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Details

Stereochemistry ABSOLUTE
Molecular Formula C8H12N4O4
Molecular Weight 228.2056
Optical Activity UNSPECIFIED
Defined Stereocenters 3 / 3
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of DECITABINE

SMILES

C1[C@@]([H])([C@@]([H])(CO)O[C@@]1([H])n2cnc(=N)nc2O)O

InChI

InChIKey=XAUDJQYHKZQPEU-KVQBGUIXSA-N
InChI=1S/C8H12N4O4/c9-7-10-3-12(8(15)11-7)6-1-4(14)5(2-13)16-6/h3-6,13-14H,1-2H2,(H2,9,11,15)/t4-,5+,6+/m0/s1

HIDE SMILES / InChI

Description
Curator's Comment:: description was created based on several sources, including http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/021790s018lbl.pdf, www.ncbi.nlm.nih.gov/pubmed/20501800

Decitabine was first synthesized by Pliml and Sorm in the Institute of Organic Chemistry, Czechoslovak Academy of Sciences in 1964. Later, the drug was approved by FDA for the treatment of myelodysplastic syndromes in patients with cancer. Upon administration the decitabine is metabolized to the active phosphorylated metabolite which is incorporated into DNA and thus inhibits DNA methyltransferase (decitabine deplete DNMT1).

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
Target ID: CHEMBL1993
Sources: www.ncbi.nlm.nih.gov/pubmed/20501800
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
DACOGEN

Approved Use

Dacogen is a nucleoside metabolic inhibitor indicated for treatment of patients with 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.

