Drug intelligence / Profile preview

napabucasin + regorafenib

Development stage
Preclinical
Lead developer
Sumitomo Pharma America
Modality
Small Molecules
Administration
Oral
01

Overview

napabucasin + regorafenib is an experimental combination therapy for cancer, especially in metastatic colorectal cancer (mCRC). Napabucasin is an orally-administered small molecule inhibitor developed to block cancer stemness pathways via targeting the transcription factor STAT3, thereby inhibiting cancer cell proliferation, metastasis, and resistance to standard therapies. Regorafenib is a multikinase inhibitor targeting angiogenic (VEGFR1-3, TIE2), oncogenic (KIT, RET, RAF-1, BRAF), and stromal (PDGFR, FGFR) receptor tyrosine kinases, and has been approved as a standard of care for mCRC after other therapies. Both drugs are thought to work synergistically: napabucasin suppresses cancer stem cell properties and key signaling (such as STAT3 and β-catenin/Tcf signaling), while regorafenib blocks tumor proliferation and angiogenesis. There is no evidence of a uniquely named fixed-dose combination of napabucasin and regorafenib; all available information refers to experimental or off-protocol combinations in clinical trials[4][5].

Other names
GB201 + regorafenib
02

Targets

STAT3 (Signal Transducer and Activator of Transcription 3)NQO1KIT (c-KIT proto-oncogene receptor tyrosine kinase)VEGFR2 (Vascular endothelial growth factor receptor 2)RAF1 (c-Raf-1 (Y340D/Y341D))BRAF V600EVEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR3 (Vascular endothelial growth factor receptor 3)PDGFRB (Platelet-derived growth factor receptor beta)FGFR1 (Fibroblast growth factor receptor 1)RET (Rearranged during transfection receptor tyrosine kinase)

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