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elacytarabine
- Development stage
- Phase 3
- Lead developer
- Clavis Pharma
- Modality
- Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, DNA Intercalators/Alkylators → Nucleic Acid-Directed Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules
- Administration
- Intravenous
01
Overview
Elacytarabine is a lipophilic nucleoside analog and a derivative of cytarabine, developed for the treatment of acute myeloid leukemia (AML). Unlike cytarabine, which requires the human equilibrative nucleoside transporter 1 (hENT1) for cellular uptake, elacytarabine can enter leukemia cells independently of hENT1. This property was intended to overcome resistance in AML patients with low hENT1 expression. Elacytarabine acts as an antimetabolite by incorporating into DNA during replication and inhibiting DNA synthesis, leading to cell death. The drug was developed by Clavis Pharma and underwent clinical trials in relapsed or refractory AML but did not demonstrate significant survival benefit over standard treatments in phase III trials[7][10].
- Brand names
- Elacyt
- Other names
- elacytarabineC18:1(Δ9,trans) unsaturated fatty acid ester of cytarabine
02
Targets
ENT1 (Solute carrier family 29 member 1)DNA polymerase family
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