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Osimertinib mesylate, which is the methanesulfonate kind of osimertinib, is a third-generation, oral, irreparable epidermal development variable receptor created by AstraZeneca.

Its core worth hinges on fixing two major problems in lung cancer cells targeted therapy: it is effective against the T790M resistance anomaly, while having a fairly small impact on the wild-type EGFR.

Accurate targeting of drug-resistant anomalies: After the initial and second-generation EGFR TKI treatments, about fifty percent of the patients created resistance as a result of the emergence of the T790M anomaly. Osimertinib mesylate can effectively prevent the T790M anomaly, and at the same time has high activity versus sensitive mutations such as L858R and exon 19 removal, thus getting rid of the issue of drug resistance.

Minimize negative effects: It selectively inhibits the mutant EGFR, and its repressive effect on the wild-type EGFR is much weaker than that on the mutant kind. Its two major metabolites, AZ5104 and AZ7550, also have medicinal task. Among them, AZ5104 has more powerful activity against exon 19 removal and T790M anomaly.

In professional applications, Osimertinib mesylate is the core medication for dealing with non-small cell lung cancer with EGFR anomalies. It has actually been authorized for multiple indications. According to the latest info in January 2025, it has simply been accepted in China for the treatment of stage III non-small cell lung cancer cells with EGFR anomalies that is not operable. It is the first and just targeted medicine in China to be authorized for this sign.