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5-Azacytidin

Technische Universität Dresden · Phase 3 active Small molecule

5-Azacytidine is a DNA methyltransferase inhibitor that reduces DNA methylation and promotes re-expression of silenced tumor suppressor genes.

5-Azacytidine is a DNA methyltransferase inhibitor that reduces DNA methylation and promotes re-expression of silenced tumor suppressor genes. Used for Myelodysplastic syndromes, Acute myeloid leukemia.

At a glance

Generic name5-Azacytidin
SponsorTechnische Universität Dresden
Drug classDNA methyltransferase inhibitor
TargetDNA methyltransferase (DNMT)
ModalitySmall molecule
Therapeutic areaOncology
PhasePhase 3

Mechanism of action

5-Azacytidine is a cytidine analog that incorporates into DNA during replication and inhibits DNA methyltransferase (DNMT) activity, leading to hypomethylation of CpG islands. This reactivates epigenetically silenced genes, including tumor suppressors, and can induce differentiation and apoptosis in myelodysplastic and other cancer cells. It also has immunomodulatory effects that enhance anti-tumor immunity.

Approved indications

Common side effects

Key clinical trials

Primary sources

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SourceUsed for
ClinicalTrials.govTrial enrolment, design, endpoints, results