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ponatinib + trametinib
- Development stage
- Unknown
- Lead developer
- Memorial Sloan Kettering Cancer Center
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
The combination of ponatinib and trametinib is an investigational therapy for KRAS-mutant non-small cell lung cancer (NSCLC). Ponatinib is a multi-tyrosine kinase inhibitor targeting BCR-ABL, FGFR, PDGFR, VEGFR2, KIT, FLT3, and RET. Trametinib is a selective allosteric inhibitor of MEK1 and MEK2. The rationale for combining these agents is based on preclinical data showing synergistic inhibition of the MAPK pathway and tumor shrinkage in KRAS-mutant NSCLC models. Clinical trials have evaluated this combination in patients with advanced NSCLC harboring KRAS mutations who have progressed after standard therapies[1][3][6].
- Brand names
- MekinistIclusig
- Other names
- trametinib and ponatinibponatinib plus trametinib
02
Targets
FGFR (FGFR family)ABL1 (ABL proto-oncogene 1, non-receptor tyrosine kinase)MEK1 (Dual specificity mitogen-activated protein kinase kinase 1)MEK2 (Dual specificity mitogen-activated protein kinase kinase 2)PDGFRA (Platelet-derived growth factor receptor alpha)VEGFR2 (Vascular endothelial growth factor receptor 2)RET (Rearranged during transfection receptor tyrosine kinase)FLT3 (Fms related receptor tyrosine kinase 3)KIT (c-KIT proto-oncogene receptor tyrosine kinase)
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