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elenestinib
- Development stage
- Phase 3
- Lead developer
- Sanofi
- Modality
- Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Allosteric Modulators → Classical Binding Small Molecules → Small Molecules, Irreversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules
- Administration
- Oral
01
Overview
Elenestinib is an orally bioavailable, investigational small molecule tyrosine kinase inhibitor that selectively targets the D816V-mutated form of the mast/stem cell factor receptor c-Kit (KIT), a mutation found in nearly all cases of indolent systemic mastocytosis (ISM) and other related mast cell disorders. By binding to and inhibiting KIT D816V, elenestinib reduces abnormal mast cell proliferation and activity, leading to improvements in disease-related symptoms and biomarkers. It is designed with limited central nervous system penetration to minimize CNS side effects. Elenestinib is being developed primarily for ISM but may have potential in other KIT-driven diseases[1][2][3][4][5][6][7][8].
- Other names
- elenestinib phosphate
02
Targets
KIT D816V (Mast/stem cell growth factor receptor Kit D816V mutant)
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