Launch Date

1.14652794E12
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
73.8 ng/mL
15 mg/m² steady-state, intravenous
dose: 15 mg/m²
route of administration: Intravenous
experiment type: STEADY-STATE
co-administered:
DECITABINE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
163 ng × h/mL
15 mg/m² steady-state, intravenous
dose: 15 mg/m²
route of administration: Intravenous
experiment type: STEADY-STATE
co-administered:
DECITABINE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
0.62 h
15 mg/m² steady-state, intravenous
dose: 15 mg/m²
route of administration: Intravenous
experiment type: STEADY-STATE
co-administered:
DECITABINE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
99%
DECITABINE plasma
Homo sapiens
population: UNKNOWN
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
100 mg/m2 2 times / day steady, intravenous
Highest studied dose
Dose: 100 mg/m2, 2 times / day
Route: intravenous
Route: steady
Dose: 100 mg/m2, 2 times / day
Sources:
unhealthy, 52 years (range: 23 - 78 years)
n = 13
Health Status: unhealthy
Condition: chronic myelogenous leukemia (CML)
Age Group: 52 years (range: 23 - 78 years)
Sex: M+F
Population Size: 13
Sources:
20 mg/m2 1 times / day steady, intravenous
Recommended|MTD
Dose: 20 mg/m2, 1 times / day
Route: intravenous
Route: steady
Dose: 20 mg/m2, 1 times / day
Sources:
unhealthy, 59 years (range: 42–79 years)
n = 6
Health Status: unhealthy
Condition: unresectable liver-predominant metastases
Age Group: 59 years (range: 42–79 years)
Sex: M+F
Population Size: 6
Sources:
Other AEs: Anaemia, Lymphopenia...
Other AEs:
Anaemia (grade 1, 17%)
Lymphopenia (grade 2, 17%)
Neutropenia (grade 2, 17%)
Leucopenia (grade 1, 17%)
Thrombocytopaenia (grade 1, 17%)
Sources:
15 mg/m2 1 times / day steady, intravenous
Dose: 15 mg/m2, 1 times / day
Route: intravenous
Route: steady
Dose: 15 mg/m2, 1 times / day
Sources:
unhealthy, 61 years (range: 32–82 years)
n = 16
Health Status: unhealthy
Condition: CLL
Age Group: 61 years (range: 32–82 years)
Sex: M+F
Population Size: 16
Sources:
DLT: Hyperbilirubinemia, Thrombocytopenia...
Dose limiting toxicities:
Hyperbilirubinemia (grade 3, 2 patients)
Thrombocytopenia (2 patients)
Sources:
20 mg/m2 1 times / day multiple, subcutaneous
Dose: 20 mg/m2, 1 times / day
Route: subcutaneous
Route: multiple
Dose: 20 mg/m2, 1 times / day
Sources:
unhealthy, 65 years
n = 14
Health Status: unhealthy
Condition: myelodysplastic syndrome
Age Group: 65 years
Sex: M+F
Population Size: 14
Sources:
15 mg/m2 3 times / day steady, intravenous
Recommended
Dose: 15 mg/m2, 3 times / day
Route: intravenous
Route: steady
Dose: 15 mg/m2, 3 times / day
Sources:
unhealthy, 70 years (range: 65-76 years)
n = 81
Health Status: unhealthy
Condition: myelodysplastic syndromes
Age Group: 70 years (range: 65-76 years)
Sex: M+F
Population Size: 81
Sources:
Disc. AE: Anemia, Neutropenia...
Other AEs: Neutropenia, Thrombocytopenia...
AEs leading to
discontinuation/dose reduction:
Anemia (grade 5, 6 patients)
Neutropenia (grade 5, 6 patients)
Thrombocytopenia (grade 5, 6 patients)
Other AEs:
Neutropenia (grade 3-4, 87%)
Thrombocytopenia (grade 3-4, 85%)
Febrile neutropenia (grade 3-4, 23%)
Leukopenia (grade 3-4, 22%)
Sources:
15 mg/m2 1 times / day steady, intravenous
Dose: 15 mg/m2, 1 times / day
Route: intravenous
Route: steady
Dose: 15 mg/m2, 1 times / day
Sources:
unhealthy, 72 years (range: 68–75 years)
n = 4
Health Status: unhealthy
Condition: NHL
Age Group: 72 years (range: 68–75 years)
Sex: M+F
Population Size: 4
Sources:
DLT: Febrile neutropenia...
Dose limiting toxicities:
Febrile neutropenia (grade 3-4, 2 patients)
Sources:
660 mg/m2 single, intravenous
Highest studied dose
Dose: 660 mg/m2
Route: intravenous
Route: single
Dose: 660 mg/m2
Sources:
unhealthy
n = 7
Health Status: unhealthy
Condition: chronic myelogenous leukemia
Population Size: 7
Sources:
15 mg/m2 3 times / day steady, intravenous
Recommended
Dose: 15 mg/m2, 3 times / day
Route: intravenous
Route: steady
Dose: 15 mg/m2, 3 times / day
Sources: Page: p. 82
unhealthy
n = 83
Health Status: unhealthy
Population Size: 83
Sources: Page: p. 82
Other AEs: Neutropenia, Thrombocytopenia...
Other AEs:
Neutropenia (all grades, 83%)
Thrombocytopenia (all grades, 81%)
Anemia (all grades, 54%)
Splenomegaly (all grades, 2%)
Thrombocythaemia (all grades, 4%)
Tachycardia (all grades, 1%)
Pulmonary edema (all grades, 1%)
Nausea (all grades, 22%)
Constipation (all grades, 8%)
Diarrhea (all grades, 16%)
Vomiting (all grades, 8%)
Abdominal pain (all grades, 4%)
Oral mucosal petechiae (all grades, 5%)
Stomatitis (all grades, 7%)
Loose stools (all grades, 2%)
Tongue ulceration (all grades, 5%)
Dysphagia (all grades, 2%)
Pyrexia (all grades, 16%)
Fatigue (all grades, 18%)
Asthenia (all grades, 4%)
Fall (all grades, 1%)
Hyperbilirubinaemia (all grades, 4%)
Hepatomegaly (all grades, 1%)
Cellulitis (all grades, 2%)
Urinary tract infection (all grades, 1%)
Alanine aminotransferase increased (all grades, 1%)
Aspartate aminotransferase increased (all grades, 1%)
Alkaline phosphatase increased (all grades, 1%)
Hypocalcemia (all grades, 7%)
Hypoalbuminemia (all grades, 7%)
Hypomagnesaemia (all grades, 2%)
Hypokalemia (all grades, 4%)
Decreased appetite (all grades, 4%)
Anorexia (all grades, 6%)
Dehydration (all grades, 1%)
Arthralgia (all grades, 1%)
Back pain (all grades, 1%)
Headache (all grades, 10%)
Dizziness (all grades, 2%)
Hypoaesthesia (all grades, 1%)
Insomnia (all grades, 5%)
Depression (all grades, 2%)
Cough (all grades, 6%)
Dyspnea (all grades, 2%)
Pharyngitis (all grades, 4%)
Epistaxis (all grades, 4%)
Sources: Page: p. 82
AEs

