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Drug intelligence / Profile preview
R1498
- Development stage
- Preclinical
- Lead developer
- CROSS-FIELD
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
R1498 is a well-tolerated, orally active small molecule kinase inhibitor developed for the treatment of hepatocellular carcinoma and gastric cancer. Its mechanism of action involves dual targeting of angiogenic and mitotic pathways, primarily by inhibiting Aurora kinases and vascular endothelial growth factor receptor 2 (VEGFR2). R1498 inhibits tumor growth and angiogenesis, demonstrating effectiveness in both in vitro and in vivo xenograft models, with superior efficacy and toxicity profile compared to sorafenib.
02
Targets
AURKA (Aurora kinase A)AURKB (Aurora kinase B)VEGFR2 (Vascular endothelial growth factor receptor 2)AURK (Aurora kinase family)
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