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How does gefitinib work?

Gefitinib acts by inhibiting EGFR signal transduction pathways. Gefitinib selectively binds to the EGFR-tyrosine kinase domain, preventing ATP from binding and blocking subsequent receptor autophosphorylation, which results in the inhibition of signal transduction. Preclinical in Vitro Studies.Author: Cited by: Publish Year: 

What does gefitinib do to a cancer cell? Gefitinib is a type of targeted cancer drug called a tyrosine kinase inhibitor (TKI). Tyrosine kinase is a protein that sends signals telling cancer cells to grow. Gefitinib bocks these signals. For gefitinib to work the cancer cells need to have receptors for a protein called epidermal growth factor (EGFR).

What are the side effects of taking gefitinib? Gefitinib side effects. Get emergency medical help if you have signs of an allergic reaction: hives; difficult breathing; swelling of your face, lips, tongue, or throat.

What does gefitinib do to the tyrosine kinase? Mechanistically, gefitinib binds to the ATP-rich site of EGFR’s tyrosine kinase and inhibits its phosphorylation, resulting in blockade of cyclin-dependent kinase activity and a G1 phase cell cycle arrest [14–16].

How is gefitinib used in the treatment of NSCLC? Gefitinib is an orally administered, small-molecule EGFR TKI that initially held great promise in the treatment of NSCLC. With the failure of a large, randomized, multicenter trial of gefitinib versus placebo for the second- or third-line treatment of NSCLC (Thatcher et al. 2005a ), gefitinib use has been severely restricted.

What do you need to know about gefitinib for cancer?

What do you need to know about gefitinib for cancer? For gefitinib to work the cancer cells need to have receptors for a protein called epidermal growth factor (EGFR). Your doctor will test the cancer cells for this. Gefitinib is a tablet.

What does gefitinib do to the tyrosine kinase? Mechanistically, gefitinib binds to the ATP-rich site of EGFR’s tyrosine kinase and inhibits its phosphorylation, resulting in blockade of cyclin-dependent kinase activity and a G1 phase cell cycle arrest [14–16].

Which is the most common side effect of Gefitinib? The most frequent side effect of gefitinib and the class of EGFR inhibitors is skin toxicity (50–60%). This develops as an acneiform rash, especially pronounced in the skin of the face and upper trunk. In more severe cases, skin toxicity may extend to the lower body.

Which is the target of gefitinib in SkBr3 cells? In accordance with the foxm1 downregulation by gefitinib, the gefitinib target EGFR upregulated the FOXM1 protein level in SKBR3 cells ( McGovern et al., 2009 ). In SKBR3 cells, overexpression of FOXM1c reduced the level of apoptosis induced by gefitinib ( McGovern et al., 2009 ).