Firmonertinib
| Clinical data | |
|---|---|
| Other names | Alflutinib mesylate; AST-2818; Furmonertinib; Furmonertinib mesylate; Iflutinib mesylate; Ivesa; Vometinib mesylate |
| Legal status | |
| Legal status |
|
| Identifiers | |
| |
| CAS Number | |
| PubChem CID | |
| IUPHAR/BPS | |
| DrugBank | |
| ChemSpider | |
| UNII | |
| KEGG | |
| ChEBI | |
| ChEMBL | |
| Chemical and physical data | |
| Formula | C28H31F3N8O2 |
| Molar mass | 568.605g·mol−1 |
| 3D model (JSmol) | |
| |
| |
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
[edit ]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
[edit ]Firmonertinib is currently in phase 3 clinical trials in North America, Europe, and Asia for non-small cell lung cancer in the.[5]
Approvals
[edit ]It was approved for use in China in 2021 in NSCLC patients with confirmed EGFR T790M mutations.[1]
References
[edit ]- 1 2 Deeks ED (October 2021). "Furmonertinib: First Approval". Drugs. 81 (15): 1775–1780. doi:10.1007/s40265-021-01588-w. PMID 34528187.
- ↑ "Firmonertinib - Allist Pharmaceuticals". AdisInsight. Springer Nature Switzerland AG.
- ↑ Spira A, Cho BC, Felip E, Garon EB, Goto K, Johnson M, et al. (January 2025). "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. 199 108066. Amsterdam, Netherlands. doi:10.1016/j.lungcan.2024.108066. PMID 39764938.
- ↑ Verma T, Mehra A, Mittal A (February 2026). "Targeting EGFR With Indole Derivatives: Recent Advances and Therapeutic Perspectives". Chemistry & Biodiversity. 23 (2) e02968. 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
This pharmacology-related article is a stub. You can help Wikipedia by adding missing information.