you remember, use it at the same time each day...
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