Which generation of targeted drug is Afatinib? What's the difference?

Afatinib is a second-generation tyrosine kinase inhibitor (TKI) mainly used to treat patients with non-small cell lung cancer (NSCLC) with EGFR mutations. Unlike first-generation targeted drugs (such as erlotinib and gefitinib), afatinib can not only inhibit the mutant form of EGFR, but also effectively inhibit HER2, HER4 and other receptors, so its anti-tumor activity is broader. Afatinib exerts anti-cancer effects by irreversibly binding to targets such as EGFR, HER2 and HER4, inhibiting the proliferation and growth of tumor cells.

Compared with first-generation targeted drugs, afatinib has a more powerful mechanism of action. First-generation drugs usually work by reversibly inhibiting the kinase activity of EGFR, while afatinib binds to the receptor in an irreversible manner, thereby providing a longer inhibitory effect. This characteristic makes afatinib more advantageous than first-generation drugs in the face of resistance mutations such as EGFR T790M mutation.

As a second-generation targeted drug, afatinib has higher anti-tumor activity and wider adaptability. For example, afatinib can better inhibit tumor growth in patients with EGFR-sensitive mutations or some patients with drug-resistant mutations. Although the second-generation drugs have improved effects, they are also accompanied by some adverse reactions, such as rash, diarrhea, and oral ulcers. Therefore, patients need to strictly monitor side effects under the guidance of a doctor when using afatinib.
In general, afatinib is a second-generation targeted drug that provides strong anti-tumor effects by irreversibly inhibiting EGFR and other targets. Compared with first-generation drugs, afatinib shows higher efficacy in the treatment of EGFR mutation-positive non-small cell lung cancer, but it is also accompanied by more obvious side effects. During the treatment process, patients should use it under the supervision of a doctor to ensure efficacy and safety.
Reference: https://www.giotrif.com/