Drug Overview
Tarceva (erlotinib; Roche/Chugai/Astellas) is an orally available epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor. EGFR is part of the ErbB pathway, which is hyperactivated or dysregulated in many cancers, thereby leading to uncontrolled cell growth. In particular, EGFR-activating mutations such as exon 19 deletion (del19) or exon 21 point mutation L858R have previously been identified as contributing to the promotion of tumor cell growth and blocking apoptosis in non-small cell lung cancer. Tarceva reversibly inhibits the kinase activity of EGFR, and has higher binding affinity for EGFR del19 or exon 21 point mutation L858R mutations compared with wild-type receptors. This prevents the initiation of signaling cascades and results in the inhibition of EGFR-dependent proliferation.
Tarceva (erlotinib; Roche/Chugai/Astellas) is an orally available epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor. EGFR is part of the ErbB pathway, which is hyperactivated or dysregulated in many cancers, thereby leading to uncontrolled cell growth. In particular, EGFR-activating mutations such as exon 19 deletion (del19) or exon 21 point mutation L858R have previously been identified as contributing to the promotion of tumor cell growth and blocking apoptosis in non-small cell lung cancer. Tarceva reversibly inhibits the kinase activity of EGFR, and has higher binding affinity for EGFR del19 or exon 21 point mutation L858R mutations compared with wild-type receptors. This prevents the initiation of signaling cascades and results in the inhibition of EGFR-dependent proliferation.
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