Drug intelligence / Profile preview

sorafenib + pazopanib

Development stage
Unknown
Modality
Small Molecules
Administration
Oral
01

Overview

Sorafenib + pazopanib is a combination of two small molecule multi-kinase inhibitors, both of which target multiple receptor tyrosine kinases involved in tumor growth and angiogenesis. Sorafenib inhibits vascular endothelial growth factor receptors (VEGFR-1, VEGFR-2, VEGFR-3), platelet-derived growth factor receptor beta (PDGFRB), RAF kinases (including BRAF and CRAF), FLT3, c-KIT, and RET. Pazopanib targets VEGFR-1/2/3 with high affinity and also inhibits PDGFRA/B, FGFR1/2, and c-KIT. Both drugs are approved individually for the treatment of advanced renal cell carcinoma (RCC) and soft tissue sarcoma; they have also been studied in desmoid tumors and other malignancies as monotherapies. There is no evidence that the fixed combination "sorafenib + pazopanib" is an approved or widely used clinical regimen; rather, these agents are typically used sequentially or compared head-to-head in clinical trials[1][7][9]. Their mechanisms overlap but their toxicity profiles differ.

Brand names
Nexavar
Other names
pazopanib and sorafenib sequenceSWITCH-II trial regimen
02

Targets

BRAF (B-Raf proto-oncogene, serine/threonine kinase)CSF1R (Macrophage colony-stimulating factor receptor)FGFR1 (Fibroblast growth factor receptor 1)FGFR3 (Fibroblast growth factor receptor 3)VEGFR-1 (Vascular endothelial growth factor receptor 1)FLT3 (Fms related receptor tyrosine kinase 3)VEGFR4 (Vascular endothelial growth factor Receptor-3)ITK (Interleukin 2-inducible T-cell kinase)VEGFR2 (Vascular endothelial growth factor receptor 2)KIT (c-KIT proto-oncogene receptor tyrosine kinase)LCK (Proto-oncogene tyrosine-protein kinase Lck)PDGFRA (Platelet-derived growth factor receptor alpha)PDGFRB (Platelet-derived growth factor receptor beta)RAF1 (c-Raf-1 (Y340D/Y341D))RET (Rearranged during transfection receptor tyrosine kinase)FGFR2 (Keratinocyte growth factor receptor)

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