Drug intelligence / Profile preview

capecitabine + chiauranib

Development stage
Discontinued
Lead developer
Akeso
Modality
Small Molecules
Administration
Oral
01

Overview

A combination therapy of capecitabine and chiauranib being investigated for the treatment of advanced triple-negative breast cancer (TNBC) that has failed prior anthracyclines and taxanes therapy. Capecitabine is a fluoropyrimidine carbamate prodrug that is converted to 5-fluorouracil (5-FU) by enzymes expressed in higher concentrations in tumors. Chiauranib is a novel multi-targeted kinase inhibitor that simultaneously inhibits angiogenesis-related kinases (VEGFR2, VEGFR1, VEGFR3, PDGFRa, and c-Kit), mitosis-related kinase Aurora B, and chronic inflammation-related kinase CSF-1R.

02

Targets

AURKB (Aurora kinase B)CSF1R (Macrophage colony-stimulating factor receptor)PDGFRA (Platelet-derived growth factor receptor alpha)TS (Thymidylate synthase)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)DDR1 (Discoidin domain receptor 1)

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