AEs

AESignificanceDosePopulation
Anaemia grade 1, 17%
20 mg/m2 1 times / day steady, intravenous
Recommended|MTD
Dose: 20 mg/m2, 1 times / day
Route: intravenous
Route: steady
Dose: 20 mg/m2, 1 times / day
Sources:
unhealthy, 59 years (range: 42–79 years)
n = 6
Health Status: unhealthy
Condition: unresectable liver-predominant metastases
Age Group: 59 years (range: 42–79 years)
Sex: M+F
Population Size: 6
Sources:
Leucopenia grade 1, 17%
20 mg/m2 1 times / day steady, intravenous
Recommended|MTD
Dose: 20 mg/m2, 1 times / day
Route: intravenous
Route: steady
Dose: 20 mg/m2, 1 times / day
Sources:
unhealthy, 59 years (range: 42–79 years)
n = 6
Health Status: unhealthy
Condition: unresectable liver-predominant metastases
Age Group: 59 years (range: 42–79 years)
Sex: M+F
Population Size: 6
Sources:
Thrombocytopaenia grade 1, 17%
20 mg/m2 1 times / day steady, intravenous
Recommended|MTD
Dose: 20 mg/m2, 1 times / day
Route: intravenous
Route: steady
Dose: 20 mg/m2, 1 times / day
Sources:
unhealthy, 59 years (range: 42–79 years)
n = 6
Health Status: unhealthy
Condition: unresectable liver-predominant metastases
Age Group: 59 years (range: 42–79 years)
Sex: M+F
Population Size: 6
Sources:
Lymphopenia grade 2, 17%
20 mg/m2 1 times / day steady, intravenous
Recommended|MTD
Dose: 20 mg/m2, 1 times / day
Route: intravenous
Route: steady
Dose: 20 mg/m2, 1 times / day
Sources:
unhealthy, 59 years (range: 42–79 years)
n = 6
Health Status: unhealthy
Condition: unresectable liver-predominant metastases
Age Group: 59 years (range: 42–79 years)
Sex: M+F
Population Size: 6
Sources:
Neutropenia grade 2, 17%
20 mg/m2 1 times / day steady, intravenous
Recommended|MTD
Dose: 20 mg/m2, 1 times / day
Route: intravenous
Route: steady
Dose: 20 mg/m2, 1 times / day
Sources:
unhealthy, 59 years (range: 42–79 years)
n = 6
Health Status: unhealthy
Condition: unresectable liver-predominant metastases
Age Group: 59 years (range: 42–79 years)
Sex: M+F
Population Size: 6
Sources:
Thrombocytopenia 2 patients
DLT
15 mg/m2 1 times / day steady, intravenous
Dose: 15 mg/m2, 1 times / day
Route: intravenous
Route: steady
Dose: 15 mg/m2, 1 times / day
Sources:
unhealthy, 61 years (range: 32–82 years)
n = 16
Health Status: unhealthy
Condition: CLL
Age Group: 61 years (range: 32–82 years)
Sex: M+F
Population Size: 16
Sources:
Hyperbilirubinemia grade 3, 2 patients
DLT
15 mg/m2 1 times / day steady, intravenous
Dose: 15 mg/m2, 1 times / day
Route: intravenous
Route: steady
Dose: 15 mg/m2, 1 times / day
Sources:
unhealthy, 61 years (range: 32–82 years)
n = 16
Health Status: unhealthy
Condition: CLL
Age Group: 61 years (range: 32–82 years)
Sex: M+F
Population Size: 16
Sources:
Leukopenia grade 3-4, 22%
15 mg/m2 3 times / day steady, intravenous
Recommended
Dose: 15 mg/m2, 3 times / day
Route: intravenous
Route: steady
Dose: 15 mg/m2, 3 times / day
Sources:
unhealthy, 70 years (range: 65-76 years)
n = 81
Health Status: unhealthy
Condition: myelodysplastic syndromes
Age Group: 70 years (range: 65-76 years)
Sex: M+F
Population Size: 81
Sources:
Febrile neutropenia grade 3-4, 23%
15 mg/m2 3 times / day steady, intravenous
Recommended
Dose: 15 mg/m2, 3 times / day
Route: intravenous
Route: steady
Dose: 15 mg/m2, 3 times / day
Sources:
unhealthy, 70 years (range: 65-76 years)
n = 81
Health Status: unhealthy
Condition: myelodysplastic syndromes
Age Group: 70 years (range: 65-76 years)
Sex: M+F
Population Size: 81
Sources:
Thrombocytopenia grade 3-4, 85%
15 mg/m2 3 times / day steady, intravenous
Recommended
Dose: 15 mg/m2, 3 times / day
Route: intravenous
Route: steady
Dose: 15 mg/m2, 3 times / day
Sources:
unhealthy, 70 years (range: 65-76 years)
n = 81
Health Status: unhealthy
Condition: myelodysplastic syndromes
