Cat. No.   G160000

CAS. No.   184475-35-2  

Gefitinib is used to treat lung cancer. It works by slowing or stopping the growth of cancer cells. Gefitinib blocks a certain protein (an enzyme called tyrosine kinase).

On 13 July, 2015 the US Food and Drug Administration (FDA) approved gefitinib for the first-line treatment of patients with metastatic non-small cell lung cancer (NSCLC) whose tumours harbour specific types of epidermal growth factor receptor (EGFR) gene mutations, as detected by an FDA-approved test.

Gefitinib belongs to the group of medicines called antineoplastics (cancer medicines). It works by interfering with the growth of cancer cells, which are eventually destroyed.

MECHANSIM OF ACTION:

The EGFR belongs to the erbB family of four closely related cell membrane receptors: EGFR (HER1 or erbB1), erbB2(HER2), erbB3(HER3) and erbB4(HER4). These receptors comprise an extracellular ligand-binding domain, a transmembrane domain and an intracellular domain with tyrosine kinase activity mediating signal transduction. EGFR (HER 1, erbB1) activation occurs in response to ligand binding via dimerization of the receptor.

Activation of the EGFR signalling pathway in cancer cells has been linked to increased cell proliferation, angiogenesis, metastasis and decreased apoptosis. In addition, aberrant EGFR signalling in tumours has been associated with poor prognosis and drug resistance.

Gefitinib, a small molecule capable of entering the cell, competes with adenosine triphosphate at the kinase ATP binding sites of EGFR, preventing its tyrosine kinase activity, thus blocking EGFR signal transduction.

In addition to reducing proliferation in transformed cells, gefitinib induces cell cycle arrest, increases apoptosis and has antiangiogenic activity. Gefitinib has been shown to have antimetastatic properties in the following human tumour types: head and neck, prostate, breast, ovarian, colon, small-cell lung and NSCL (3, 5–7).

Factors such as the level of activated or phosphorylated EGFR and the level of ligand expression may also be important.

Some of the impurities of Gefitinib are-