Drug intelligence / Profile preview

regorafenib + FOLFOX

Development stage
Phase 3
Lead developer
Bayer
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

Regorafenib + FOLFOX is a combination regimen used primarily in the treatment of metastatic colorectal cancer. Regorafenib is an oral multikinase inhibitor that targets multiple protein kinases involved in tumor angiogenesis, oncogenesis, and the tumor microenvironment. It inhibits kinases such as VEGFR1/2/3, PDGFR, FGFR, KIT, RET, RAF1/BRAF among others. The FOLFOX regimen consists of folinic acid (leucovorin), fluorouracil (5-FU), and oxaliplatin; it acts as cytotoxic chemotherapy by interfering with DNA synthesis and function in rapidly dividing cells. This combination has been studied for its safety and efficacy as first-line or subsequent therapy for metastatic colorectal cancer patients who have progressed on standard treatments[1][2][3]. While some studies suggest potential survival benefits from combining regorafenib with conventional chemotherapy like FOLFOX compared to monotherapy[3], increased toxicity has also been observed[1][2]. The optimal dosing schedule remains under investigation.

Brand names
Eloxatin
Other names
regorafenib plus FOLFOXregorafenib and FOLFOX combination therapy
02

Targets

ABL1 (ABL proto-oncogene 1, non-receptor tyrosine kinase)BRAF V600ECSF1R (Macrophage colony-stimulating factor receptor)DDR2 (Discoidin domain receptor tyrosine kinase 2)DNAEPHA2 (Ephrin type-A receptor 2)FGFR1 (Fibroblast growth factor receptor 1)FGFR2 (Keratinocyte growth factor receptor)KIT (c-KIT proto-oncogene receptor tyrosine kinase)NTRK1 (Tropomyosin-related receptor kinase A)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)TEK (Tie2)TS (Thymidylate synthase)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR2 (Vascular endothelial growth factor receptor 2)VEGFR4 (Vascular endothelial growth factor Receptor-3)RK (Ribokinase)

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