Drug intelligence / Profile preview

irinotecan + regorafenib

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

Overview

Irinotecan + regorafenib is an investigational combination therapy composed of two small molecule drugs, primarily studied for the treatment of metastatic colorectal cancer and other advanced gastrointestinal malignancies. Irinotecan is a topoisomerase I inhibitor that interferes with DNA replication in cancer cells, leading to cell death. Regorafenib is an oral multikinase inhibitor targeting several protein kinases involved in tumor angiogenesis (such as VEGFR1/2/3), oncogenesis (including KIT, RET, RAF), and the tumor microenvironment. The combination aims to leverage the cytotoxic effects of irinotecan with the antiangiogenic and antiproliferative properties of regorafenib to improve outcomes in patients who have progressed on standard therapies[1][2][4][8]. This regimen has been evaluated in multiple phase II and III clinical trials for metastatic colorectal cancer after failure of standard treatments[1][4][8].

Brand names
Stivarga (regorafenib)Camptosar (irinotecan hydrochloride)
Other names
REGIRIregorafenib plus irinotecanregorafenib and irinotecan combination
02

Targets

PDGFRA (Platelet-derived growth factor receptor alpha)KIT (c-KIT proto-oncogene receptor tyrosine kinase)VEGFR2 (Vascular endothelial growth factor receptor 2)RAF1 (c-Raf-1 (Y340D/Y341D))PDGFRB (Platelet-derived growth factor receptor beta)TOP1 (DNA Topoisomerase I)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR3 (Vascular endothelial growth factor receptor 3)RET (Rearranged during transfection receptor tyrosine kinase)

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