Age Group: 70 years (range: 65-76 years)
Sex: M+F
Population Size: 81
Sources:
Neutropenia grade 3-4, 87%
15 mg/m2 3 times / day steady, intravenous
Recommended
Dose: 15 mg/m2, 3 times / day
Route: intravenous
Route: steady
Dose: 15 mg/m2, 3 times / day
Sources:
unhealthy, 70 years (range: 65-76 years)
n = 81
Health Status: unhealthy
Condition: myelodysplastic syndromes
Age Group: 70 years (range: 65-76 years)
Sex: M+F
Population Size: 81
Sources:
Anemia grade 5, 6 patients
Disc. AE
15 mg/m2 3 times / day steady, intravenous
Recommended
Dose: 15 mg/m2, 3 times / day
Route: intravenous
Route: steady
Dose: 15 mg/m2, 3 times / day
Sources:
unhealthy, 70 years (range: 65-76 years)
n = 81
Health Status: unhealthy
Condition: myelodysplastic syndromes
Age Group: 70 years (range: 65-76 years)
Sex: M+F
Population Size: 81
Sources:
Neutropenia grade 5, 6 patients
Disc. AE
15 mg/m2 3 times / day steady, intravenous
Recommended
Dose: 15 mg/m2, 3 times / day
Route: intravenous
Route: steady
Dose: 15 mg/m2, 3 times / day
Sources:
unhealthy, 70 years (range: 65-76 years)
n = 81
Health Status: unhealthy
Condition: myelodysplastic syndromes
Age Group: 70 years (range: 65-76 years)
Sex: M+F
Population Size: 81
Sources:
Thrombocytopenia grade 5, 6 patients
Disc. AE
15 mg/m2 3 times / day steady, intravenous
Recommended
Dose: 15 mg/m2, 3 times / day
Route: intravenous
Route: steady
Dose: 15 mg/m2, 3 times / day
Sources:
unhealthy, 70 years (range: 65-76 years)
n = 81
Health Status: unhealthy
Condition: myelodysplastic syndromes
Age Group: 70 years (range: 65-76 years)
Sex: M+F
Population Size: 81
Sources:
Febrile neutropenia grade 3-4, 2 patients
DLT
15 mg/m2 1 times / day steady, intravenous
Dose: 15 mg/m2, 1 times / day
Route: intravenous
Route: steady
Dose: 15 mg/m2, 1 times / day
Sources:
unhealthy, 72 years (range: 68–75 years)
n = 4
Health Status: unhealthy
Condition: NHL
Age Group: 72 years (range: 68–75 years)
Sex: M+F
Population Size: 4
Sources:
Alanine aminotransferase increased all grades, 1%
15 mg/m2 3 times / day steady, intravenous
Recommended
Dose: 15 mg/m2, 3 times / day
Route: intravenous
Route: steady
Dose: 15 mg/m2, 3 times / day
Sources: Page: p. 82
unhealthy
n = 83
Health Status: unhealthy
Population Size: 83
Sources: Page: p. 82
Alkaline phosphatase increased all grades, 1%
15 mg/m2 3 times / day steady, intravenous
Recommended
Dose: 15 mg/m2, 3 times / day
Route: intravenous
Route: steady
Dose: 15 mg/m2, 3 times / day
Sources: Page: p. 82
unhealthy
n = 83
Health Status: unhealthy
Population Size: 83
Sources: Page: p. 82
Arthralgia all grades, 1%
15 mg/m2 3 times / day steady, intravenous
Recommended
Dose: 15 mg/m2, 3 times / day
Route: intravenous
Route: steady
Dose: 15 mg/m2, 3 times / day
Sources: Page: p. 82
unhealthy
n = 83
Health Status: unhealthy
Population Size: 83
Sources: Page: p. 82
Aspartate aminotransferase increased all grades, 1%
15 mg/m2 3 times / day steady, intravenous
Recommended
Dose: 15 mg/m2, 3 times / day
Route: intravenous
Route: steady
Dose: 15 mg/m2, 3 times / day
Sources: Page: p. 82
unhealthy
n = 83
Health Status: unhealthy
Population Size: 83
Sources: Page: p. 82
Back pain all grades, 1%
15 mg/m2 3 times / day steady, intravenous
Recommended
Dose: 15 mg/m2, 3 times / day
Route: intravenous
Route: steady
Dose: 15 mg/m2, 3 times / day
Sources: Page: p. 82
unhealthy
n = 83
Health Status: unhealthy
Population Size: 83
Sources: Page: p. 82
Dehydration all grades, 1%
15 mg/m2 3 times / day steady, intravenous
Recommended
Dose: 15 mg/m2, 3 times / day
Route: intravenous
Route: steady
Dose: 15 mg/m2, 3 times / day
Sources: Page: p. 82
unhealthy
n = 83
Health Status: unhealthy
Population Size: 83
Sources: Page: p. 82
Fall all grades, 1%
