Pharmacokinetic and pharmacodynamic analysis of 5-aza-2'-deoxycytidine (decitabine) in the design of its dose-schedule for cancer therapy

M Karahoca, RL Momparler - Clinical epigenetics, 2013 - Springer
Aza-2′-deoxycytidine (5-AZA-CdR, decitabine), an epigenetic drug that inhibits DNA
methylation, is currently used to treat myelodysplastic syndrome (MDS), and is under …

Epigenetic therapy of cancer with 5-aza-2′-deoxycytidine (decitabine)

RL Momparler - Seminars in oncology, 2005 - Elsevier
Epigenetic events, such as aberrant DNA methylation, have been demonstrated to silence
the expression of many genes that suppress malignancy. Since the event is reversible, it is …

Phase 1 study of low-dose prolonged exposure schedules of the hypomethylating agent 5-aza-2′-deoxycytidine (decitabine) in hematopoietic malignancies

JPJ Issa, G Garcia-Manero, FJ Giles, R Mannari… - Blood, 2004 - ashpublications.org
Abstract Decitabine (5-aza-2′-deoxycytidine) inhibits DNA methylation and has dual effects
on neoplastic cells, including the reactivation of silenced genes and differentiation at low …

Pharmacology of 5-Aza-2′-deoxycytidine (decitabine)

RL Momparler - Seminars in hematology, 2005 - Elsevier
The preclinical pharmacology of 5-aza-2′-deoxycytidine (decitabine, 5AZA-CdR) is
reviewed. 5AZA-CdR, an analogue of deoxycytidine, is a prodrug that requires metabolic …

Evolution of decitabine development: accomplishments, ongoing investigations, and future strategies

E Jabbour, JP Issa, G Garcia‐Manero… - … Journal of the …, 2008 - Wiley Online Library
Abstract Decitabine (5‐aza‐2′‐deoxycytidine) is a hypomethylating agent with a dual
mechanism of action: reactivation of silenced genes and differentiation at low doses, and …

Pharmacological approach for optimization of the dose schedule of 5-Aza-2'-deoxycytidine (Decitabine) for the therapy of leukemia

RL Momparler, S Cote, N Eliopoulos - Leukemia, 1997 - nature.com
Aza-2′-deoxycytidine (5-Aza-CdR; Decitabine) is an active antineoplastic agent in patients
with leukemia. Since 5-Aza-CdR is an S phase specific agent and has a short plasma half …

Evaluation of a 7-day continuous intravenous infusion of decitabine: inhibition of promoter-specific and global genomic DNA methylation

WE Samlowski, SA Leachman, M Wade… - Journal of Clinical …, 2005 - ascopubs.org
Purpose The nucleoside analog 5-aza-2′-deoxycytidine (5-aza-CdR, decitabine) is a
potent inhibitor of DNA methylation in vitro. Cellular treatment with this agent induces the re …

Importance of dose-schedule of 5-aza-2'-deoxycytidine for epigenetic therapy of cancer

M Lemaire, GG Chabot, NJM Raynal, LF Momparler… - BMC cancer, 2008 - Springer
Background The inactivation of tumor suppressor genes (TSGs) by aberrant DNA
methylation plays an important role in the development of malignancy. Since this epigenetic …

Delivery of 5-aza-2′-deoxycytidine to cells using oligodeoxynucleotides

CB Yoo, S Jeong, G Egger, G Liang, P Phiasivongsa… - Cancer research, 2007 - AACR
The major goal of epigenetic therapy is to reverse aberrant promoter hypermethylation and
restore normal function of tumor suppressor genes by the use of chromatin-modifying drugs …

Decitabine

M Daskalakis, N Blagitko-Dorfs… - Small Molecules in …, 2009 - Springer
Abstract The pyrimidine analogs, 5-azacytidine (azacitidine, Vidaza®) and its deoxy
derivative, 5-aza-2'-deoxycytidine (decitabine, Dacogen®), are the most widely used …