Drug intelligence / Profile preview

atezolizumab + regorafenib

Development stage
Preclinical
Lead developer
Roche
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Intravenous, Oral
01

Overview

**Atezolizumab + regorafenib** is a combination therapy consisting of atezolizumab (a monoclonal antibody immune checkpoint inhibitor targeting PD-L1) and regorafenib (a small molecule multikinase inhibitor). - **Atezolizumab** blocks the interaction between PD-L1 on tumor cells and PD-1 on T cells, thereby enhancing T-cell mediated anti-tumor immune responses. - **Regorafenib** is an oral multikinase inhibitor that targets and inhibits multiple protein kinases involved in tumor angiogenesis, oncogenesis, and the tumor microenvironment, including VEGF receptors 1-3, PDGFRα/β, FGFR1/2, TIE2, KIT, RET, and BRAF. This combination is being investigated primarily for refractory/metastatic cancer indications, including colorectal and hepatocellular carcinoma, with interest in combining immune checkpoint inhibition and broad-spectrum tyrosine kinase inhibition. There are ongoing phase trials evaluating its efficacy and safety.

Other names
atezolizumab and regorafenibTecentriq + Stivarga
02

Targets

CD274 (Programmed cell death protein 1 ligand 1)TEK (Tie2)KIT (c-KIT proto-oncogene receptor tyrosine kinase)FGFR1 (Fibroblast growth factor receptor 1)PDGFRB (Platelet-derived growth factor receptor beta)BRAF V600ERAF1 (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)PDGFRA (Platelet-derived growth factor receptor alpha)RET (Rearranged during transfection receptor tyrosine kinase)FGFR2 (Keratinocyte growth factor receptor)

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