15 mg/m2 3 times / day steady, intravenous
Recommended
Dose: 15 mg/m2, 3 times / day
Route: intravenous
Route: steady
Dose: 15 mg/m2, 3 times / day
Sources: Page: p. 82
unhealthy
n = 83
Health Status: unhealthy
Population Size: 83
Sources: Page: p. 82
Hepatomegaly all grades, 1%
15 mg/m2 3 times / day steady, intravenous
Recommended
Dose: 15 mg/m2, 3 times / day
Route: intravenous
Route: steady
Dose: 15 mg/m2, 3 times / day
Sources: Page: p. 82
unhealthy
n = 83
Health Status: unhealthy
Population Size: 83
Sources: Page: p. 82
Hypoaesthesia all grades, 1%
15 mg/m2 3 times / day steady, intravenous
Recommended
Dose: 15 mg/m2, 3 times / day
Route: intravenous
Route: steady
Dose: 15 mg/m2, 3 times / day
Sources: Page: p. 82
unhealthy
n = 83
Health Status: unhealthy
Population Size: 83
Sources: Page: p. 82
Pulmonary edema all grades, 1%
15 mg/m2 3 times / day steady, intravenous
Recommended
Dose: 15 mg/m2, 3 times / day
Route: intravenous
Route: steady
Dose: 15 mg/m2, 3 times / day
Sources: Page: p. 82
unhealthy
n = 83
Health Status: unhealthy
Population Size: 83
Sources: Page: p. 82
Tachycardia all grades, 1%
15 mg/m2 3 times / day steady, intravenous
Recommended
Dose: 15 mg/m2, 3 times / day
Route: intravenous
Route: steady
Dose: 15 mg/m2, 3 times / day
Sources: Page: p. 82
unhealthy
n = 83
Health Status: unhealthy
Population Size: 83
Sources: Page: p. 82
Urinary tract infection all grades, 1%
15 mg/m2 3 times / day steady, intravenous
Recommended
Dose: 15 mg/m2, 3 times / day
Route: intravenous
Route: steady
Dose: 15 mg/m2, 3 times / day
Sources: Page: p. 82
unhealthy
n = 83
Health Status: unhealthy
Population Size: 83
Sources: Page: p. 82
Headache all grades, 10%
15 mg/m2 3 times / day steady, intravenous
Recommended
Dose: 15 mg/m2, 3 times / day
Route: intravenous
Route: steady
Dose: 15 mg/m2, 3 times / day
Sources: Page: p. 82
unhealthy
n = 83
Health Status: unhealthy
Population Size: 83
Sources: Page: p. 82
Diarrhea all grades, 16%
15 mg/m2 3 times / day steady, intravenous
Recommended
Dose: 15 mg/m2, 3 times / day
Route: intravenous
Route: steady
Dose: 15 mg/m2, 3 times / day
Sources: Page: p. 82
unhealthy
n = 83
Health Status: unhealthy
Population Size: 83
Sources: Page: p. 82
Pyrexia all grades, 16%
15 mg/m2 3 times / day steady, intravenous
Recommended
Dose: 15 mg/m2, 3 times / day
Route: intravenous
Route: steady
Dose: 15 mg/m2, 3 times / day
Sources: Page: p. 82
unhealthy
n = 83
Health Status: unhealthy
Population Size: 83
Sources: Page: p. 82
Fatigue all grades, 18%
15 mg/m2 3 times / day steady, intravenous
Recommended
Dose: 15 mg/m2, 3 times / day
Route: intravenous
Route: steady
Dose: 15 mg/m2, 3 times / day
Sources: Page: p. 82
unhealthy
n = 83
Health Status: unhealthy
Population Size: 83
Sources: Page: p. 82
Cellulitis all grades, 2%
15 mg/m2 3 times / day steady, intravenous
Recommended
Dose: 15 mg/m2, 3 times / day
Route: intravenous
Route: steady
Dose: 15 mg/m2, 3 times / day
Sources: Page: p. 82
unhealthy
n = 83
Health Status: unhealthy
Population Size: 83
Sources: Page: p. 82
Depression all grades, 2%
15 mg/m2 3 times / day steady, intravenous
Recommended
Dose: 15 mg/m2, 3 times / day
Route: intravenous
Route: steady
Dose: 15 mg/m2, 3 times / day
Sources: Page: p. 82
unhealthy
n = 83
Health Status: unhealthy
Population Size: 83
Sources: Page: p. 82
Dizziness all grades, 2%
15 mg/m2 3 times / day steady, intravenous
Recommended
Dose: 15 mg/m2, 3 times / day
Route: intravenous
Route: steady
Dose: 15 mg/m2, 3 times / day
Sources: Page: p. 82
unhealthy
n = 83
Health Status: unhealthy
Population Size: 83
Sources: Page: p. 82
Dysphagia all grades, 2%
15 mg/m2 3 times / day steady, intravenous
Recommended
Dose: 15 mg/m2, 3 times / day
