Drug intelligence / Profile preview

regorafenib + dabrafenib + trametinib

Development stage
Unknown
Lead developer
Universitair Ziekenhuis Brussel
Modality
Small Molecules
Administration
Oral
01

Overview

This triplet therapy is an investigational combination regimen being evaluated by the Universitair Ziekenhuis Brussel (UZ Brussel) for the treatment of advanced, pretreated melanoma. The regimen consists of the oral multi-kinase inhibitor regorafenib (Stivarga) administered in combination with a standard-of-care BRAF inhibitor and MEK inhibitor pair, such as dabrafenib plus trametinib or encorafenib plus binimetinib. Regorafenib targets multiple kinases involved in angiogenesis (VEGFR1-3, TIE2), oncogenesis (KIT, RET, RAF-1, BRAF), and the tumor microenvironment (PDGFR, FGFR). By adding regorafenib to the targeted MAPK pathway inhibition provided by BRAF and MEK inhibitors, the therapy aims to overcome acquired resistance and improve outcomes in patients who have progressed on prior immune checkpoint inhibitors and standard targeted therapies, including those with refractory melanoma brain metastases.

Brand names
StivargaTafinlarMekinistBraftoviMektovi
Other names
regorafenib + encorafenib + binimetinibtriplet therapy-Universitair Ziekenhuis Brussel-melanoma
02

Targets

BRAF (B-Raf proto-oncogene, serine/threonine kinase)KIT (c-KIT proto-oncogene receptor tyrosine kinase)VEGFR2 (Vascular endothelial growth factor receptor 2)PDGFRA (Platelet-derived growth factor receptor alpha)TEK (Tie2)RAF1 (c-Raf-1 (Y340D/Y341D))CAPN3 (B-Raf proto-oncogene, serine/threonine kinase)MEK1 (Dual specificity mitogen-activated protein kinase kinase 1)RET (Rearranged during transfection receptor tyrosine kinase)VEGFR-1 (Vascular endothelial growth factor receptor 1)

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