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regorafenib + irinotecan drug-eluting beads
- Development stage
- Unknown
- Lead developer
- Sun Yat-sen University
- Modality
- Small Molecules
- Administration
- Oral, Intra-arterial
01
Overview
This combination therapy consists of regorafenib, an oral multi-kinase inhibitor, and irinotecan-loaded drug-eluting beads (DEBIRI) administered via transarterial chemoembolization (TACE). Regorafenib (brand name Stivarga) targets multiple protein kinases involved in tumor angiogenesis (VEGFR1, -2, -3, TIE2), oncogenesis (KIT, RET, RAF-1, BRAF), and the tumor microenvironment (PDGFR, FGFR). The DEBIRI component involves the locoregional delivery of high-dose irinotecan, a topoisomerase I inhibitor, directly into the hepatic artery supplying liver metastases. This approach aims to maximize local tumor cytotoxicity while minimizing systemic side effects. The regimen is currently being evaluated in the Phase 3 RIDER trial, sponsored by Sun Yat-sen University, as a third-line treatment for patients with colorectal cancer liver metastases who have progressed on standard chemotherapy.
- Brand names
- Stivarga
- Other names
- regorafenib + DEBIRIregorafenib + DIBIRIRegorafenib Combined With Irinotecan Drug-Eluting Beads
02
Targets
KIT (c-KIT proto-oncogene receptor tyrosine kinase)VEGFR2 (Vascular endothelial growth factor receptor 2)RAF1 (c-Raf-1 (Y340D/Y341D))TEK (Tie2)VEGFR-1 (Vascular endothelial growth factor receptor 1)BRAF V600EVEGFR3 (Vascular endothelial growth factor receptor 3)TOP1 (DNA Topoisomerase I)PDGFRB (Platelet-derived growth factor receptor beta)FGFR1 (Fibroblast growth factor receptor 1)RET (Rearranged during transfection receptor tyrosine kinase)
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