Route: intravenous
Route: steady
Dose: 15 mg/m2, 3 times / day
Sources: Page: p. 82
unhealthy
n = 83
Health Status: unhealthy
Population Size: 83
Sources: Page: p. 82
Dyspnea all grades, 2%
15 mg/m2 3 times / day steady, intravenous
Recommended
Dose: 15 mg/m2, 3 times / day
Route: intravenous
Route: steady
Dose: 15 mg/m2, 3 times / day
Sources: Page: p. 82
unhealthy
n = 83
Health Status: unhealthy
Population Size: 83
Sources: Page: p. 82
Hypomagnesaemia all grades, 2%
15 mg/m2 3 times / day steady, intravenous
Recommended
Dose: 15 mg/m2, 3 times / day
Route: intravenous
Route: steady
Dose: 15 mg/m2, 3 times / day
Sources: Page: p. 82
unhealthy
n = 83
Health Status: unhealthy
Population Size: 83
Sources: Page: p. 82
Loose stools all grades, 2%
15 mg/m2 3 times / day steady, intravenous
Recommended
Dose: 15 mg/m2, 3 times / day
Route: intravenous
Route: steady
Dose: 15 mg/m2, 3 times / day
Sources: Page: p. 82
unhealthy
n = 83
Health Status: unhealthy
Population Size: 83
Sources: Page: p. 82
Splenomegaly all grades, 2%
15 mg/m2 3 times / day steady, intravenous
Recommended
Dose: 15 mg/m2, 3 times / day
Route: intravenous
Route: steady
Dose: 15 mg/m2, 3 times / day
Sources: Page: p. 82
unhealthy
n = 83
Health Status: unhealthy
Population Size: 83
Sources: Page: p. 82
Nausea all grades, 22%
15 mg/m2 3 times / day steady, intravenous
Recommended
Dose: 15 mg/m2, 3 times / day
Route: intravenous
Route: steady
Dose: 15 mg/m2, 3 times / day
Sources: Page: p. 82
unhealthy
n = 83
Health Status: unhealthy
Population Size: 83
Sources: Page: p. 82
Abdominal pain all grades, 4%
15 mg/m2 3 times / day steady, intravenous
Recommended
Dose: 15 mg/m2, 3 times / day
Route: intravenous
Route: steady
Dose: 15 mg/m2, 3 times / day
Sources: Page: p. 82
unhealthy
n = 83
Health Status: unhealthy
Population Size: 83
Sources: Page: p. 82
Asthenia all grades, 4%
15 mg/m2 3 times / day steady, intravenous
Recommended
Dose: 15 mg/m2, 3 times / day
Route: intravenous
Route: steady
Dose: 15 mg/m2, 3 times / day
Sources: Page: p. 82
unhealthy
n = 83
Health Status: unhealthy
Population Size: 83
Sources: Page: p. 82
Decreased appetite all grades, 4%
15 mg/m2 3 times / day steady, intravenous
Recommended
Dose: 15 mg/m2, 3 times / day
Route: intravenous
Route: steady
Dose: 15 mg/m2, 3 times / day
Sources: Page: p. 82
unhealthy
n = 83
Health Status: unhealthy
Population Size: 83
Sources: Page: p. 82
Epistaxis all grades, 4%
15 mg/m2 3 times / day steady, intravenous
Recommended
Dose: 15 mg/m2, 3 times / day
Route: intravenous
Route: steady
Dose: 15 mg/m2, 3 times / day
Sources: Page: p. 82
unhealthy
n = 83
Health Status: unhealthy
Population Size: 83
Sources: Page: p. 82
Hyperbilirubinaemia all grades, 4%
15 mg/m2 3 times / day steady, intravenous
Recommended
Dose: 15 mg/m2, 3 times / day
Route: intravenous
Route: steady
Dose: 15 mg/m2, 3 times / day
Sources: Page: p. 82
unhealthy
n = 83
Health Status: unhealthy
Population Size: 83
Sources: Page: p. 82
Hypokalemia all grades, 4%
15 mg/m2 3 times / day steady, intravenous
Recommended
Dose: 15 mg/m2, 3 times / day
Route: intravenous
Route: steady
Dose: 15 mg/m2, 3 times / day
Sources: Page: p. 82
unhealthy
n = 83
Health Status: unhealthy
Population Size: 83
Sources: Page: p. 82
Pharyngitis all grades, 4%
15 mg/m2 3 times / day steady, intravenous
Recommended
Dose: 15 mg/m2, 3 times / day
Route: intravenous
Route: steady
Dose: 15 mg/m2, 3 times / day
Sources: Page: p. 82
unhealthy
n = 83
Health Status: unhealthy
Population Size: 83
Sources: Page: p. 82
Thrombocythaemia all grades, 4%
15 mg/m2 3 times / day steady, intravenous
Recommended
Dose: 15 mg/m2, 3 times / day
Route: intravenous
Route: steady
Dose: 15 mg/m2, 3 times / day
Sources: Page: p. 82
