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cabozantinib + lorlatinib
- Development stage
- Preclinical
- Lead developer
- Exelixis
- 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
Cabozantinib + lorlatinib is a combination of two small molecule tyrosine kinase inhibitors used together in the treatment of non-small cell lung cancer (NSCLC), particularly in cases with ROS1 rearrangements that have developed resistance to prior targeted therapies. Cabozantinib inhibits multiple receptor tyrosine kinases including MET, VEGFR2, RET, AXL, KIT, and others. Lorlatinib is a third-generation inhibitor targeting ALK and ROS1 kinases. This combination has shown efficacy in overcoming specific resistance mutations such as ROS1 L2086F that are refractory to other available TKIs. The regimen has demonstrated clinical benefit and tolerability in case reports for patients with advanced NSCLC harboring complex resistance patterns[1][2][3].
- Other names
- cabozantinib and lorlatinibcabozantinib plus lorlatiniblorlatinib and cabozantinib
02
Targets
ALK (Anaplastic lymphoma kinase receptor tyrosine kinase)AXL (AXL receptor tyrosine kinase)MET (Mesenchymal-epithelial transition factor receptor)KIT (c-KIT proto-oncogene receptor tyrosine kinase)VEGFR2 (Vascular endothelial growth factor receptor 2)ROS1 (Proto-oncogene tyrosine-protein kinase ROS)RET (Rearranged during transfection receptor tyrosine kinase)
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