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.