Which generation of targeted drugs is Osimertinib/Tagrisso? Revealing its role in lung cancer treatment

Osimertinib is a third-generation EGFR inhibitor specifically targeting patients with epidermal growth factor receptor (EGFR)-mutated non-small cell lung cancer (NSCLC). Osimertinib is designed as a "targeted drug" whose main function is to inhibit EGFR mutations, especially the T790M mutation. This mutation is common in patients who fail treatment with second-generation EGFR inhibitors (such as erlotinib and gefitinib). Therefore, the emergence of osimertinib brings new hope to EGFR mutation-positive patients.

Osimertinib, as a third-generation targeted drug, can selectively inhibit EGFR harboring theT790M mutation. It also has a strong inhibitory effect on wild-type EGFR and other types of EGFR mutations.

Unlike first-generation (eg, gefitinib, erlotinib) and second-generation (eg, afatinib) drugs, osimertinib significantly improves treatment efficacy by providing greater selectivity and better resistance management. Especially after the second-generation EGFR inhibitors are ineffective, osimertinib can effectively overcome the drug resistance caused by the T790M mutation. This feature makes it occupy an important position in clinical practice.

Osimertinib has now become one of the standard treatment options for patients with EGFR mutated non-small cell lung cancer. Especially for those patients with EGFR T790M mutation, osimertinib not only has significant efficacy but also effectively prolongs progression-free survival (PFS). In clinical trials, osimertinib monotherapy has a very high response rate for patients with EGFR-mutated non-small cell lung cancer, and its side effects are relatively controllable and well tolerated by patients.

In addition, osimertinib, as a "cross-generation" drug, is also widely used in first-line treatment. Studies have shown that osimertinib also has significant efficacy in untreated patients with EGFR mutation-positive non-small cell lung cancer and can significantly prolong the overall survival (OS) of patients. Therefore, osimertinib has become the first-choice treatment for patients with EGFR mutation-positive non-small cell lung cancer, especially in patients with advanced and metastatic lung cancer, and its efficacy and safety have been widely recognized.

Reference materials:https://go.drugbank.com/drugs/DB09330