Afatinib
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| Trade names | Gilotrif, Giotrif |
| AHFS/Drugs.com | Multum Consumer Information |
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Oral |
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| Pharmacokinetic data | |
| Protein binding | 95% |
| Metabolism | not involved |
| Biological half-life | 37 hours |
| Excretion | Faeces (85%), urine (4%) |
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| Synonyms | BIBW 2992 |
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| ECHA InfoCard | 100.239.035 |
| Chemical and physical data | |
| Formula | C24H25ClFN5O3 |
| Molar mass | 485.937 g/mol |
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Afatinib (INN; trade name Gilotrif in the US and Giotrif in Europe, previously Tomtovok and Tovok) is a drug approved in United States, Europe, Taiwan, Mexico, Chile and Japan as well as other countries for the first-line treatment of patients with distinct types of metastatic (EGFR mutation positive) non-small cell lung carcinoma (NSCLC), developed by Boehringer Ingelheim. It acts as an irreversible covalent inhibitor of the receptor tyrosine kinases epidermal growth factor receptor (EGFR) and erbB-2 (HER2).
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.
Adverse effects by frequency include:
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 mutations such as T790M which are 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.
In March 2010 a Phase III trial in NSCLC patients called Lux-Lung 5 began with this drug. Fall 2010 interim results suggested the drug extended progression-free survival threefold compared to placebo, but did not extend overall survival. In May 2012, the Phase IIb/III trial Lux-Lung 1 came to the same conclusion.
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