Giotrif(afatinib)

Giotrif (afatinib) is indicated as monotherapy for the treatment of Epidermal Growth Factor Receptor (EGFR) TKI-naïve adult patients with locally advanced or metastatic non-small cell lung cancer (NSCLC) with activating EGFR mutation(s). Afatinib demonstrates an IC50 on EGFR of 0.5 nM, on HER2 of 14 nM, and on ErbB4 of 1 nM. For comparison, gefitinib has an IC50 on EGFR of 1 nM and on ErbB4 of 323 nM, while canertinib has an IC50 on EGFR of 0.3 nM, on HER2 of 30 nM, and on ErbB4 of 1 nM. Afatinib shows an IC50 on BIRK of > 100000 nM and on c-src of > 4000 nM.

Safety findings indicate that possibly clinically significant potassium abnormality occurred in 8.4% of patients treated with afatinib compared to 1.9% with chemotherapy. Possibly clinically significant AST abnormality was observed in 8.4% with afatinib versus 0.9% with chemotherapy, and ALT abnormality in 10.2% with afatinib versus 4.6% with chemotherapy. For afatinib 50 mg, possibly clinically significant haemoglobin abnormality was 14.5% and potassium abnormality was 6.2%.

The Marketing Authorisation application for Giotrif was submitted on 28 August 2012, with the CHMP positive opinion issued on 25 July 2013. The Marketing Authorisation date was 12 July 2013, and the initial EU approval date was 25 September 2013. The approved indication is for monotherapy in EGFR TKI-naïve adult patients with locally advanced or metastatic NSCLC with activating EGFR mutation(s).