What are DNA methyltransferase inhibitor drugs?

DNA methyltransferase inhibitor drugs are pharmacologic agents that share a common mechanism (typically targeting DNA methyltransferase (DNMT)). 4 are currently marketed, with 5 more in clinical development.

What are the marketed DNA methyltransferase inhibitor drugs?

Marketed DNA methyltransferase inhibitor drugs include Azacitidine (AZA), decitabine injection, Azacytidine, HAG Regimen, Azacitidine Injection.

DNA methyltransferase inhibitor

Name: Drug Landscape Pharmaceutical Database
Creator: Drug Landscape
Published: 2026-01-01
License: https://creativecommons.org/licenses/by/4.0/

4 marketed 3 in Phase 3 2 in Phase 2

This page covers all DNA methyltransferase inhibitor drugs tracked by Drug Landscape: marketed products and active clinical-stage compounds, targeting DNA methyltransferase (DNMT), DNA methyltransferase, DNA methyltransferase, DNA.

Targets

DNA methyltransferase (DNMT) · DNA methyltransferase · DNA methyltransferase, DNA

Marketed (4)

Azacitidine (AZA) · Memorial Sloan Kettering Cancer Center · Oncology
Azacitidine inhibits DNA methyltransferase, leading to DNA demethylation and reactivation of silenced tumor suppressor genes.
decitabine injection · Janssen Korea, Ltd., Korea · Oncology
Decitabine is a DNA methyltransferase inhibitor that reduces DNA methylation, reactivating silenced tumor suppressor genes and promoting differentiation and apoptosis in myelodysplastic cells.
Azacytidine, HAG Regimen · Shenzhen Second People's Hospital · Oncology
Azacytidine is a DNA methyltransferase inhibitor that demethylates DNA and promotes differentiation of myelodysplastic cells.
Azacitidine Injection · Ascentage Pharma Group Inc. · Oncology
Azacitidine is a DNA methyltransferase inhibitor that causes hypomethylation of DNA and promotes differentiation and apoptosis of abnormal hematopoietic cells.

Phase 3 pipeline (3)

5-Azacytidin · Technische Universität Dresden · Oncology
5-Azacytidine is a DNA methyltransferase inhibitor that reduces DNA methylation and promotes re-expression of silenced tumor suppressor genes.
Decitabine/Cedazuridine · Astex Pharmaceuticals, Inc. · Oncology
Decitabine is a DNA methyltransferase inhibitor that causes hypomethylation of DNA, leading to reactivation of silenced tumor suppressor genes and differentiation of myelodysplastic cells.
Dacogen (decitabine) only · Eisai Inc. · Oncology
Decitabine is a DNA methyltransferase inhibitor that reduces DNA methylation, reactivating silenced tumor suppressor genes and promoting differentiation and apoptosis in myelodysplastic cells.

Phase 2 pipeline (2)

Azacitidine associated with Lenalidomide · Assistance Publique - Hôpitaux de Paris · Oncology
Azacitidine is a DNA methyltransferase inhibitor.
Azacitidine associated with Idarubicine · Assistance Publique - Hôpitaux de Paris · Oncology
Azacitidine is a DNA methyltransferase inhibitor, and Idarubicin is an anthracycline antibiotic that intercalates DNA.

Patent intelligence

dna methyltransferase inhibitor patent landscape — aggregated cliff calendar, attackable patents, originator estates