Limertinib: First Approval

Declarations

Funding The preparation of this review was not supported by any external funding.

Authorship and Conflict of interest During the peer review process the manufacturer of the agent under review was offered an opportunity to comment on the article. Changes resulting from any comments received were made by the authors on the basis of scientific completeness and accuracy. Arnold Lee is a contracted employee of Adis International Ltd/Springer Nature, and declares no relevant conflicts of interest. All authors contributed to this article and are responsible for its content.

Ethics approval, Consent to participate, Consent to publish, Availability of data and material, Code availability not applicable

Additional information about this Adis Drug Review can be found here.

Abstract

Limertinib (Aoyixin) is an orally available, third-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI), which has been developed for the treatment of non-small cell lung cancer (NSCLC). In clinical trials, limertinib demonstrated efficacy in patients who are positive for the T790M gatekeeper mutation. Limertinib received its first approval for the treatment of adults with locally advanced or metastatic NSCLC with disease progression following treatment with an EGFR TKI and are positive for the EGFR T790M mutation in China in January 2025. In April 2025, limertinib was also approved in China for first-line treatment for adult patients with locally advanced or metastatic NSCLC harbouring EGFR exon 19 deletions or exon 21 L858R mutations. This article summarizes the milestones in the development of limertinib leading to this first approval.

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