Drug intelligence / Profile preview

regorafenib + vudalimab

Development stage
Unknown
Lead developer
Bayer
Modality
Bispecific Antibodies → Multispecific Antibodies → Engineered Antibody Formats → Antibody-Based Therapeutics, Small Molecules
Administration
Oral (regorafenib), Intravenous (vudalimab)
01

Overview

Regorafenib + vudalimab is an investigational **combination therapy** under clinical evaluation for the treatment of advanced or metastatic solid tumors, including colorectal cancer. **Regorafenib** is a small molecule multi-kinase inhibitor targeting angiogenic (VEGFR1-3), oncogenic (KIT, RET, RAF), and stromal (PDGFR, FGFR, CSF1R) receptor tyrosine kinases, inhibiting tumor angiogenesis and proliferation. **Vudalimab** (XmAb20717) is a bispecific monoclonal antibody targeting **programmed cell death protein 1 (PD-1)** and **cytotoxic T-lymphocyte–associated antigen 4 (CTLA-4)**, functioning as a dual immune checkpoint inhibitor to potentiate T cell–mediated anti-tumor responses. The combination is being studied primarily in advanced **colorectal cancer**, including stage II–IV and metastatic setting, aiming to enhance immune checkpoint blockade and anti-angiogenic activity synergistically for improved clinical outcomes[3][6]. Regorafenib is developed and marketed by Bayer, whereas vudalimab is developed by Xencor.

Brand names
Stivarga (for regorafenib)
Other names
regorafenib + XmAb20717
02

Targets

PDCD1 (Programmed cell death protein 1 receptor)KIT (c-KIT proto-oncogene receptor tyrosine kinase)VEGFR2 (Vascular endothelial growth factor receptor 2)FGFR1 (Fibroblast growth factor receptor 1)BRAF (B-Raf proto-oncogene, serine/threonine kinase)PDGFRB (Platelet-derived growth factor receptor beta)CTLA-4 (Cytotoxic t-lymphocyte–associated protein 4)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR3 (Vascular endothelial growth factor receptor 3)PDGFRA (Platelet-derived growth factor receptor alpha)RET (Rearranged during transfection receptor tyrosine kinase)

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