Which generation of targeted drugs does dacomitinib (dacomitinib) belong to?

Dacomitinib (Dacomitinib) is a second-generation EGFR (epidermal growth factor receptor) tyrosine kinase inhibitor (TKI). EGFRis an important therapeutic target, especially in non-small cell lung cancer (NSCLC). EGFRgene mutations are a common mutation type in NSCLC patients, accounting for about 15%-20% of lung adenocarcinoma patients. Therefore, targeted therapy for EGFR mutations is of great clinical significance.

First-generationEGFR-TKI, such as gefitinib (Gefitinib) and erlotinib (Erlotinib), have achieved efficacy in inhibiting EGFR activity and prolonged the survival of many patients. However, patients often develop drug resistance after using it for a period of time, and the most common resistance mechanism is the EGFR T790M mutation. To solve this problem, scientists have developed second- and third-generation EGFR-TKIs.

Dacomitinib , as a second-generation EGFR-TKI, has stronger inhibitory activity than first-generation drugs. It irreversibly binds to EGFR tyrosine kinase and can effectively inhibit various EGFR mutations, including common L858R and Exon 19 deletion mutations. Dacomitinib (Dacomitinib) has shown better efficacy than first-generation EGFR-TKI in clinical trials, especially in delaying disease progression and improving patient survival.

In 2018,dacomitinib (dacomitinib) was approved by the U.S. Food and Drug Administration (FDA) for the treatment of patients with EGFRPatients with metastatic non-small cell lung cancer. The approval was based on results from the ARCHER 1050 clinical trial, which showed that dacomitinib (dacomitinib) prolonged progression-free survival (PFS) and overall survival (OS) compared with gefitinib. However, dacomitinib is also associated with a higher incidence of adverse reactions, such as rash, diarrhea, and stomatitis, which require careful monitoring and management by clinicians during use.

Althoughdacomitinib has shown promising results in the treatment ofEGFRmutatedNSCLC With the emergence of third-generation EGFR-TKIs such as Osimertinib (Osimertinib), treatment strategies are also constantly evolving. The third generation EGFR-TKI can effectively target the T790M resistance mutation and has improved safety and tolerability. Therefore, in actual clinical applications, doctors will choose the most appropriate EGFR-TKI based on the patient's specific mutation type and drug resistance.