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Erlotinib

State of affairs after 12 years of experience


Erlotinib (Tarceva®) was the first EGFR tyrokinase inhibitor to be authorized for the treatment of non-small-cell lung carcinoma (NSCLC). It enabled outpatient treatment, and has a more favourable adverse effects profile than the existing chemotherapy. The authorisation of erlotinib has meanwhile been specified to patients with NSCLC who have a mutation in the gene for epidermal growth factor receptor (EGFR). 

New developments regarding the treatment of NSCLC include the second- and third-generation EGFR tyrosine kinase inhibitors. Of these, osimertinib in particular appears to offer a better prognosis for progression-free survival. Dual blockage of EGFR and vascular EGFR using a combination of ramucirumab and erlotinib appears to extend the progression-free survival period further than erlotinib as monotherapy. A second extension of the indication for erlotinib concerns the treatment of pancreatic carcinoma, but adding erlotinib to gemcitabine on average adds only one month to the total survival of these patients, and has more adverse effects. 


  • Compared to chemotherapy, erlotinib extends the progression-free survival of patients with non-small-cell lung carcinoma who have an EGFR-activating mutation (which occurs in 10% of the Dutch population), but not the total survival. 
  • For patients with non-small-cell lung carcinoma stage IIIb of IV who have an EGFR-activating mutation, combining osimertinib or possibly ramucirumab with erlotinib is to be preferred over erlotinib as monotherapy. 
  • In the treatment of pancreatic cancer, adding erlotinib to gemcitabine offers no added value, and hence has no place in the therapy.
  • Adverse effects of erlotinib are generally not serious, the most common being skin rashes. The latter may also predict a response.

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Authors

  • Juul M Cox
  • Lisanne L. Krens, dr, pharmacist