Drug intelligence / Profile preview

crizotinib + dacomitinib

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

Overview

Crizotinib + dacomitinib is a combination of two small molecule tyrosine kinase inhibitors investigated for the treatment of advanced non-small cell lung cancer (NSCLC). Crizotinib targets and inhibits anaplastic lymphoma kinase (ALK), ROS1, and mesenchymal epithelial transition factor (MET) receptor tyrosine kinases, thereby blocking signaling pathways that promote tumor cell proliferation and survival. Dacomitinib is an irreversible inhibitor of the human epidermal growth factor receptor (EGFR/HER1), HER2, and HER4 tyrosine kinases, covalently binding to cysteine residues in their catalytic domains to block downstream signaling involved in tumor growth and resistance. The combination was studied primarily in patients with NSCLC who had progressed after prior therapies; however, clinical trials showed limited antitumor activity with substantial toxicity[1][2][3].

Brand names
XalkoriVizimpro
Other names
crizotinib + dacomitinib
02

Targets

ALK (Anaplastic lymphoma kinase receptor tyrosine kinase)AXL (AXL receptor tyrosine kinase)MET (Mesenchymal-epithelial transition factor receptor)LCK (Proto-oncogene tyrosine-protein kinase Lck)ERBB2 (Erb-b2 receptor tyrosine kinase 2)EPHA6ROS1 (Proto-oncogene tyrosine-protein kinase ROS)ERBB4 (Erb-b2 receptor tyrosine kinase 4)MKNK1 (Mitogen‑activated protein kinase‑interacting serine/threonine-protein kinase 1)DDR1 (Discoidin domain receptor 1)EGFR T790M (Epidermal growth factor receptor T790M mutant)DDR2 (Discoidin domain receptor tyrosine kinase 2)

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