For the treatment of patients with locally advanced or metastatic non-small cell lung cancer after failure of at least one prior chemotherapy regimen.

The mechanism of clinical antitumor action of erlotinib is not fully characterized.Erlotinib inhibits the intracellular phosphorylation of tyrosine kinase associated with the epidermal growth factor receptor (EGFR). Specificity of inhibition with regard to other tyrosine kinase receptors has not been fully characterized. EGFR is expressed on the cell surface of normal cells and cancer cells.

Bioavailability:∼ 60 %, and increased by food to almost 100 %; protein bound to albumin and alpha-1 acid glycoprotein: ∼93%; Erlotinib is metabolized primarily by CYP3A4 and to a lesser extent by CYP1A2, and CYP1A2. Excretion: 83% in feces and 8% in urine. Elimination half-life: 36.2 hrs(median)

in patients with severe hypersensitivity to erlotinib or to any component of Tarceva

D

Avoided

Rash(75%)，Diarrhea(54%)，Anorexia (52%)，Fatigue(52%)，Dyspnea( 41%)，Cough (33%)，Nausea (33%)，Infection (24%)，Vomiting (23%)，Stomatitis( 17%)，Pruritus (13%)，Dry skin (12%)，Conjunctivitis (12%)，Keratoconjunctivitis sicca (12%)，Abdominal pain (11%)

150 mg once daily, taken at least one hour before or two hours after the ingestion of food. Dose adjustment: may require dose increase of erlotinib when concomitant use with CYP3A4 inducer; when concomitant use with CYP3A4 inhibitors, may require dose reduction of erlotinib if severe reactions occur