Drug intelligence / Profile preview

alectinib + capmatinib

Development stage
Preclinical
Lead developer
Chugai Pharmaceutical
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Allosteric Modulators → Classical Binding Small Molecules → Small Molecules, Irreversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules
Administration
Oral
01

Overview

Alectinib + capmatinib is an investigational combination therapy consisting of two oral small molecule tyrosine kinase inhibitors, each targeting distinct oncogenic drivers in non-small cell lung cancer (NSCLC). Alectinib is a highly selective inhibitor of anaplastic lymphoma kinase (ALK), approved for the treatment of ALK-positive NSCLC. Capmatinib is a selective MET inhibitor, approved for NSCLC with MET exon 14 skipping mutations or MET amplification. The rationale for combining these agents arises from the observation that acquired resistance to ALK inhibitors in ALK-rearranged NSCLC can occur via secondary activation or amplification of the MET pathway. Dual inhibition with alectinib and capmatinib aims to overcome this resistance mechanism by simultaneously blocking both ALK and MET signaling pathways. Early clinical reports suggest moderate antitumor activity and manageable safety profiles in patients with concurrent ALK rearrangement and acquired MET amplification[1][2]. This regimen remains investigational, primarily used off-label or within clinical studies.

Other names
alectinib + capmatinib combination therapy
02

Targets

ALK (Anaplastic lymphoma kinase receptor tyrosine kinase)MET (Mesenchymal-epithelial transition factor receptor)

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