Drug intelligence / Profile preview

muzastotug + pembrolizumab + fruquintinib

Development stage
Phase 2
Lead developer
Adagene
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Intravenous, Oral
01

Overview

muzastotug + pembrolizumab + fruquintinib is an investigational triple combination regimen being evaluated for the treatment of late-line, microsatellite-stable (MSS) metastatic colorectal cancer (CRC). The regimen combines muzastotug (ADG126), a masked anti-CTLA-4 IgG1 monoclonal antibody developed by Adagene; pembrolizumab (Keytruda), an anti-PD-1 monoclonal antibody developed by Merck & Co.; and fruquintinib (Fruzaqla), an oral small molecule inhibitor of VEGFR-1, -2, and -3 developed by HUTCHMED and Takeda. Muzastotug is designed for tumor-selective activation via protease-mediated cleavage in the tumor microenvironment, which widens its therapeutic index, partially blocks CTLA-4 signaling, and selectively depletes intratumoral regulatory T cells (Tregs). The combination of CTLA-4 and PD-1 checkpoint inhibition with the anti-angiogenic effects of fruquintinib is intended to provide synergistic anti-tumor activity, particularly in patients with liver metastases. The triplet is being evaluated in the Phase 1b/2 clinical trial NCT05405595.

Other names
ADG126 + Keytruda + FruzaqlaADG126 + Pembro + FruqADG126 + pembrolizumab + fruqADG126 + pembrolizumab + fruquintinibmuzastotug + Keytruda + Fruzaqlamuzastotug + pembrolizumab + fruq
02

Targets

CTLA-4 (Cytotoxic t-lymphocyte–associated protein 4)FGFR1 (Fibroblast growth factor receptor 1)PDCD1 (Programmed cell death protein 1 receptor)RET (Rearranged during transfection receptor tyrosine kinase)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR2 (Vascular endothelial growth factor receptor 2)VEGFR4 (Vascular endothelial growth factor Receptor-3)KIT (c-KIT proto-oncogene receptor tyrosine kinase)

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