Drug intelligence / Profile preview

serplulimab + regorafenib

Development stage
Unknown
Lead developer
Henlius
Modality
Small Molecules
Administration
Intravenous
01

Overview

The combination of serplulimab and regorafenib is a novel therapeutic approach being investigated for colorectal cancer, primarily in patients with liver metastases. It combines serplulimab, a fully humanized anti-PD-1 monoclonal antibody with a unique binding mechanism that induces robust PD-1 receptor endocytosis, with regorafenib, a small-molecule multikinase inhibitor targeting pathways involved in tumor angiogenesis, oncogenesis, and the tumor microenvironment. This dual approach aims to enhance efficacy by simultaneously targeting immune evasion mechanisms and tumor cell signaling pathways. Serplulimab is approved in China and has a positive opinion from the EMA for small cell lung cancer. Regorafenib is approved in China as a third-line treatment for metastatic colorectal cancer.

02

Targets

PDGFRB (Platelet-derived growth factor receptor beta)KIT (c-KIT proto-oncogene receptor tyrosine kinase)TEK (Tie2)PDCD1 (Programmed cell death protein 1 receptor)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)FGFR1 (Fibroblast growth factor receptor 1)RET (Rearranged during transfection receptor tyrosine kinase)

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