Drug intelligence / Profile preview

fruquintinib + immune checkpoint inhibitor + trifluridine + tipiracil + bevacizumab

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

Overview

This drug combination is an investigational multi-agent regimen being evaluated for the treatment of metastatic colorectal cancer (mCRC), particularly in patients who have progressed after second-line standard therapies. The regimen consists of **fruquintinib**, a highly selective oral tyrosine kinase inhibitor of VEGFR 1, 2, and 3; an **immune checkpoint inhibitor** (typically targeting the PD-1/PD-L1 pathway); **trifluridine/tipiracil** (TAS-102), an oral cytotoxic chemotherapy; and **bevacizumab**, a monoclonal antibody that targets VEGF-A. The rationale behind this combination is to leverage the synergistic effects of anti-angiogenesis (via fruquintinib and bevacizumab) and cytotoxic chemotherapy (TAS-102) to modulate the tumor microenvironment, potentially converting 'cold' microsatellite stable (MSS) tumors into 'hot' tumors that are more responsive to immune checkpoint blockade. This specific regimen is being studied in a Phase Ib/II clinical trial sponsored by the Tianjin Medical University Cancer Institute and Hospital.

Brand names
Lonsurf
Other names
Fruquintinib + Checkpoint Inhibitor + TAS-102 + BevacizumabFruquintinib + PD-1 inhibitor + Trifluridine/Tipiracil + Bevacizumab
02

Targets

VEGFR2 (Vascular endothelial growth factor receptor 2)PDCD1 (Programmed cell death protein 1 receptor)TS (Thymidylate synthase)TYMP (Thymidine phosphorylase)VEGFA (Vascular endothelial growth factor A)DNAVEGFR3 (Vascular endothelial growth factor receptor 3)VEGFR-1 (Vascular endothelial growth factor receptor 1)

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