A review of erlotinib and its clinical use.
Erlotinib is an orally available, reversible tyrosine kinase inhibitor of the epidermal growth factor receptor. Encouraging activity as a single agent and in combination with other targeted agents has been demonstrated in Phase II trials in many tumour types. Erlotinib has an established role in the treatment of advanced, refractory non-small cell lung cancer-based on a pivotal trial demonstrating a survival advantage over best supportive care. In a Phase III trial, the addition of erlotinib to gemcitabine improved survival in advanced pancreatic cancer. The toxicity profile of erlotinib includes diarrhoea and rash, with no haematological side effects. Predictive factors for response include the presence of a rash, epidermal growth factor receptor expression and mutation status. This article reviews the current clinical status of erlotinib.
Tang
Patricia A
PA
Department of Medical Oncology and Hematology, Princess Margaret Hospital, University of Toronto, Toronto, M5G 2M9, Canada.
Tsao
Ming-Sound
MS
Moore
Malcolm J
MJ
D017322:Clinical Trials, Phase II as Topic; D017326:Clinical Trials, Phase III as Topic; D066246:ErbB Receptors / Q000037:antagonists & inhibitors / Q000378:metabolism; D000069347:Erlotinib Hydrochloride; D006801:Humans; D047428:Protein Kinase Inhibitors / Q000494:pharmacology / Q000627:therapeutic use*; D011799:Quinazolines / Q000009:adverse effects / Q000627:therapeutic use*
D047428:Protein Kinase Inhibitors; D011799:Quinazolines; D000069347:Erlotinib Hydrochloride; D066246:ErbB Receptors