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derazantinib
- Development stage
- Phase 2
- Lead developer
- Basilea Pharmaceutica
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Derazantinib is an investigational oral small molecule multi-kinase inhibitor that preferentially targets fibroblast growth factor receptors FGFR1, FGFR2, and FGFR3. It also inhibits colony stimulating factor-1 receptor (CSF1R) and vascular endothelial growth factor receptor 2 (VEGFR2). Derazantinib is being developed primarily for the treatment of intrahepatic cholangiocarcinoma (iCCA) with FGFR2 gene fusions, mutations or amplifications. The drug has demonstrated clinically meaningful efficacy in patients with iCCA harboring these genetic alterations and has a manageable safety profile. Additional studies are ongoing in other cancers such as gastric cancer and urogenital cancers[2][3][7].
- Other names
- derazantinib hydrochloride
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)RET (Rearranged during transfection receptor tyrosine kinase)
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