Drug intelligence / Profile preview

TKI + anti-PD-1 antibody-China Medical University, China-colorectal adenocarcinoma

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

Overview

This combination therapy refers to a Phase II clinical trial regimen (NCT04716634) led by China Medical University for patients with microsatellite stable/mismatch repair proficient (MSS/pMMR) metastatic colorectal adenocarcinoma. The study evaluates the efficacy and safety of combining a tyrosine kinase inhibitor (TKI)—specifically either fruquintinib or regorafenib—with the anti-PD-1 monoclonal antibody toripalimab. Fruquintinib is a highly selective inhibitor of VEGFR1, 2, and 3, while regorafenib is a multi-kinase inhibitor targeting VEGFRs, TIE2, PDGFR, FGFR, KIT, RET, and RAF. Toripalimab is a biologic that blocks the PD-1 receptor, facilitating an anti-tumor immune response. This combination is particularly aimed at overcoming the resistance of MSS/pMMR colorectal cancers to standard immunotherapy by leveraging the immunomodulatory effects of anti-angiogenic TKIs to create a more favorable tumor microenvironment.

Brand names
ElunateStivargaTuoyi
Other names
fruquintinib + toripalimabregorafenib + toripalimabTKI + anti-PD-1 antibody
02

Targets

TEK (Tie2)ARAF (Proto-oncogene serine/threonine-protein kinase A-Raf)VEGFR2 (Vascular endothelial growth factor receptor 2)PDCD1 (Programmed cell death protein 1 receptor)PDGFR (PDGFR family)FGFR (Fibroblast growth factor receptor)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR3 (Vascular endothelial growth factor receptor 3)KIT (c-KIT proto-oncogene receptor tyrosine kinase)RET (Rearranged during transfection receptor tyrosine kinase)

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