Almonertinib

DB16640ApprovedInvestigationalSmall molecule

Almonertinib is a third-generation, irreversible epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) indicated for the treatment of patients with metastatic EGFR T790M mutation-positive non-small cell lung cancer (NSCLC). Unlike other third-generation EGFR TKIs, almonertinib is a pyrimidine-based drug that forms a covalent bond to the binding site of the EGFR tyrosine kinase domain.

Mechanism: Almonertinib is an irreversible, small molecule tyrosine kinase inhibitor (TKI) of EGFR with inhibitory activity against EGFR TKI sensitizing mutations (EGFR exon 19 [Ex19Del] deletion and EGFR L858R, respectively) and EGFR TKI resistance mutation (EGFR T790M). The major active metabolite of almonertinib, HAS-719, retains pharmacological activity but shows less potency than almonertinib. Almonertinib binds covalently and irreversibly to cysteine-797 at the adenosine triphosphate-binding site of the EGFR tyrosine kinase domain.
Curator reviewed · 6 references
Primary indication: Almonertinib is indicated for the treatment of the first-line treatment of adult patients with advanced non-small cell lung cancer (NSCLC) whose tumours have EGFR exon 19 deletions or exon 21 (L858R) substitution mutations.Curator reviewed · 3 structured indications
Formula / weight: C₃₀H₃₅N₇O₂ · 525.657 g/mol (avg)
First approval: European Union, 2026
Also known as: 2-Propenamide, N-[5-[[4-(1-cyclopropyl-1H-indol-3-yl)-2-pyrimidinyl]amino]-2-[[2-(dimethylamino)ethyl]methylamino]-4-methoxyphenyl]- · Ametinib · Aumolertinib · EGFR T790M INHIBITOR HS-10296 · N-[5-[[4-(1-Cyclopropyl-1H-indol-3-yl)-2-pyrimidinyl]amino]-2-[[2-(dimethylamino)ethyl]methylamino]-4-methoxyphenyl]-2-propenamide
Code names: EQ-143 · HS-10296