|Appearance||White crystalline powder|
|Storage and Handling||Store it at room temperature and away from excess heat and moisture.|
Afatinib, sold under the brand name Gilotrif among others, is a medication used to treat non-small cell lung carcinoma (NSCLC).It belongs to the tyrosine kinase inhibitor family of medications.It is taken by mouth.
Afatinib is mainly used to treat cases of NSCLC that harbour mutations in the epidermal growth factor receptor (EGFR) gene.
Afatinib 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.
Afatinib 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.
Afatinib Side Effects & Warning
Very common (>10% frequency)
▪ Diarrhea (>90%)
▪ Rash/dermatitis acneform
▪ Decreased appetite
▪ Nose bleed
▪ Dry skin
Common (1–10% frequency)
▪ Dehydration,Taste changes,Dry eye
▪ Runny/stuffy nose
▪ Low amount of potassium in the blood
▪ Increased ALT
▪ Increased AST
▪ Hand-foot syndrome
▪ Muscle spasms
▪ Kidney impairment and/or failure
Uncommon (0.1-1% frequency)
▪ Interstitial lung disease