Erlotinib (Tarceva®) is a specific and powerful inhibitor of the phosphorylation of the epidermal growth-factor receptor (EGFR/HER1), a tyrosine kinase receptor. This results in an inhibition of signal transduction and therefore decreased cell division and motility and increased apoptosis.
The agent is indicated for the treatment of patients with advanced metastasised non-small-cell lung carcinoma after cytostatic therapy has failed. Patients with activating EGFR mutations display a higher response during erlotinib therapy. Most frequent side effects are rash and diarrhea, and seldomly pulmonary toxicity.