Information about Afatinib
Afatinib is a tyrosine kinase receptor inhibitor that is used in the therapy of selected forms of metastatic non-small cell lung cancer.
Liver safety of Afatinib
Afatinib is associated with transient elevations in serum aminotransferase levels during therapy and has been reported to cause clinically apparent acute liver injury and rare instances of death.
Mechanism of action of Afatinib
Afatinib (a fa' ti nib) is a small molecule tyrosine kinase receptor inhibitor with potent activity against epidermal growth factor receptor 2 (EGFR2 or ErbB1) and human epidermal growth factor receptor 2 (HER2 or ErbB2). These tyrosine kinase receptors are often mutated and over expressed in tumor tissue and cause unregulated cell growth and proliferation. Inhibition of the unregulated receptor can lead to reversal of progression of the cancer, although clinical responses are sometimes limited by the development of tumor resistance caused by further mutations in the receptor gene. In several large controlled trials, afatinib was shown to improve progression-free survival in patients with non-small cell lung cancer (NSCLC) with mutated EGFR2. Afatinib has also shown promise in therapy of some cases of advanced breast cancer.
FDA approval information for Afatinib
Afatinib received approval for use in the United States in 2013. Current indications are as primary therapy for metastatic NSCLC with EGFR2 mutations and as second line therapy in patients with previously treated and refractory squamous cell lung cancer.
Dosage and administration for Afatinib
Afatinib is available in tablets of 20, 30 and 40 mg under the brand name Gilotrif. The recommended initial dose is 40 mg once daily, continued until disease progresses or intolerable toxicity occurs.
Side effects of Afatinib
Side effects are common and include diarrhea, rash, stomatitis, anorexia, nausea, dry skin, paronychia and pruritus. Uncommon, but potentially severe side effects include severe diarrhea leading to dehydration and renal failure, bullous and exfoliative skin rashes, Stevens Johnson syndrome, interstitial lung disease and embryo-fetal toxicity.