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Boehringer Ingelheim
Afatinib* is an oral, once daily investigational compound. It is an irreversible blocker of the erbB-receptor family.1 The ErbB-receptor family consists of four related members: ErbB1 also known as epidermal growth factor receptor (EGFR, HER1) and ErbB2, ErbB3 and ErbB4 (HER2-4; human epidermal growth factor receptor kinases 2-4).2
An active ErbB-receptor is formed by the union of two molecules, a process called dimerisation, which is an important regulatory mechanism of single receptors. Dimers can be formed between similar receptors e.g. ErbB1+ErbB1 (homodimers) or different receptors e.g. ErbB1+ErbB2 (heterodimers).
ErbB-receptor signalling is involved in fundamental cellular processes including cell proliferation, migration, metabolism and survival3 and their inhibition may play a critical role in the prevention of tumour growth and spread. Afatinib* irreversibly binds to the receptor tyrosine kinases and inhibits the downstream signalling cascade, which in turn may inhibit cell growth and induce apoptosis (programmed cell death) in cancer cells.
Afatinib* is currently being investigated for various tumour types, including non-small cell lung cancer (NSCLC), breast cancer, head and neck cancer, glioblastoma and colorectal cancer.2,4 Afatinib* is currently in Phase III clinical development in NSCLC and breast cancer.
Source for healthcare professionals: www.inoncology.com
* Nintedanib (BIBF 1120), afatinib (BIBW 2992) and volasertib (BI 6727) are investigational compounds. Their safety and efficacy have not yet been fully established.
