Afatinib belongs to the first generation of targeted therapy drugs

Afatinib (Afatinib) is a second-generation EGFR (epidermal growth factor receptor) tyrosine kinase inhibitor (EGFR-TKI span>), mainly used to treat patients with non-small cell lung cancer (NSCLC) carrying EGFR gene mutations. Compared with the first-generation targeted drugs such as gefitinib (Gefitinib) and erlotinib (Erlotinib), afatinib has different effects on EGFR family receptors. The reversible inhibitory effect not only acts on EGFR mutants, but also inhibits HER2 and HER4 receptors at the same time, so it also shows certain efficacy in some drug-resistant patients.

Afatinib is widely used to treat patients with advanced non-small cell lung cancer who have sensitive EGFR mutations (such as 19 exon deletion or 21 L858R point mutation). Studies have shown that afatinib can prolong the progression-free survival (PFS) of patients and also shows certain central nervous system activity in patients with brain metastases. Due to its irreversible inhibitory effect on multiple EGFR family members, it has a more durable anti-cancer effect than the first-generation drugs in clinical practice.

Although afatinib, as a second-generation drug, has certain advantages in efficacy, its side effects are relatively obvious. Common adverse reactions include diarrhea, rash, stomatitis, and paronychia. These side effects are particularly common in the early stages of use, and some patients may need to reduce the dose or take medication intermittently to improve tolerance. Therefore, the patient's response should be closely monitored during use and the treatment plan should be adjusted in a timely manner.

In the field of targeted therapy, afatinib, as the second generationEGFR-TKI, fills some gaps after the emergence of resistance to first-generation drugs, but for the most common T790MResistance mutations are not sensitive and require the use of third-generation EGFR inhibitors such as Osimertinib (Osimertinib). Therefore, the current common clinical practice is: after the first or second generation drug treatment fails, if the T790M mutation is found, the patient can switch to the third generation drug. Afatinib still occupies an important position in the entire EGFR treatment sequence.

References：https://www.giotrif.com/