Aumolertinib — Investigational Agent
EGFR Inhibitor · Approved Abroad / Investigational in US · Hansoh Pharma / EQRx
Mechanism of Action
Aumolertinib is a third-generation, irreversible EGFR tyrosine kinase inhibitor that selectively targets both EGFR sensitizing mutations (e.g., Exon 19 del, L858R) and the T790M resistance mutation. It works by covalently binding to the Cys797 residue of the EGFR kinase domain, sparing wild-type EGFR. The molecule includes a cyclopropyl group that enhances its metabolic stability and CNS penetration. By inhibiting mutant EGFR, it suppresses the MAPK/ERK and PI3K/Akt pathways, leading to tumor regression in EGFR-driven NSCLC.
Investigational Indications
- EGFR-mutant non-small cell lung cancer (1st line)
- EGFR T790M-positive non-small cell lung cancer