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Regorafenib (BAY 73-4506) is a novel and orally active multikinase inhibitor of receptor tyrosine kinases VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit, RET, Raf-1, B-RAF and B-RAFV600E with IC50 values of 13 nM/4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM, 2.5 nM, 28 nM and 19 nM [1].

VEGFR1/2/3 are vascular endothelial growth factor receptor plays an important role in the formation of normal and tumor vasculature. platelet-derived growth factor receptor-β (PDGFRβ) is a receptor for the platelet-derived growth factor family. Kit, RET and B-RAF are both receptor tyrosine kinases that encoded by proto-oncogenes [1].

Regorafenib (BAY 73-4506) is a novel and orally active receptor tyrosine kinases inhibitor. In NIH-3T3/VEGFR2 cells, regorafenib potently inhibited VEGFR2 autophosphorylation with IC50 value of 3 nM. Regorafenib also inhibited TIE2 and PDGFR-β autophosphorylation with IC50 values of 31 and 90 nM. Regorafenib potently inhibited KITK642E and RETC634W with IC50 values of ~20 and ~10 nM, respectively. In addition, regorafenib inhibited the proliferation of VEGF165-stimulated HUVECs with IC50 value of ~3 nM [1].

In GS9L glioblastoma xenografted rat model, regorafenib administered orally at 10 mg/kg significantly reduced the extravasation of Gadomer in the vasculature. In various preclinical human xenograft mice models, regorafenib exhibited potent dose-dependent tumor growth inhibition (TGI) [1]. In murine metastatic colorectal cancer (CRC) liver metastasis model, regorafenib significantly delayed disease progression by inhibiting the growth of liver metastases and preventing the formation of new metastases in other organs [2].

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