Furmonertinib — Investigational Agent

EGFR Inhibitor · Approved Abroad / Investigational in US · ArriVent BioPharma / Allist Pharmaceuticals

Mechanism of Action

Furmonertinib is an oral, third-generation, irreversible EGFR tyrosine kinase inhibitor. It covalently targets a broad range of activating EGFR mutations — classical exon 19 deletions and L858R, the T790M resistance mutation, and, notably, EGFR (and HER2) exon 20 insertion mutations — while relatively sparing wild-type EGFR. Both the parent drug and its active metabolite (AST5902) are pharmacologically active, and the compound achieves good central nervous system penetration.

Investigational Indications

• EGFR exon 20 insertion-mutant NSCLC (first-line; investigational in US)
• EGFR-mutant (exon 19 del / L858R / T790M) advanced NSCLC
• NSCLC with CNS/leptomeningeal involvement (CNS-penetrant activity)

Key Trials