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Limertinib: First Approval
1Springer Nature, Private Bag 65901, Mairangi Bay, Auckland 0754, New Zealand. dru@adis.com.
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.
Insights
Limertinib, a third-generation EGFR TKI, shows efficacy in non-small cell lung cancer (NSCLC) patients with T790M mutations. It received approval in China for both second-line and first-line treatment of NSCLC.
Area of Science:
- Oncology
- Pharmacology
Background:
- Limertinib is an orally available, third-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI).
- It is developed for the treatment of non-small cell lung cancer (NSCLC).
Purpose of the Study:
- To summarize the development milestones of limertinib.
- To highlight its first approval for NSCLC treatment.
Main Methods:
- Clinical trials were conducted to evaluate limertinib's efficacy.
- Regulatory submissions were made based on trial data.
Main Results:
- Limertinib demonstrated efficacy in patients positive for the T790M gatekeeper mutation.
- The drug received approval in China for advanced or metastatic NSCLC with disease progression after prior EGFR TKI treatment and T790M mutation.
- Further approval was granted in China for first-line treatment of NSCLC with EGFR exon 19 deletions or exon 21 L858R mutations.
Conclusions:
- Limertinib represents a significant advancement in NSCLC treatment.
- The drug offers new therapeutic options for patients with specific EGFR mutations.
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