Anti - Cancer #3249535

gefitinib is a selective small molecule inhibitor of the epidermal growth factor receptor tyrosine kinase and is an effective treatment for patients with tumours with activating mutations of the egfr tyrosine kinas domain regardless of line of therapy. this drug used for the treatment of locally advanced or metastatic non-small cell lung cancer, after failure of both platinum-based and taxane-based chemotherapies.

geftinat 250mg tablets is manufactured by natco pharma india and contains the drug gefitinib i.p 250 mg in each tablet that is a targeted therapy.gefitinib tablets which classified as a signal transduction inhibitor. gefitinib i.p 250mg inhibits egfr tyrosine kinase by binding to the adenosine triphosphate (atp)-binding site of the enzyme.

mechanism of action and pharmacodynamic effects

the epidermal growth factor and its receptor have been identified as key drivers in the process of cell growth and proliferation for normal and cancer cells.egfr activating mutation within a cancer cell is an important factor in promotion of tumour cell growth, blocking of apoptosis, increasing the production of angiogenic factors and facilitating the processes of metastasis.

no clinically relevant activity has been shown in patients with known egfr mutation-negative tumours.

drug class and mechanism

gefitinib tablet is a drug that is used to treat several types of lung cancer. it works by preventing lung cancer cells from growing and multiplying.

many cells, including cancer cells, have receptors on their surfaces for epidermal growth factor (egf), a protein that is normally produced by the body and that promote s the growth and multiplication of cells.

when egf attaches to epidermal growth factor receptors (egfrs), it causes an enzyme called tyrosine kinas to become active within the cells.

tyrosine kinas triggers chemical processes that cause the cells, including cancer cells, to grow, multiply, and spread.

gefitinib attaches to egfrs and thereby blocks the attachment of egf and the activation of tyrosine kinas. this mechanism for stopping cancer cells from growing and multiplying is very different from the mechanisms of chemotherapy and hormonal therapy. gefitinib was approved by the fda in may 2003.

uses of geftinib tablets

gefitinib is prescribed to treat lung cancer. it is proven to help to slow down cancerous cells growth and reproduction. it works by blocking a certain protein enzyme called tyrosine kinase.

dosage and administration

most patients who have been prescribed geftinib tablets are told to dose once a day, with or without food. unless otherwise instruct by your physician, tablets should always be swallowed whole and should not be chewed, crushed or dissolved in liquid.

erlotinib is an epidermal growth factor receptor/human epidermal growth factor receptor type 1 tyrosine kinas inhibitor. erlotinib tablet potently inhibits the intracellular phosphorylation of egfr. egfr is expressed on the cell surface of normal cells and cancer cells.

the potent effectiveness of erlotinib in blocking egfr-mediated signalling in these egfr mutation positive tumours is attributed to the tight binding of erlotinib to the atp-binding site in the mutated kinas domain of the egfr.

due to the blocking of downstream-signalling, the proliferation of cells is stopped, and cell death is induced through the intrinsic apoptotic pathway.

tumour regression is observed in mouse models of enforced expression of these egfr activating mutations.

erlotinib dosing information

usual adult dose for non-small cell lung cancer:

150 mg orally once a day

duration of therapy: until disease progression or unacceptable toxicity

uses:

first-line treatment of patient with metastatic non-small cell lung cancer (nsclc) whose tumors have epidermal growth factor receptor (egfr) exon 19 deletions or exon 21 (l858r) substitution mutations

maintenance treatment of patient with locally advanced or metastatic nsclc whose disease has not progressed after four cycle of platinum-based first-line chemotherapy.

erlotinib tablets side effects

get emergency medical help if you have any signs of an allergic reaction to erlotinib: hives; difficult breathing; swelling of your face, lips, tongue, or throat.

do not use erlotinib at once if you have:

sudden chest pain

discomfort

wheezing

dry cough

feeling short of breath