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tremelimumab + sunitinib
- Development stage
- Phase 1
- Lead developer
- AstraZeneca
- Modality
- Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
- Administration
- Intravenous (tremelimumab), Oral (sunitinib)
01
Overview
This is a combination therapy of **tremelimumab**, a monoclonal antibody targeting cytotoxic T-lymphocyte-associated antigen 4 (CTLA-4), and **sunitinib**, an oral small molecule multi-targeted receptor tyrosine kinase inhibitor. Tremelimumab acts as an immune checkpoint inhibitor to enhance T-cell mediated antitumor responses, while sunitinib inhibits multiple receptor tyrosine kinases (including VEGFR, PDGFR, KIT, FLT3, CSF-1R, RET), interrupting tumor growth, angiogenesis, and metastatic progression. This combination has been investigated in clinical trials for metastatic renal cell carcinoma based on the potential for additive or synergistic immunostimulatory and antitumor effects[1][7].
02
Targets
CSF1R (Macrophage colony-stimulating factor receptor)CTLA-4 (Cytotoxic t-lymphocyte–associated protein 4)FLT3 (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)GFRA4 (GDNF family receptor alpha-4)
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