Drug intelligence / Profile preview

regorafenib + ruxolitinib

Development stage
Discontinued
Lead developer
Incyte
Modality
Small Molecules
Administration
Oral
01

Overview

Regorafenib + ruxolitinib is an investigational combination therapy consisting of two small molecule inhibitors, regorafenib and ruxolitinib. Regorafenib is a multi-kinase inhibitor that targets several protein kinases involved in tumor angiogenesis (such as vascular endothelial growth factor receptors), oncogenesis (including KIT, RET, RAF-1, BRAF), and the tumor microenvironment. Ruxolitinib is a potent inhibitor of Janus kinase 1 and 2 (JAK1/2), which are key components of the JAK-STAT signaling pathway implicated in inflammation and cancer cell survival. This combination has been studied primarily for relapsed or refractory metastatic colorectal cancer to assess whether dual inhibition of these pathways could improve outcomes compared to standard therapies. Clinical trials have shown that while the combination did not increase safety concerns compared to monotherapy, it did not improve overall survival or progression-free survival versus regorafenib alone[3][5][7].

02

Targets

BRAF V600EFGFR1 (Fibroblast growth factor receptor 1)JAK1 (Janus kinase 1)JAK2 (Janus kinase 2)JAK3 (Janus kinase 3)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)TYK2 (Tyrosine kinase 2)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR2 (Vascular endothelial growth factor receptor 2)VEGFR4 (Vascular endothelial growth factor Receptor-3)BRAF (B-Raf proto-oncogene, serine/threonine kinase)PDGFRA (Platelet-derived growth factor receptor alpha)

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