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tremelimumab + sunitinib
- Development stage
- Unknown
- 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
PDGFRA (Platelet-derived growth factor receptor alpha)KIT (c-KIT proto-oncogene receptor tyrosine kinase)VEGFR2 (Vascular endothelial growth factor receptor 2)CSF1R (Macrophage colony-stimulating factor receptor)PDGFRB (Platelet-derived growth factor receptor beta)CTLA-4 (Cytotoxic t-lymphocyte–associated protein 4)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR3 (Vascular endothelial growth factor receptor 3)RET (Rearranged during transfection receptor tyrosine kinase)FLT3 (Fms related receptor tyrosine kinase 3)
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