Products
Afatinib was approved in the US and EU in 2013 and in many countries in 2014 in film-coated tablet form (Giotrif).
Structure and properties
Afatinib (C24H25ClFN5O3, Mr = 485.9 g/mol) is a 4-aniline quinazoline derivative that is present in drugs as afatinib dimaleate, a white to brownish-yellow powder that is soluble in water. It is structurally related to other EGFR TKIs.
Effects
Afatinib (ATC L01XE13) has antitumor and antiproliferative properties. The effects are due to covalent binding to the kinase domains of EGFR (epidermal growth factor receptor), HER2, and HER4. This leads to inhibition of the ErbB pathway. Afatinib has a long half-life of up to 37 hours.
Indications
For the treatment of metastatic, end-stage non-small cell lung cancer (NSCLC).
Dosage
According to the SmPC. Tablets are taken once daily on a fasting basis.
Contraindications
- Hypersensitivity
- Pregnancy
- Lactation contraindicated
Full precautions can be found in the drug label.
Interactions
Afatinib is a substrate and inhibitor of P-glycoprotein. Appropriate drug-drug interactions are possible with P-gp inhibitors and inducers.
Adverse effects
The most common potential adverse effects include diarrhea, rash, oral mucositis, circulation, dry skin, poor appetite, and pruritus.
