Decitabine.

Article Details

Citation

Daskalakis M, Blagitko-Dorfs N, Hackanson B

Decitabine.

Recent Results Cancer Res. 2010;184:131-57. doi: 10.1007/978-3-642-01222-8_10.

PubMed ID
20072836 [ View in PubMed
]
Abstract

The pyrimidine analogs, 5-azacytidine (azacitidine, Vidaza) and its deoxy derivative, 5-aza-2'-deoxycytidine (decitabine, Dacogen, are the most widely used inhibitors of DNA methylation which trigger demethylation leading to a consecutive reactivation of epigenetically silenced tumor suppressor genes in vitro and in vivo. Although the antileukemic capacity of decitabine has been known for almost 40 years, its therapeutic potential in hematologic malignancies is still under intensive investigation. Multiple clinical trials have shown the promising activity of low-dose decitabine in AML, MDS, CML, and hemoglobinopathies, whereas its efficacy in solid tumors is rather limited.Clinical responses appear to be induced by both epigenetic alterations and the induction of cell-cycle arrest and/or apoptosis. Recent clinical trials have been investigating new dosing schedules, routes of administration, and combination of decitabine with other agents, including histone deacetylase (HDAC) inhibitors.

DrugBank Data that Cites this Article

Drugs
Drug Targets
DrugTargetKindOrganismPharmacological ActionActions
DecitabineDNANucleotideHumans
Yes
Other/unknown
Details
DecitabineDNA (cytosine-5)-methyltransferase 1ProteinHumans
Yes
Inhibitor
Details
Drug Enzymes
DrugEnzymeKindOrganismPharmacological ActionActions
DecitabineCytidine deaminaseProteinHumans
No
Substrate
Details
DecitabineDeoxycytidine kinaseProteinHumans
Yes
Substrate
Details