Erlotinib 

Historical story:

Erlotinib, like gefitinib, is an EGFR tyrosine kinase inhibitor used in molecular targeted therapy, introduced in clinical trials in the early 2000s and FDA-approved in NSCLC in 2004. Erlotinib was evaluated in a well-designed clinical trial, which enrolled 700-plus patients who had progressed after one or two courses of chemotherapy. Treatment was with erlotinib or placebo. Improved survival as well as improvement in cough, shortness of breath, and pain were demonstrated in erlotinib patients.

 mechanism of action 

• 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.

  Uses

Erlotinib is used for the treatment of metastatic (cancer that has already spread) non-small cell lung cancer in patients who have certain types of abnormal epidermal growth factor (EGFR) gene mutations. Your doctor will perform a test before you take this medicine

  Side Effects

 • Burning, tingling, numbness or pain in the hands, arms, feet, or legs 

• cough or hoarseness 

• diarrhea (severe) 

• difficult or labored breathing 

• fever or chills 

• lower back or side pain 

• painful or difficult urination 

• rash (severe) 

• sensation of pins and needles 

• stabbing chest pain 

• tightness in the chest