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| Product name | Afatinib |
| Cas number | 850140-72-6 |
| Appearance | White powder |
| MF | C24H25ClFN5O3 |
| MW | 485.9 |
Afatinib is an irreversible ErbB family of blockers that suppress information transmission and block the major pathways involved in cancer cell growth and division. Because ErbB family information transduction mechanism can be triggered by multiple homodimers and heterodimers, simultaneous inhibition of multiple ErbB family members (such as EGFR, HER2, ErbB3 and ErbB4) can effectively interrupt the downstream information transduction.
Afatinib is a drug approved for the treatment non-small cell lung carcinoma (NSCLC). It acts as a angiokinase inhibitor.
Like lapatinib and neratinib, afatinib is a tyrosine kinase inhibitor (TKI) that also irreversibly inhibits human epidermal growth factor receptor 2 (Her2) and EGFR kinases. Afatinib is not only active against EGFR mutations targeted by first generation TKIs, but also against those not sensitive to these standard therapies. Because of its additional activity against Her2, it is being investigated for breast cancer as well as other EGFR and Her2 driven cancers.
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