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
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.