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vatalanib + everolimus
- Development stage
- Unknown
- Lead developer
- Novartis
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Combination of the small-molecule VEGFR tyrosine kinase inhibitor vatalanib with the mTOR inhibitor everolimus for advanced solid tumors, including renal cell carcinoma. Vatalanib inhibits vascular endothelial growth factor receptors (VEGFR-1/2/3) and related angiogenic kinases, suppressing tumor angiogenesis; everolimus inhibits mTOR complex 1, reducing tumor cell growth, proliferation, and metabolism. Phase I/Ib studies established maximum tolerated doses and showed manageable toxicity with signals of antitumor activity across tumor types and in metastatic RCC dose-expansion cohorts. Investigated in trials such as NCT00655655 and other early-phase studies.
- Other names
- vatalanib plus everolimusvatalanib and everolimusvatalanib PTK787 ZK222584 plus everolimus RAD001
02
Targets
FKBP1APDGFRB (Platelet-derived growth factor receptor beta)VEGFR3 (Vascular endothelial growth factor receptor 3)KIT (c-KIT proto-oncogene receptor tyrosine kinase)VEGFR2 (Vascular endothelial growth factor receptor 2)Mechanistic target of rapamycin complex 1CSF1R (Macrophage colony-stimulating factor receptor)VEGFR-1 (Vascular endothelial growth factor receptor 1)
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