Mechanism of Action: DNA methyltransferase (DNMT) inhibition
Indication: Hematologic Malignancies
How this therapy can help
ASTX727 is a unique fixed-dose combination of the hypomethylating agent decitabine, the active ingredient in Dacogen®, and the novel cytidine deaminase inhibitor, E7727. ASTX727 was designed to deliver decitabine by oral administration. By inhibiting cytidine deaminase, E7727 inhibits the major mechanism by which decitabine is degraded in the gut and liver, and the combination therefore permits the efficient delivery of decitabine orally.
Astex is completing a Phase 1/2 clinical study of ASTX727 in the treatment of intermediate – high risk myelodysplastic syndromes (MDS). Astex also plans to develop a low-dose formulation of ASTX727 for the treatment of chronic conditions where oral delivery of a hypomethylating agent would be preferred. These include low-risk MDS, and in AML maintenance following intensive chemotherapy.
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