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asp5878
- Development stage
- Phase 1
- Lead developer
- Astellas Pharma
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
ASP5878 is an orally bioavailable, selective small-molecule inhibitor of fibroblast growth factor receptors (FGFRs) 1, 2, 3, and 4. It acts as a pan-FGFR antagonist with potent antineoplastic activity by inhibiting the kinase activity of these receptors. Preclinical studies demonstrated that ASP5878 suppresses cell proliferation in cancer cell lines harboring FGFR3 mutations or fusions and retains efficacy even in chemoresistant models. The drug was developed primarily for the treatment of solid tumors such as urothelial carcinoma and has also been investigated for achondroplasia. Clinical trials included patients with various solid tumors exhibiting FGFR genetic alterations[1][2][3][4][5][6].
- Other names
- FGFR inhibitor ASP5878
02
Targets
FGFR1 (Fibroblast growth factor receptor 1)FGFR2 (Keratinocyte growth factor receptor)FGFR3 (Fibroblast growth factor receptor 3)FGFR4 (Fibroblast growth factor receptor 4)
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