Afatinib

Afatinib (molecular formula: C24H25ClFN5O3), an oral 4-aniline quinazoline derivative (the compound is present in drugs as afatinib dimaleate), is an antitumor agent in the tyrosine kinase inhibitor group used for the treatment of advanced or metastatic non-small cell lung cancer with activating EGFR mutations (Sequist E V et al 2013; Yang J CH et al 2013).

The effects are based on covalent binding to the kinase domains of EGFR (Epidermal Growth Factor Receptor), HER2 and HER4. Afatinib thus causes an inhibition of the ErbB signalling pathway. Afatinib is taken once daily on an empty stomach in a dosage of 40mg/day p.o. The drug has a long half-life of up to 37 hours.

EGFR tyrosine kinase inhibitor (TKI)-naive adult patients with locally advanced and/or metastatic non-small cell lung cancer (NSCLC) with activating EGFR mutations

Locally advanced or metastatic NSCLC with squamous epithelial histology progressing under or after platinum-based chemotherapy

The most common possible adverse effects include diarrhea, exanthema, epistaxis, stomatitis, inflammation of the oral mucosa, purulent paronychia, dry skin, lack of appetite and itching.

Afatinib is a substrate and inhibitor of P-glycoprotein. Corresponding drug interactions are possible with P-gp inhibitors and inducers.

S.a. Technical information

Giotrif® (afatinib was approved in the USA and EU in 2013).

1. Chen X. et al (2013) Clinical perspective of afatinib in non-small cell lung cancer. Lung cancer 81: 155-61
2. Giotrif 50mg Professional info (2020)
3. Hirsh V. Afatinib (2011) Development in non-small-cell lung cancer. Future Oncol 7:817-825
4. Nelson V et al (2013) Emerging next-generation tyrosine kinase inhibitor for NSCLC. Onco Targets Ther 6: 135-143
5. Sequist E V et al (2013) Phase III Study of Afatinib or Cisplatin Plus Pemetrexed in Patients With Metastatic Lung Adenocarcinoma With EGFR Mutations. Journal of Clinical Oncology 31:3327-3334
6. Yang J CH et al (2013): Symptom Control and Quality of Life in LUX-Lung 3: A Phase III Study of Afatinib or Cisplatin/Pemetrexed in Patients With Advanced Lung Adenocarcinoma With EGFR Mutations. Journal of Clinical Oncology 31:3342-3350