Drug intelligence / Profile preview

SIR-Spheres + regorafenib

Development stage
Unknown
Lead developer
Sirtex
Modality
Small Molecules, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics
Administration
Intra-arterial, Oral
01

Overview

SIR-Spheres + regorafenib is a combination therapy consisting of selective internal radiation therapy (SIRT) using SIR-Spheres (yttrium-90 resin microspheres) and the oral multikinase inhibitor regorafenib. This regimen is being investigated for the treatment of patients with refractory metastatic colorectal cancer (mCRC) with liver metastases. - **SIR-Spheres** deliver targeted radiotherapy directly to liver tumors via intra-arterial administration of yttrium-90–labeled resin microspheres, causing localized tumor cell death through beta radiation. - **Regorafenib** is a small molecule inhibitor that targets multiple protein kinases involved in angiogenesis (such as VEGFR1/2/3), oncogenesis (such as KIT, RET), and the tumor microenvironment. It acts primarily by inhibiting angiogenic signaling pathways and tumor proliferation. The combination aims to enhance local control of hepatic metastases while also targeting systemic disease progression[1][2][6].

Brand names
Stivarga
Other names
SIR-Spheres + regorafenibSIRT + regorafenibselective internal radiation therapy with yttrium-90 resin microspheres plus regorafenib
02

Targets

BRAF (B-Raf proto-oncogene, serine/threonine kinase)KIT (c-KIT proto-oncogene receptor tyrosine kinase)TEK (Tie2)PDGFRB (Platelet-derived growth factor receptor beta)RAF1 (c-Raf-1 (Y340D/Y341D))VEGFR3 (Vascular endothelial growth factor receptor 3)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR2 (Vascular endothelial growth factor receptor 2)FGFR1 (Fibroblast growth factor receptor 1)RET (Rearranged during transfection receptor tyrosine kinase)

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