Demethylation agents

Oxford American handbook of oncology. Second Edition. Oxford University Press (2015)


Methylation of DNA by DNA methyltransferase can suppress the transcription of tumor suppressor genes. By inhibiting DNA methyltransferase in a malignant cell, innate tumor suppressor activity can be restored. Active hypomethylating agents include the following.

Azacitidine (Vidaza)

  • Mechanism: cytosine analog that is incorporated into DNA and rNA, irreversibly inhibiting DNA methyltransferase
  • Route: intravenous
  • Uses: myelodysplastic syndromes, acute myelogenous leukemia
  • Notes: causes myelosuppression

Decitabine (Dacogen)

  • Mechanism: deoxyribose form of azacitidine, a cytosine analog that incorporates into DNA only, irreversibly inhibits DNA methyltransferase
  • Route: intravenous
  • Uses: myelodysplastic syndromes, acute myelogenous leukemia
  • Notes: causes myelosuppression
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