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Generic Name Erlotinib 25 mg, 100 mg and 150 mg tablets Brand Name Tarceva Manufacturer OSI Pharmaceuticals Summary Erlotinib, being a Human Epidermal Growth Factor Receptor Type 1/Epidermal Growth Factor Receptor (HER1/EGFR) tyrosine kinase inhibitor, is indicated for the treatment of patients with locally advanced or metastatic non-small-cell lung cancer (NSCLC) after failure of at least one prior chemotherapy regimen. It has proven effective across most patient populations, regardless of prognostic factors. Co-treatment with the potent CYP3A4 inhibitor or inducers should be cautious. Most common side effects associated with erlotinib are mild to moderate rash, diarrhea and pulmonary toxicity. Due to the fact that the drug is eliminated by hepatic metabolism and biliary excretion, it should be administered cautiously in patients with hepatic impairment. Use also with care in pregnancy. Mechanism of Action Erlotonib is a Human Epidermal Growth Factor Receptor Type 1/Epidermal Growth Factor Receptor (HER1/EGFR) tyrosine kinase inhibitor. It inhibits the intracellular phosphorylation of tyrosine kinase associated with the epidermal growth factor receptor, which is expressed on the cell surface of normal cells and cancer cells. Pharmacokinetics Absorption : Erlotinib is about 60% absorbed after oral administration, its bioavailability is substantially increased by food to almost 100% and peak plasma levels occur 4 hours after dosing. Its half-life is about 36 hours and it is cleared predominantly by CYP3A4 metabolism and to a lesser extent by CYP1A2. Distribution : Following absorption, erlotinib is approximately 93% protein bound to albumin and alpha-1 acid glycoprotein and it has an apparent volume of distribution of 232