Decitabine
M Daskalakis, N Blagitko-Dorfs… - Small Molecules in …, 2009 - Springer
M Daskalakis, N Blagitko-Dorfs, B Hackanson
Small Molecules in Oncology, 2009•SpringerAbstract 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 …
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 …
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.
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