Drug intelligence / Profile preview

ST316 + fruquintinib

Development stage
Phase 1
Lead developer
Sapience Therapeutics
Modality
Small Molecules, Peptides
Administration
Intravenous, Oral
01

Overview

ST316 + fruquintinib is an experimental combination therapy under clinical investigation primarily for advanced or metastatic colorectal cancer. ST316 is a novel peptide drug that disrupts the interaction of β-catenin with BCL9, leading to inhibition of the Wnt/β-catenin signaling pathway, a pathway known to drive tumor growth, survival, and immune evasion in colorectal cancer. Fruquintinib is a small molecule inhibitor that selectively targets vascular endothelial growth factor receptors 1, 2, and 3 (VEGFR1-3), suppressing tumor angiogenesis and lymphangiogenesis. The rationale for the combination is to block tumor vascularization and modulate the tumor microenvironment while simultaneously inhibiting oncogenic transcriptional activity mediated by aberrant Wnt/β-catenin signaling. Early-phase clinical trials suggest that the combination is under investigation for safety, pharmacodynamics, and antitumor activity, with preliminary evidence of biological activity and tolerability in colorectal cancer[3][4].

02

Targets

VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR2 (Vascular endothelial growth factor receptor 2)VEGFR4 (Vascular endothelial growth factor Receptor-3)BCL9 (B-cell lymphoma 9 protein)CTNNB1 (Beta-catenin)

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