Drug intelligence / Profile preview

crizotinib + furmonertinib

Development stage
Preclinical
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

Crizotinib + furmonertinib is a combination of two small molecule tyrosine kinase inhibitors used in the treatment of advanced non-small cell lung cancer (NSCLC) with specific genetic alterations. Crizotinib is a multitargeted TKI that inhibits anaplastic lymphoma kinase (ALK), ROS1, and MET kinases, while furmonertinib is a third-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor designed to target EGFR mutations, including uncommon mutations and those associated with resistance to earlier EGFR-TKIs. This combination has been investigated for overcoming acquired resistance in NSCLC patients harboring both EGFR mutations and MET amplification, particularly after progression on prior EGFR-TKI therapies. Clinical case reports and small studies suggest that this dual inhibition can induce partial remission or disease control in patients with these molecular profiles[5][6]. Furmonertinib has demonstrated efficacy against CNS metastases due to its high brain penetration[2].

Other names
crizotinib + furmonertinib
02

Targets

ALK (Anaplastic lymphoma kinase receptor tyrosine kinase)MST1R (Recepteur d'origine nantais)MET (Mesenchymal-epithelial transition factor receptor)EGFR T790M (Epidermal growth factor receptor T790M mutant)ROS1 (Proto-oncogene tyrosine-protein kinase ROS)

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