Decitabine

Decitabine
Clinical data
Trade names Dacogen
AHFS/Drugs.com Monograph
MedlinePlus a608009
Pregnancy
category
  • D
Routes of
administration		 Intravenous
ATC code L01BC08 (WHO)
Legal status
Legal status
  • ℞ (Prescription only)
Pharmacokinetic data
Protein binding <1%
Biological half-life 30 minutes
Identifiers
CAS Number 2353-33-5 YesY
PubChem (CID) 451668
IUPHAR/BPS 6805
DrugBank DB01262 YesY
ChemSpider 397844 YesY
UNII 776B62CQ27 YesY
KEGG D03665 YesY
ChEBI CHEBI:50131 YesY
ChEMBL CHEMBL1201129 N
ECHA InfoCard 100.017.355
Chemical and physical data
Formula C8H12N4O4
Molar mass 228.206 g/mol
3D model (Jmol) Interactive image
 NYesY (what is this?)  (verify)

Decitabine (trade name Dacogen), or 5-aza-2'-deoxycytidine, acts as an Nucleic Acid Synthesis Inhibitor.[1] It is a drug for the treatment of myelodysplastic syndromes, a class of conditions where certain blood cells are dysfunctional, and for acute myeloid leukemia (AML).[2] Chemically, it is a cytidine analog.

Mechanism

Decitabine is a hypomethylating agent.[3][4] It hypomethylates DNA by inhibiting DNA methyltransferase.

It functions in a similar manner to azacitidine, although decitabine can only be incorporated into DNA strands while azacitidine can be incorporated into both DNA and RNA chains.

Clinical uses

Decitabine is indicated for the treatment of myelodysplastic syndromes (MDS) including previously treated and untreated, de novo and secondary MDS of all French-American-British subtypes (refractory anemia, refractory anemia with ringed sideroblasts, refractory anemia with excess blasts, refractory anemia with excess blasts in transformation, and chronic myelomonocytic leukemia) and Intermediate-1, Intermediate-2, and High-Risk International Prognostic Scoring System groups. In patients with renal insufficiency, Batty and colleagues reported the first case series on the feasibility of therapy with hypomethylating agents in patients with renal insufficiency.[5]

It also has EU approval for acute myeloid leukemia (AML).[2]

References

  1. ↑ "Decitabine". National Center for Biotechnology Information. Retrieved September 24, 2016.
  2. 1 2 "EC Approves Marketing Authorization Of DACOGEN For Acute Myeloid Leukemia". 2012-09-28. Retrieved 28 September 2012.
  3. ↑ Kantarjian H, Issa JP, Rosenfeld CS, et al. (April 2006). "Decitabine improves patient outcomes in myelodysplastic syndromes: results of a phase III randomized study". Cancer. 106 (8): 1794–1803. doi:10.1002/cncr.21792. PMID 16532500.
  4. ↑ Kantarjian HM, O'Brien S, Cortes J, et al. (August 2003). "Results of decitabine (5-aza-2'deoxycytidine) therapy in 130 patients with chronic myelogenous leukemia". Cancer. 98 (3): 522–528. doi:10.1002/cncr.11543. PMID 12879469.
  5. ↑ Ravandi, F.; Kantarjian, J. E.; Issa, S.; Jabbour, S.; Santos, G.; McCue, D.; Garcia-Manero, F. P. S.; Pierce, E.; O'Brien, J. P.; Cortés, J. E.; Ravandi, F. (2010). "Feasibility of Therapy with Hypomethylating Agents in Patients with Renal Insufficiency". Clinical Lymphoma, Myeloma & Leukemia. 10 (3): 205–210. doi:10.3816/CLML.2010.n.032. PMC 3726276Freely accessible. PMID 20511166.

Further reading


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