Drug intelligence / Profile preview

regorafenib + toripalimab

Development stage
Phase 2
Lead developer
Hengrui Therapeutics
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)BRAF (B-Raf proto-oncogene, serine/threonine kinase)CSF1R (Macrophage colony-stimulating factor receptor)DDR2 (Discoidin domain receptor tyrosine kinase 2)EPHA2 (Ephrin type-A receptor 2)FGFR1 (Fibroblast growth factor receptor 1)FGFR2 (Keratinocyte growth factor receptor)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR4 (Vascular endothelial growth factor Receptor-3)VEGFR2 (Vascular endothelial growth factor receptor 2)KIT (c-KIT proto-oncogene receptor tyrosine kinase)MAPK14 (p38 mitogen-activated protein kinase alpha)NTRK1 (Tropomyosin-related receptor kinase A)PDCD1 (Programmed cell death protein 1 receptor)PDGFRA (Platelet-derived growth factor receptor alpha)PDGFRB (Platelet-derived growth factor receptor beta)RAF1 (c-Raf-1 (Y340D/Y341D))RET (Rearranged during transfection receptor tyrosine kinase)TEK (Angiopoietin-1 receptor)TEK (Tie2)

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