Drug intelligence / Profile preview

regorafenib + toripalimab

Development stage
Unknown
Lead developer
Hengrui Pharmaceutical
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Oral, Intravenous
01

Overview

Regorafenib + toripalimab is an investigational combination therapy consisting of regorafenib, a small molecule multi-kinase inhibitor, and toripalimab, a monoclonal antibody targeting programmed cell death protein 1 (PD-1). Regorafenib inhibits multiple tyrosine kinases involved in tumor angiogenesis (such as VEGFR1-3), oncogenesis (including KIT, RET, RAF), and the tumor microenvironment (such as CSF1R and TIE2), thereby reducing tumor growth and modulating immune suppression. Toripalimab is an immune checkpoint inhibitor that blocks PD-1 on T cells to enhance anti-tumor immunity. The combination aims to synergistically improve anti-tumor efficacy by both directly inhibiting cancer cell proliferation/angiogenesis and enhancing the host immune response against tumors. This regimen has been primarily studied in patients with advanced or metastatic microsatellite stable colorectal cancer who have failed standard therapies[1][8]. Early-phase clinical trials suggest modest objective response rates with manageable toxicity profiles.

02

Targets

ABL1 (ABL proto-oncogene 1, non-receptor tyrosine kinase)FGFR2 (Keratinocyte growth factor receptor)BRAF (B-Raf proto-oncogene, serine/threonine kinase)VEGFR4 (Vascular endothelial growth factor Receptor-3)RET (Rearranged during transfection receptor tyrosine kinase)PDGFRA (Platelet-derived growth factor receptor alpha)VEGFR2 (Vascular endothelial growth factor receptor 2)PDCD1 (Programmed cell death protein 1 receptor)FGFR1 (Fibroblast growth factor receptor 1)EPHA2 (Ephrin type-A receptor 2)DDR2 (Discoidin domain receptor tyrosine kinase 2)RAF1 (c-Raf-1 (Y340D/Y341D))MAPK14 (p38 mitogen-activated protein kinase alpha)KIT (c-KIT proto-oncogene receptor tyrosine kinase)CSF1R (Macrophage colony-stimulating factor receptor)PDGFRB (Platelet-derived growth factor receptor beta)NTRK1 (Tropomyosin-related receptor kinase A)VEGFR-1 (Vascular endothelial growth factor receptor 1)TEK (Angiopoietin-1 receptor)

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