Dacomitinib/Dacomitinib belongs to the first generation of EGFR targeting drugs

Dacomitinib/Dacomitinib (Dacomitinib) is a second-generation EGFR-targeted drug. It is an irreversible epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI). Compared with first-generation EGFR-TKIs (such as gefitinib and erlotinib) which only reversibly inhibit the EGFR receptor, dacomitinib has a stronger binding ability and can irreversibly inhibit EGFR and its family members HER2 and HER4, thus blocking the signaling pathways of cancer cells more broadly.

As a second-generation TKI drug, dacomitinib is designed to improve tumor suppression efficacy, delay the emergence of drug resistance, and achieve more durable treatment responses in some patients. Its main indication is as first-line treatment for patients with metastatic non-small cell lung cancer (NSCLC) who are confirmed to have EGFR sensitive mutations (such as exon 19 deletion or L858R mutation).

In the international multi-centerARCHER 1050 study, dacomitinib was confirmed to have significantly longer progression-free survival (PFS) and overall survival (OS) than the first-generation EGFR-TKI gefitinib. However, the enhanced inhibitory effect of second-generation EGFR-TKI is also accompanied by an increased risk of toxicity, such as a higher incidence of side effects such as rash, diarrhea, stomatitis, etc. Therefore, close monitoring and individualized dose adjustment are required in clinical use. Nonetheless, dacomitinib offers a more potent and longer-lasting treatment option for a subset of patients who do not respond satisfactorily to first-generation drugs.

It is currently listed as a first-line recommended drug for EGFR mutation-positive lung cancer by international guidelines It is especially suitable for people with a low risk of brain metastasis and good tolerance. In the context of the rapid development of precision medicine, dacomitinib, as an important representative of the second-generation EGFR-TKI, is increasingly changing the survival pattern of patients with non-small cell lung cancer.

Reference materials:https://www.pfizer.com/products/product-detail/vizimpro