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ximiteinib
- Development stage
- Unknown
- Lead developer
- Shanghai Runshi Pharmaceutical Technology
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Ximiteinib (also known as RS1805 or SIMM1805) is an orally administered small molecule kinase inhibitor that selectively targets the fibroblast growth factor receptors 1, 2, and 3 (FGFR1/2/3). Developed through a collaboration between the Shanghai Institute of Materia Medica (SIMM) and Shanghai Runshi Pharmaceutical, ximiteinib is designed to block the FGFR signaling pathway, which is a key driver in the pathogenesis of various malignancies, including esophageal squamous cell carcinoma (ESCC) and gastric cancer. The drug is currently being evaluated in Phase II clinical trials in China, specifically in combination with irinotecan for patients with advanced ESCC who have failed first-line platinum-based chemoimmunotherapy. Its mechanism involves competitive binding to the ATP-binding site of the FGFR kinase domain, thereby inhibiting receptor autophosphorylation and downstream signaling cascades such as MAPK/ERK and PI3K/AKT.
- Other names
- ximiteinib
02
Targets
VEGFR2 (Vascular endothelial growth factor receptor 2)CSF1R (Macrophage colony-stimulating factor receptor)FGFR3 (Fibroblast growth factor receptor 3)FGFR2 (Keratinocyte growth factor receptor)FGFR1 (Fibroblast growth factor receptor 1)
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