Drug intelligence / Profile preview

capmatinib + dabrafenib + trametinib

Development stage
Preclinical
Lead developer
Novartis
Modality
Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

Capmatinib + dabrafenib + trametinib is an investigational combination therapy comprising three small-molecule targeted agents. Capmatinib is a selective inhibitor of the MET receptor tyrosine kinase, which is involved in tumor cell growth and survival. Dabrafenib inhibits mutant BRAF kinases, particularly BRAF V600E, blocking aberrant MAPK pathway signaling that drives cancer proliferation. Trametinib inhibits MEK1 and MEK2, downstream effectors in the same MAPK pathway. This triple combination targets tumors with co-occurring alterations such as BRAF fusions/mutations and MET amplification or dysregulation, aiming to overcome resistance mechanisms that may arise with single- or double-agent regimens. The regimen has been reported in case studies for advanced non-small cell lung cancer (NSCLC) harboring both KIAA1549-BRAF fusion and MET amplification[2]. Its use remains investigational; further clinical validation is needed.

02

Targets

MEK2 (Dual specificity mitogen-activated protein kinase kinase 2)MEK1 (Dual specificity mitogen-activated protein kinase kinase 1)BRAF (B-Raf proto-oncogene, serine/threonine kinase)MET (Mesenchymal-epithelial transition factor receptor)

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