Dacomitinib (dacomitinib) tablets belong to which generation of targeted drugs and introduction to their characteristics

Dacomitinib (also known as dacomitinib) is a second-generation EGFRtyrosine kinase inhibitor (EGFR-TKI), mainly used to treat patients with non-small cell lung cancer (NSCLC) with epidermal growth factor receptor (EGFR) gene mutations. Compared with the first-generation targeted drugs such as gefitinib and erlotinib, dacomitinib is structurally optimized and can irreversibly bind and inhibit multiple members of the EGFR family (including EGFR FR/HER1, HER2 and HER4), thus having a broader spectrum and longer-lasting inhibitory effect.

One of the greatest features of dacomitinib is its irreversible binding mechanism. This combination not only prolongs the action time of the drug and the receptor, but also enhances its killing power against EGFR mutant tumors. At the same time, dacomitinib's inhibition of HER2 and other related receptors may enhance the anti-tumor effect and reduce the risk of partial resistance in certain mutation backgrounds. This is also its key advantage that distinguishes it from the first-generation EGFR-TKI.

In clinical trials, dacomitinib showed superior efficacy to gefitinib. ARCHER 1050 Phase III study results show that dacomitinib can significantly prolong progression-free survival (PFS) and overall survival (OS), especially in EGFR sensitive mutations ( For example, patients with 19 exon deletion and 21L858R mutation)-positive NSCLC patients have better efficacy. However, it should also be noted that its side effects are more significant, such as rash, diarrhea, stomatitis, etc., which require strengthened management during the treatment process.

In general, dacomitinib, as a second-generation EGFR-TKI, has the characteristics of irreversible binding, broad-spectrum targets and high efficacy. In EGFRProvides new treatment options for patients with mutation-positive advanced lung cancer. Although side effects require attention, for certain patients, dacomitinib is still a targeted drug worth trying, especially for patients who want to prolong progression-free survival and have good physical tolerance.

Reference materials:https://www.drugs.com