Chemistry:Firmonertinib
Firmonertinib (previously referred to as alflutinib and furmonertinib) is targeted drug that that is approved in China for the treatment of non-small cell lung cancer (NSCLC).[1] The originator of the drug was Shanghai Allist Pharmaceuticals. It is now being developed outside China through a licensing deal with ArriVent BioPharma, Inc. for the same indication. It is a epidermal growth factor receptor (EGFR) antagonist.[2][3]
Pharmacology
Firmonertinib is an EGFR inhibitor that binds irreversibly through a chemical reactive acrylamide to the Cys-797 residue of the ATP-binding site of EGFR via a Michael addition to form a covalent bond. It has binding selectivity for T790M mutant over wild‑type EGFR.[4]
Clinical trials
Firmonertinib is currently in phase 3 clinical trials in North America, Europe, and Asia for non-small cell lung cancer in the.[5]
Approvals
It was approved for use in China in 2021 in NSCLC patients with confirmed EGFR T790M mutations.[1]
References
- ↑ 1.0 1.1 "Furmonertinib: First Approval". Drugs 81 (15): 1775–1780. October 2021. doi:10.1007/s40265-021-01588-w. PMID 34528187.
- ↑ "Firmonertinib - Allist Pharmaceuticals". AdisInsight. Springer Nature Switzerland AG. https://adisinsight.springer.com/drugs/800048377.
- ↑ "FURVENT: Phase 3 trial of firmonertinib vs chemotherapy as first-line treatment for advanced NSCLC with EGFR exon 20 insertion mutations (FURMO-004)". Lung Cancer (Amsterdam, Netherlands) 199. January 2025. doi:10.1016/j.lungcan.2024.108066. PMID 39764938.
- ↑ "Targeting EGFR With Indole Derivatives: Recent Advances and Therapeutic Perspectives". Chemistry & Biodiversity 23 (2). February 2026. doi:10.1002/cbdv.202502968. PMID 41664998.
- ↑ Clinical trial number NCT07185997 for "Study to Evaluate Efficacy and Safety of Firmonertinib Compared With Investigator's Choice of EGFR Inhibitor as First-Line Treatment in Participants Who Have Locally Advanced or Metastatic NSCLC With EGFR P-Loop and Alpha C-Helix Compressing (PACC) Uncommon Mutations" at ClinicalTrials.gov
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