unhealthy
n = 83
Health Status: unhealthy
Population Size: 83
Sources: Page: p. 82
Insomnia all grades, 5%
15 mg/m2 3 times / day steady, intravenous
Recommended
Dose: 15 mg/m2, 3 times / day
Route: intravenous
Route: steady
Dose: 15 mg/m2, 3 times / day
Sources: Page: p. 82
unhealthy
n = 83
Health Status: unhealthy
Population Size: 83
Sources: Page: p. 82
Oral mucosal petechiae all grades, 5%
15 mg/m2 3 times / day steady, intravenous
Recommended
Dose: 15 mg/m2, 3 times / day
Route: intravenous
Route: steady
Dose: 15 mg/m2, 3 times / day
Sources: Page: p. 82
unhealthy
n = 83
Health Status: unhealthy
Population Size: 83
Sources: Page: p. 82
Tongue ulceration all grades, 5%
15 mg/m2 3 times / day steady, intravenous
Recommended
Dose: 15 mg/m2, 3 times / day
Route: intravenous
Route: steady
Dose: 15 mg/m2, 3 times / day
Sources: Page: p. 82
unhealthy
n = 83
Health Status: unhealthy
Population Size: 83
Sources: Page: p. 82
Anemia all grades, 54%
15 mg/m2 3 times / day steady, intravenous
Recommended
Dose: 15 mg/m2, 3 times / day
Route: intravenous
Route: steady
Dose: 15 mg/m2, 3 times / day
Sources: Page: p. 82
unhealthy
n = 83
Health Status: unhealthy
Population Size: 83
Sources: Page: p. 82
Anorexia all grades, 6%
15 mg/m2 3 times / day steady, intravenous
Recommended
Dose: 15 mg/m2, 3 times / day
Route: intravenous
Route: steady
Dose: 15 mg/m2, 3 times / day
Sources: Page: p. 82
unhealthy
n = 83
Health Status: unhealthy
Population Size: 83
Sources: Page: p. 82
Cough all grades, 6%
15 mg/m2 3 times / day steady, intravenous
Recommended
Dose: 15 mg/m2, 3 times / day
Route: intravenous
Route: steady
Dose: 15 mg/m2, 3 times / day
Sources: Page: p. 82
unhealthy
n = 83
Health Status: unhealthy
Population Size: 83
Sources: Page: p. 82
Hypoalbuminemia all grades, 7%
15 mg/m2 3 times / day steady, intravenous
Recommended
Dose: 15 mg/m2, 3 times / day
Route: intravenous
Route: steady
Dose: 15 mg/m2, 3 times / day
Sources: Page: p. 82
unhealthy
n = 83
Health Status: unhealthy
Population Size: 83
Sources: Page: p. 82
Hypocalcemia all grades, 7%
15 mg/m2 3 times / day steady, intravenous
Recommended
Dose: 15 mg/m2, 3 times / day
Route: intravenous
Route: steady
Dose: 15 mg/m2, 3 times / day
Sources: Page: p. 82
unhealthy
n = 83
Health Status: unhealthy
Population Size: 83
Sources: Page: p. 82
Stomatitis all grades, 7%
15 mg/m2 3 times / day steady, intravenous
Recommended
Dose: 15 mg/m2, 3 times / day
Route: intravenous
Route: steady
Dose: 15 mg/m2, 3 times / day
Sources: Page: p. 82
unhealthy
n = 83
Health Status: unhealthy
Population Size: 83
Sources: Page: p. 82
Constipation all grades, 8%
15 mg/m2 3 times / day steady, intravenous
Recommended
Dose: 15 mg/m2, 3 times / day
Route: intravenous
Route: steady
Dose: 15 mg/m2, 3 times / day
Sources: Page: p. 82
unhealthy
n = 83
Health Status: unhealthy
Population Size: 83
Sources: Page: p. 82
Vomiting all grades, 8%
15 mg/m2 3 times / day steady, intravenous
Recommended
Dose: 15 mg/m2, 3 times / day
Route: intravenous
Route: steady
Dose: 15 mg/m2, 3 times / day
Sources: Page: p. 82
unhealthy
n = 83
Health Status: unhealthy
Population Size: 83
Sources: Page: p. 82
Thrombocytopenia all grades, 81%
15 mg/m2 3 times / day steady, intravenous
Recommended
Dose: 15 mg/m2, 3 times / day
Route: intravenous
Route: steady
Dose: 15 mg/m2, 3 times / day
Sources: Page: p. 82
unhealthy
n = 83
Health Status: unhealthy
Population Size: 83
Sources: Page: p. 82
Neutropenia all grades, 83%
15 mg/m2 3 times / day steady, intravenous
Recommended
Dose: 15 mg/m2, 3 times / day
Route: intravenous
Route: steady
Dose: 15 mg/m2, 3 times / day
Sources: Page: p. 82
unhealthy
n = 83
Health Status: unhealthy
Population Size: 83
Sources: Page: p. 82
Overview

