Drug intelligence / Profile preview

sunitinib + sorafenib + pazopanib

Development stage
Unknown
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

This is a combination of three small molecule tyrosine kinase inhibitors—sunitinib, sorafenib, and pazopanib. Each drug individually targets multiple receptor tyrosine kinases involved in tumor growth and angiogenesis, including vascular endothelial growth factor receptors (VEGFR) and platelet-derived growth factor receptors (PDGFR). Sunitinib inhibits VEGFR-1/2/3, PDGFR-α/β, c-KIT, FLT3, RET; sorafenib inhibits VEGFR-2/3, PDGFR-β, RAF kinases; pazopanib inhibits VEGFR-1/2/3, PDGFR-α/β, c-KIT. All three are approved for the treatment of advanced renal cell carcinoma and have been studied as monotherapies or in sequential regimens but not as a triple combination due to overlapping toxicities. Their mechanisms involve blocking angiogenesis and tumor proliferation pathways[1][6][7]. There is no evidence that this specific triple combination is used clinically or has been formally studied as a single regimen.

02

Targets

FLT3 (Fms related receptor tyrosine kinase 3)KIT (c-KIT proto-oncogene receptor tyrosine kinase)ARAF (Proto-oncogene serine/threonine-protein kinase A-Raf)RET (Rearranged during transfection receptor tyrosine kinase)PDGFRA (Platelet-derived growth factor receptor alpha)PDGFRB (Platelet-derived growth factor receptor beta)RAF1 (c-Raf-1 (Y340D/Y341D))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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