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everolimus + sunitinib
- Development stage
- Phase 1
- Lead developer
- Novartis
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
A two-drug oral combination of the mTOR inhibitor everolimus and the multi‑target VEGF/PDGF receptor tyrosine kinase inhibitor sunitinib, investigated primarily in metastatic renal cell carcinoma to achieve simultaneous inhibition of the PI3K/AKT/mTOR pathway and angiogenic signaling. Phase I studies found the combination produced responses but was associated with significant acute and chronic toxicities, and was only tolerated at attenuated doses or modified schedules; daily coadministration was poorly tolerated, and weekly everolimus with reduced‑dose sunitinib was the most feasible regimen explored.[3][2][1]
- Other names
- everolimus and sunitinibsunitinib plus everolimus
02
Targets
CSF1R (Macrophage colony-stimulating factor receptor)FKBP1AFLT3 (Fms related receptor tyrosine kinase 3)KIT (c-KIT proto-oncogene receptor tyrosine kinase)PDGFRA (Platelet-derived growth factor receptor alpha)PDGFRB (Platelet-derived growth factor receptor beta)RET (Rearranged during transfection receptor tyrosine kinase)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR2 (Vascular endothelial growth factor receptor 2)VEGFR4 (Vascular endothelial growth factor Receptor-3)Mechanistic target of rapamycin complex 1
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