Afatinib* is an irreversible ErbB Family Blocker that is an oral, once daily investigational targeted therapy.1
The ErbB Family of receptors consists of four related members: EGFR (ErbB1), HER2 (ErbB2), ErbB3, and ErbB4.2 These receptors are often overexpressed or mutated in many cancers, including lung, breast, head and neck, and colorectal cancers. An active ErbB-receptor is formed by the union of two molecules, a process called dimerisation. Dimers can be formed between identical receptors e.g. EGFR and EGFR (homodimers) or different receptors e.g. EGFR and HER2 (heterodimers). The ErbB Family of receptors are involved in fundamental cellular processes including cell proliferation, migration, metabolism and survival3, which allow the tumour cells to grow and proliferate.
Inhibiting the ErbB receptor signalling may play a critical role in the prevention of tumour growth and spread. Afatinib* irreversibly binds to the intracellular tyrosine kinase domain of ErbB Family receptors and inhibits the downstream signalling cascade, which in turn may inhibit cell growth and induce apoptosis (programmed cell death) in cancer cells.
*Afatinib is an investigational compound and is not yet approved. Its safety and efficacy has not yet been fully established.
- BI Data on File.
- Hynes NE, Lane HA. ERBB receptors and cancer: the complexity of targeted inhibitors. Nat Rev Cancer 2005;5:341-54.
- Hynes NE, MacDonald G. ErbB receptors and signalling pathways in cancer. Curr Opin Cell Biol 2009;21:177-84.