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Temsirolimus + sunitinib
- Development stage
- Phase 2
- Lead developer
- Pfizer
- Modality
- Small Molecules
- Administration
- Intravenous, Oral
01
Overview
Temsirolimus + sunitinib is a combination of two targeted cancer therapies investigated primarily for the treatment of advanced or metastatic renal cell carcinoma (RCC). Temsirolimus is an inhibitor of mammalian target of rapamycin (mTOR), binding to FKBP-12 and blocking mTOR activity, which leads to cell cycle arrest in tumor cells. Sunitinib is a multi-targeted tyrosine kinase inhibitor that blocks vascular endothelial growth factor receptors (VEGFRs), platelet-derived growth factor receptors (PDGFRs), colony-stimulating factor receptor, and c-KIT, thereby inhibiting angiogenesis and tumor proliferation. Both drugs are approved individually for RCC but have been studied together due to their different mechanisms and non-overlapping toxicities. However, clinical trials have shown that concurrent use at standard doses results in significant dose-limiting toxicities, making this combination not recommended for routine use[1][2][3][5].
- Other names
- temsirolimus + sunitinib
02
Targets
CSF1R (Macrophage colony-stimulating factor receptor)CYP2D6 (Cytochrome P450 2D6)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)mTOR (Mammalian target of rapamycin kinase)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR2 (Vascular endothelial growth factor receptor 2)VEGFR4 (Vascular endothelial growth factor Receptor-3)
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