Erlotinib, a kinase inhibitor, is a quinazolinamine with the chemical name N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)4-quinazolinamine. Erlotinib reversibly inhibits the kinase activity of EGFR, preventing autophosphorylation of tyrosine residues associated with the receptor and thereby inhibiting further downstream signaling. Erlotinib binding affinity for EGFR exon 19 deletion or exon 21 (L858R) mutations is higher than its affinity for the wild type receptor. Erlotinib inhibition of other tyrosine kinase receptors has not been fully characterized.
Erlocent 100 Tablet
Locally advanced or metastatic non-small cell lung carcinoma: 150 mg once daily until disease progression or unacceptable toxicity. Reduce dose in decrements of 50 mg when necessary.
Locally advanced, unresectable or metastatic pancreatic cancer: As 1st-line treatment with gemcitabine: 100 mg once daily, reduce dose in decrements of 50 mg when necessary.
Patient on CYP3A4 or CYP1A2 inhibitor: Reduce dose in decrements of 50 mg when necessary.
Smokers or patient on CYP3A4 inducer: Increase dose as tolerated in increments of 50 mg at 2-wk intervals.