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Elacytarabine + idarubicin
- Development stage
- Unknown
- 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
- Administration
- Intravenous
01
Overview
Elacytarabine + idarubicin is a combination therapy investigated for the treatment of relapsed or refractory acute myeloid leukemia (AML). Elacytarabine is a novel lipophilic nucleoside analogue and an elaidic acid ester derivative of cytarabine. It was designed to overcome resistance mechanisms associated with standard cytarabine therapy by enabling cell entry independent of the human equilibrative nucleoside transporter 1 (hENT1) and resisting deactivation by cytidine deaminase. Once inside cells, elacytarabine is metabolized to cytarabine and inhibits both DNA and RNA synthesis, leading to cell death[6][8]. Idarubicin is an anthracycline antineoplastic agent that intercalates into DNA and inhibits topoisomerase II activity, preventing DNA replication and repair[1]. The combination has shown clinical activity in patients with refractory AML in early-phase trials[3][7].
- Brand names
- ELACYT
- Other names
- 5′-elaidic acid derivative of cytarabineelaidic acid ester of cytarabine
02
Targets
DNA polymerase familyDNATOP2A (DNA topoisomerase II)TOP2B (DNA topoisomerase II beta)
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