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Release date: 2024-11-18 17:07:54 Recommended: 90
The chemical name of afatinib is N-{4-(3-chloro-4-fluorophenylamino)-7-(tetrahydrofuran-3-yloxy)quinazolin-6-yl}-2-(dimethylamino)acetamide, the molecular formula is C24H25ClFN5O3, and the molecular weight is 485.94. Afatinib is a second-generation irreversible tyrosine kinase inhibitor (TKI) whose molecular structure allows it to irreversibly bind to EGFR and other HER family receptors.
Afatinib inhibits tumor cell proliferation by inhibiting the activity of EGFR and other HER family receptors (e.g., HER2, HER4) and blocking these receptor-mediated signaling pathways. It is particularly suitable for patients with non-small cell lung cancer with EGFR mutations such as Exon 19 deletion or Exon 21 L858R mutation. These mutations make cancer cells abnormally active, but afatinib can effectively block this abnormal signaling.
Afatinib is usually given in tablet form, and the recommended starting dose is 40 mg once daily on an empty stomach (at least 1 hour before or 2 hours after a meal). Depending on the patient's tolerance, the doctor may adjust the dose to 30 mg or 50 mg. Regular check-ups should be done during treatment to monitor the patient's response and possible side effects.
Afatinib was developed by German biopharmaceutical company Boehringer Ingelheim and was first approved by the FDA in 2013 for the treatment of patients with metastatic non-small cell lung cancer harboring EGFR mutations. Afatinib is an irreversible inhibitor compared to first-generation EGFR-TKIs such as gefitinib and erlotinib, allowing it to show stronger efficacy in certain patient populations.
Afatinib blocks the activation of these receptors by irreversibly binding to the tyrosine kinase regions of EGFR, HER2, and HER4. EGFR mutations cause sustained tyrosine kinase activity, allowing cells to continue to divide and lead to tumor growth. Afatinib inhibits these receptors, especially against common EGFR mutations, thereby stopping the growth and spread of cancer cells. In addition, afatinib also has inhibitory effects on HER2 and HER4, which gives it a potential therapeutic effect in certain complex tumor types as well.
Afatinib is a second-generation EGFR-TKI-targeted drug primarily used for the treatment of patients with non-small cell lung cancer (NSCLC) harboring EGFR mutations. It inhibits the proliferation and spread of tumor cells by irreversibly inhibiting the signaling pathways of EGFR and other HER family receptors. Compared with the first-generation EGFR-TKI, afatinib has a more durable effect and is suitable for patients with drug-resistant mutations.
