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Drug intelligence / Profile preview
pazopanib + everolimus
- Development stage
- Phase 2
- Lead developer
- Novartis
- Modality
- Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Allosteric Modulators → Classical Binding Small Molecules → Small Molecules
- Administration
- Oral
01
Overview
Pazopanib + everolimus is a combination of two small molecule targeted therapies used primarily in oncology clinical trials. Pazopanib is a second-generation multitargeted tyrosine kinase inhibitor that blocks vascular endothelial growth factor receptor 1 (VEGFR1), vascular endothelial growth factor receptor 2 (VEGFR2), vascular endothelial growth factor receptor 3 (VEGFR3), platelet-derived growth factor receptor alpha, platelet-derived growth factor receptor beta, and c-Kit. This inhibits angiogenesis and tumor cell proliferation. Everolimus is an mTOR (mechanistic target of rapamycin) inhibitor that binds to FKBP-12 to inhibit mTORC1 activity, leading to reduced cell proliferation and angiogenesis. The combination aims to synergistically block both the VEGF pathway (angiogenesis) and the PI3K/AKT/mTOR pathway (cell growth/survival). It has been studied in advanced solid tumors including metastatic renal cell carcinoma and urothelial carcinoma[1][2][4].
- Other names
- Votrient + AfinitorPazopanib and Everolimus combination
02
Targets
FKBP1APDGFRA (Platelet-derived growth factor receptor alpha)PDGFRB (Platelet-derived growth factor receptor beta)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR2 (Vascular endothelial growth factor receptor 2)VEGFR4 (Vascular endothelial growth factor Receptor-3)KIT (c-KIT proto-oncogene receptor tyrosine kinase)Mechanistic target of rapamycin complex 1
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