Erlotinib (Tarceva®)

Erlotinib is an epidermal growth factor receptor (EGFR) used in the treatment of advanced pancreatic cancer and some types of lung cancer.  It interacts with the intracellular ATP-binding site of the tyrosine kinase of EGFR, inhibiting downstream RAS, PI3K and STAT signaling pathways.  Erlotinib produces cell cycle blockade, slowed angiogenesis and decreased tumor burden in responsive malignancies.

Erlotinib is specifically indicated for unresectable or metastatic pancreatic cancer and non-small cell lung cancer (NSCLC) with exon 19 deletion or an L to R mutation at site 858.  Its efficacy in lung cancer with other EGFR mutations has not yet been established.

Erlotinib therapy may cause significant toxicity, with around 1% of patients developing interstitial lung disease.  Some patients have also experienced hepatotoxicity, GI perforation, severe skin disorders, and ocular dysfunction.  The most common side effects are nausea, diarrhea, rash, and fatigue.




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