Drug intelligence / Profile preview

ADG126 + pembrolizumab + fruquintinib

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

Overview

This is a **triple combination regimen** consisting of ADG126, pembrolizumab, and fruquintinib for the investigational treatment of cancer. - **ADG126** is a monoclonal antibody that targets transforming growth factor-beta receptor II (TGF-βRII), acting as a TGF-beta pathway antagonist. Developed by Adagene, it is designed to modulate the tumor microenvironment and enhance anti-tumor immune responses by inhibiting immunosuppressive TGF-beta signaling. - **Pembrolizumab** is a humanized monoclonal IgG4 antibody that targets the programmed cell death protein 1 (PD-1) receptor on T cells, blocking its interaction with PD-L1 and PD-L2, thereby releasing an immune checkpoint and enhancing the immune response against tumor cells[1][3][5]. - **Fruquintinib** is a small molecule inhibitor of vascular endothelial growth factor receptors (VEGFR) 1, 2, and 3, which suppresses angiogenesis, starving tumors of vascular supply[2][4][6]. Fruquintinib is approved for metastatic colorectal cancer after standard therapies[4][2][6]. This combination is being explored primarily for synergistic immuno-oncology effects in advanced or refractory solid tumors where TGF-beta pathway activation, immune checkpoint engagement, and angiogenesis all contribute to tumor escape and progression.

02

Targets

VEGFR2 (Vascular endothelial growth factor receptor 2)PDCD1 (Programmed cell death protein 1 receptor)CTLA-4 (Cytotoxic t-lymphocyte–associated protein 4)VEGFR3 (Vascular endothelial growth factor receptor 3)VEGFR-1 (Vascular endothelial growth factor receptor 1)

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