Drug intelligence / Profile preview

fruquintinib + capecitabine

Development stage
Unknown
Lead developer
HUTCHMED
Modality
Small Molecules
Administration
Oral
01

Overview

Fruquintinib + capecitabine is a combination therapy being investigated primarily for metastatic colorectal cancer (mCRC). Fruquintinib is a highly selective small molecule tyrosine kinase inhibitor that potently inhibits VEGFR-1, VEGFR-2, and VEGFR-3, which are key regulators of angiogenesis associated with tumor growth and metastasis. It prevents VEGF receptor structural change and dimerization, thereby inhibiting phosphorylation and downstream signaling cascades. Capecitabine is a prodrug that is enzymatically converted to fluorouracil (5-FU) in tumor cells, where it inhibits DNA synthesis and slows tumor growth. This combination has shown promising efficacy and tolerability as maintenance therapy, particularly in RAS/BRAF wild-type metastatic colorectal cancer patients who have achieved disease control after first-line standard chemotherapy.

02

Targets

TS (Thymidylate synthase)VEGFR2 (Vascular endothelial growth factor receptor 2)VEGFR-1 (Vascular endothelial growth factor receptor 1)DNAVEGFR3 (Vascular endothelial growth factor receptor 3)

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