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FOLFIRI + regorafenib
- Development stage
- Phase 2
- Lead developer
- Bayer
- Modality
- Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Allosteric Modulators → Classical Binding Small Molecules → Small Molecules, Irreversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules, Reversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules, DNA Intercalators/Alkylators → Nucleic Acid-Directed Small Molecules → Small Molecules, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, Bivalent/Multivalent Binders → Multivalent & Scaffold-Based Small Molecules → Small Molecules, Fragment-Derived Small Molecules → Multivalent & Scaffold-Based Small Molecules → Small Molecules, Recombinant Proteins and Enzymes
- Administration
- Intravenous, Oral
01
Overview
FOLFIRI + regorafenib is a combination therapy used primarily in the treatment of metastatic colorectal cancer, especially in patients who have progressed after standard first-line therapies. FOLFIRI is a chemotherapy regimen consisting of folinic acid (leucovorin), fluorouracil (5-FU), and irinotecan. Folinic acid enhances the effectiveness of 5-FU, which acts as an antimetabolite to disrupt DNA synthesis, while irinotecan inhibits topoisomerase I, blocking DNA replication and leading to cancer cell death[6][8][10]. 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 VEGFR1-3, PDGFR-β, FGFR1/2/3/4, KIT, RET, RAF-1/BRAF (including mutant BRAF), TIE2 and others[4][7]. The combination aims to leverage both cytotoxic chemotherapy and targeted inhibition of key signaling pathways for improved disease control. Clinical studies suggest this regimen can provide modest improvements in progression-free survival compared to FOLFIRI alone but may be associated with increased toxicity[3][4][5].
- Other names
- regorafenib plus FOLFIRIregorafenib + folinic acid + fluorouracil + irinotecan
02
Targets
BRAF (B-Raf proto-oncogene, serine/threonine kinase)FGFR1 (Fibroblast growth factor receptor 1)FGFR2 (Keratinocyte growth factor receptor)KIT (c-KIT proto-oncogene receptor tyrosine kinase)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)TOP1 (DNA Topoisomerase I)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR2 (Vascular endothelial growth factor receptor 2)VEGFR4 (Vascular endothelial growth factor Receptor-3)FGFR (FGFR family)ARAF (Proto-oncogene serine/threonine-protein kinase A-Raf)
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