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sunitinib + sorafenib

Development stage: Unknown
Lead developer: Pfizer
Modality: Small Molecules
Administration: Oral

Overview

Sunitinib + sorafenib is a combination of two small-molecule multi-targeted receptor tyrosine kinase inhibitors (TKIs), each approved individually for the treatment of advanced renal cell carcinoma and other malignancies. Both drugs inhibit multiple kinases involved in tumor angiogenesis and proliferation. Sunitinib targets vascular endothelial growth factor receptors (VEGFR-1, VEGFR-2, VEGFR-3), platelet-derived growth factor receptors (PDGFR-alpha and PDGFR-beta), KIT (CD117), RET, Flt3, and colony-stimulating factor 1 receptor (CSF-1R). Sorafenib inhibits CRAF, BRAF, VEGFRs 1–3, PDGFR-beta/3, RET, Flt3 and c-Kit. The combination has been explored primarily in sequential therapy for metastatic renal cell carcinoma due to their overlapping but distinct target profiles[1][2][8]. Both agents are orally administered.

Brand names: Nexavar
Other names: sunitinib malatesorafenib tosylate

Targets

BRAF (B-Raf proto-oncogene, serine/threonine kinase)CSF1R (Macrophage colony-stimulating factor receptor)PDGFRB (Platelet-derived growth factor receptor beta)RAF1 (c-Raf-1 (Y340D/Y341D))VEGFR2 (Vascular endothelial growth factor receptor 2)FGFR1 (Fibroblast growth factor receptor 1)RET (Rearranged during transfection receptor tyrosine kinase)FLT3 (Fms related receptor tyrosine kinase 3)KIT (c-KIT proto-oncogene receptor tyrosine kinase)

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