Drug intelligence / Profile preview

capmatinib + crizotinib + tepotinib

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

Overview

This is a combination of three small molecule tyrosine kinase inhibitors—capmatinib, crizotinib, and tepotinib—all of which target the mesenchymal-epithelial transition (MET) receptor tyrosine kinase. Capmatinib and tepotinib are highly selective MET inhibitors that block ATP binding to the MET receptor, thereby inhibiting downstream oncogenic signaling pathways involved in cell proliferation and survival. Crizotinib is a multikinase inhibitor that targets MET as well as ALK and ROS1 kinases. All three agents have demonstrated efficacy in non-small cell lung cancer (NSCLC), particularly in tumors harboring MET exon 14 skipping mutations or amplifications. Each drug has been approved individually for use in metastatic NSCLC with specific molecular alterations; however, there is no evidence supporting the clinical use or approval of this exact triple combination.

02

Targets

ALK (Anaplastic lymphoma kinase receptor tyrosine kinase)AXL (AXL receptor tyrosine kinase)MET (Mesenchymal-epithelial transition factor receptor)ROS1 (Proto-oncogene tyrosine-protein kinase ROS)IRAK1 (Interleukin-1 receptor-associated kinase 1)

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