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Product Overview
Erlotinib (Tarceva©), a highly potent, selective and orally available human epidermal growth factor receptor (HER1/EGFR) tyrosine-kinase (TK) inhibitor, is a valuable new treatment option with a proven survival benefit in advanced non-small-cell lung cancer (NSCLC).1 In addition to NSCLC, erlotinib is advanced in clinical trials for a range of other indications. The latest news, data and research are available online at HER1Update.com.
Mechanism of action
HER1/EGFR has a pivotal role in the growth and progression of many types of human cancer. Erlotinib inhibits the binding of adenosine triphosphate to the intracellular TK domain of HER1/EGFR, blocking receptor phosphorylation and associated downstream signalling.2 As a result, cellular processes associated with tumour growth and progression, such as proliferation, angiogenesis, metastasis and protection from apoptosis, are inhibited.2
Preclinical data
Erlotinib is highly specific for HER1/EGFR TK.2
Erlotinib has activity against human colorectal,3 head and neck,4
NSCLC,5 glioma6 and pancreatic7 tumour cell lines or xenografts, resulting in stasis or regression.
Combining erlotinib with several commonly used chemotherapeutic agents in a human tumour xenograft model has an additive effect on antitumour activity with no increase in toxicity.3–5 These data suggest that this approach may improve clinical efficacy.
Erlotinib inhibits the constitutively active mutant receptor – EGFRvIII.8 |