STIVARGA® (regorafenib) is an oral inhibitor of multiple kinases

Target normal cellular functions and pathological processes such as oncogenesis, tumor angiogenesis, metastasis, and tumor immunity1,2

  • In in vitro biochemical or cellular assays, STIVARGA or its major human active metabolites, M-2 and M-5, inhibited the activity of RET, VEGFR1, VEGFR2, VEGFR3, KIT, PDGFR-alpha, PDGFR-beta, FGFR1, FGFR2, TIE2, DDR2, TrkA, Eph2A, RAF-1, BRAF, BRAFV600E, SAPK2, PTK5, Abl, and CSF1R at concentrations of STIVARGA that have been achieved clinically1
  • In in vivo models, STIVARGA demonstrated anti-angiogenic activity in a rat tumor model and inhibition of tumor growth in several mouse xenograft models including some for human colorectal carcinoma. STIVARGA also demonstrated anti-metastatic activity in a mouse xenograft model and 2 mouse orthotopic models of human colorectal carcinoma1

View aspects of mCRC mechanism of disease at the cellular level

This video explores key aspects of tumor function and pathologic processes in the mCRC tumor microenvironment.

Test

STIVARGA demonstrated the following activity3-8:

How STIVARGA (regorafenib) may work. Visit hcp.stivarga-us.com to see full safety and Prescribing Information, including Boxed Warning.

Oncogenesis

  • STIVARGA potently blocks multiple protein kinases, including KIT, RAF-1, and RET, which are important in oncogenesis1,3,4
Tumor Immunity
Tumor Cell
How STIVARGA (regorafenib) may work. Visit hcp.stivarga-us.com to see full safety and Prescribing Information, including Boxed Warning.

Tumor Angiogenesis

  • STIVARGA inhibits key angiogenic receptors: VEGFR1, 2, and 3; TIE2; PDGFR-alpha and -beta; and FGFR1 and 2 via kinase inhibition1,3-5
Endothelial Cell
Endothelial Cell
How STIVARGA (regorafenib) may work. Visit hcp.stivarga-us.com to see full safety and Prescribing Information, including Boxed Warning.

Metastasis

  • STIVARGA inhibits VEGFR2 and 3, important mediators involved in endothelial cell proliferation and migration1,4,6
  • Blocks PDGFR, believed to play a role in cancer-associated, fibroblast-induced metastasis1,7
Pericyte
Pericyte
How STIVARGA (regorafenib) may work. Visit hcp.stivarga-us.com to see full safety and Prescribing Information, including Boxed Warning.

Tumor Immunity

  • STIVARGA disrupts tumor immunity by inhibiting CSF1R, a receptor important for macrophage proliferation1,8
Macrophage
Macrophage