|Trade names||Gilotrif, Giotrif, Afanix|
|Other names||BIBW 2992|
|Drug class||Tyrosine kinase inhibitor|
|Main uses||Non-small cell lung carcinoma (NSCLC)|
|Side effects||Diarrhea, rash, mouth inflammation, dry skin, nausea, itchiness|
|Typical dose||40 mg OD|
|Metabolism||CYP not involved|
|Elimination half-life||37 hours|
|Excretion||Faeces (85%), urine (4%)|
|Chemical and physical data|
|Molar mass||485.94 g·mol−1|
|3D model (JSmol)|
|(what is this?)|
Afatinib, sold under the brand name Gilotrif among others, is a medication used to treat non-small cell lung carcinoma (NSCLC). It is mainly used in advanced cases with a non-resistant epidermal growth factor receptor (EGFR) mutation. It is taken by mouth.
Common side effects include diarrhea, rash, mouth inflammation, dry skin, nausea, and itchiness. Other side effects may include interstitial lung disease, liver problems, gastrointestinal perforation, and corneal inflammation. Use in pregnancy may harm the baby. It is a tyrosine kinase inhibitor which blocks a family of proteins known as ErbB.
Afatinib was approved for medical use in the United States and Europe in 2013. It is on the World Health Organization's List of Essential Medicines as an alternative to erlotinib. In the United Kingdom 4 weeks costs the NHS about £2,000 as of 2021. This amount in the United States costs about 9,800 USD.
It has received regulatory approval for use as a treatment for non-small cell lung cancer, although there is emerging evidence to support its use in other cancers such as breast cancer.
- Very common (>10% frequency)
- Common (1–10% frequency)
- Uncommon (0.1-1% frequency)
Mechanism of action
Like lapatinib and neratinib, afatinib is a protein kinase inhibitor that also irreversibly inhibits human epidermal growth factor receptor 2 (Her2) and epidermal growth factor receptor (EGFR) kinases. Afatinib is not only active against EGFR mutations targeted by first generation tyrosine-kinase inhibitors (TKIs) like erlotinib or gefitinib, but also against less common mutations which are resistant to these drugs. However, it is not active against the T790M mutation which generally requires third generation drugs like osimertinib. Because of its additional activity against Her2, it is being investigated for breast cancer as well as other EGFR and Her2 driven cancers.
Society and culture
In Bangladesh under the trade name Afanix.
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