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Limerinib (also known as HS-10370) is an orally bioavailable, third-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) developed by Hansoh Pharmaceutical. It is designed to irreversibly and selectively inhibit EGFR sensitizing mutations (such as Exon 19 deletions and L858R) as well as the T790M resistance mutation, while exhibiting significantly less activity against wild-type EGFR to minimize skin and gastrointestinal toxicities. A key pharmacological feature of limerinib is its high blood-brain barrier permeability, which allows for therapeutic concentrations in the central nervous system. This makes it particularly suitable for treating patients with EGFR-mutant non-small cell lung cancer (NSCLC) who have developed brain metastases or meningeal metastasis. It is currently undergoing clinical evaluation in China for advanced solid tumors and CNS-involved NSCLC.
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