OverviewOther

Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
no
no
no
no
no
no
no
no
no
weak
yes
Drug as victim

Drug as victim

Tox targets
Sourcing

Sourcing

Vendor/AggregatorIDURL
PubMed

PubMed

TitleDatePubMed
Targeting hypomethylation of DNA to achieve cellular differentiation in myelodysplastic syndromes (MDS).
2001
The E-cadherin/catenin complex: an important gatekeeper in breast cancer tumorigenesis and malignant progression.
2001
Autoreactive murine Th1 and Th2 cells kill syngeneic macrophages and induce autoantibodies.
2001
Unnatural enantiomers of 5-azacytidine analogues: syntheses and enzymatic properties.
2001 Apr-Jul
Cytogenetic responses in high-risk myelodysplastic syndrome following low-dose treatment with the DNA methylation inhibitor 5-aza-2'-deoxycytidine.
2001 Aug
Reversion of transcriptional repression of Sp1 by 5 aza-2' deoxycytidine restores TGF-beta type II receptor expression in the pancreatic cancer cell line MIA PaCa-2.
2001 Aug 15
Molecular mechanisms for aberrant expression of the human breast cancer specific gene 1 in breast cancer cells: control of transcription by DNA methylation and intronic sequences.
2001 Aug 23
[Chemotherapy and radiation therapy].
2001 Dec
Identification and characterization of differentially methylated CpG islands in pancreatic carcinoma.
2001 Dec 1
Expression of the Hypermethylated in Cancer gene (HIC-1) is associated with good outcome in human breast cancer.
2001 Dec 14
Reversal of GSTP1 CpG island hypermethylation and reactivation of pi-class glutathione S-transferase (GSTP1) expression in human prostate cancer cells by treatment with procainamide.
2001 Dec 15
Antineoplastic action of 5-aza-2'-deoxycytidine and histone deacetylase inhibitor and their effect on the expression of retinoic acid receptor beta and estrogen receptor alpha genes in breast carcinoma cells.
2001 Jul
Loss of mismatch repair activity in simian virus 40 large T antigen-immortalized BPH-1 human prostatic epithelial cell line.
2001 Jul
Regulation of the intestinal mucin MUC2 gene expression in vivo: evidence for the role of promoter methylation.
2001 Jul 10
Decitabine with allogeneic peripheral blood stem cell transplantation in the therapy of leukemia relapse following a prior transplant: results of a phase I study.
2001 Jun
Transcriptional silencing of Cyclooxygenase-2 by hyper-methylation of the 5' CpG island in human gastric carcinoma cells.
2001 Jun 1
Large scale mapping of methylcytosines in CTCF-binding sites in the human H19 promoter and aberrant hypomethylation in human bladder cancer.
2001 Nov 1
Glypican-3 expression is silenced in human breast cancer.
2001 Nov 1
Hypermethylation in human cancers of the RIZ1 tumor suppressor gene, a member of a histone/protein methyltransferase superfamily.
2001 Nov 15
Reduced expression of intercellular adhesion molecule-1 in ovarian adenocarcinomas.
2001 Nov 2
Increased expression of unmethylated CDKN2D by 5-aza-2'-deoxycytidine in human lung cancer cells.
2001 Nov 22
Silencing of HTR1B and reduced expression of EDN1 in human lung cancers, revealed by methylation-sensitive representational difference analysis.
2001 Nov 8
E-cadherin expression is commonly downregulated by CpG island hypermethylation in esophageal carcinoma cells.
2001 Nov 8
Reduced expression of syndecan-1 affects metastatic potential and clinical outcome in patients with colorectal cancer.
2001 Oct
Dynamic DNA methylation change in the CpG island region of p15 during human myeloid development.
2001 Oct
DNA hypermethylation is a mechanism for loss of expression of the HLA class I genes in human esophageal squamous cell carcinomas.
2001 Oct
Frequent epigenetic inactivation of RASSF1A by aberrant promoter hypermethylation in human gastric adenocarcinoma.
2001 Oct 1
Synergistic activation of functional estrogen receptor (ER)-alpha by DNA methyltransferase and histone deacetylase inhibition in human ER-alpha-negative breast cancer cells.
2001 Oct 1
Chloroplast DNA methylation and inheritance in Chlamydomonas.
2001 Oct 1
Rexpression of HLA class I antigens and restoration of antigen-specific CTL response in melanoma cells following 5-aza-2'-deoxycytidine treatment.
2001 Oct 15
CpG hypermethylation of the promoter region inactivates the estrogen receptor-beta gene in patients with prostate carcinoma.
2001 Oct 15
Methylation in hMLH1 promoter interferes with its binding to transcription factor CBF and inhibits gene expression.
2001 Oct 25
Methylation-dependent silencing of the reduced folate carrier gene in inherently methotrexate-resistant human breast cancer cells.
2001 Oct 26
Pharmacological reactivation of inactive genes: the fragile X experience.
2001 Oct-Nov 1
Evolving treatment options of myelodysplastic syndromes.
2001 Sep
Selection of drug-resistant transduced cells with cytosine nucleoside analogs using the human cytidine deaminase gene.
2001 Sep
Epigenetic regulation of the KAI1 metastasis suppressor gene in human prostate cancer cell lines.
2001 Sep
CpG methylation of promoter region inactivates E-cadherin gene in renal cell carcinoma.
2001 Sep
Promoter hypermethylation of MGMT is associated with protein loss in gastric carcinoma.
2001 Sep
Sensitization for death receptor- or drug-induced apoptosis by re-expression of caspase-8 through demethylation or gene transfer.
2001 Sep 13
Hypermethylation of CpG islands in the mouse asparagine synthetase gene: relationship to asparaginase sensitivity in lymphoma cells. Partial methylation in normal cells.
2001 Sep 14
Frequent epigenetic inactivation of RASSF1A in human bladder carcinoma.
2001 Sep 15
Altered hox gene expression and cellular pathogenesis of 5-aza-2'-deoxycytidine-induced murine hindlimb dysmorphogenesis.
2001 Sep-Oct
Frequent allelic losses on the short arm of chromosome 1 and decreased expression of the p73 gene at 1p36.3 in squamous cell carcinoma of the oral cavity.
2002 Feb
Methylation-mediated silencing of TMS1/ASC is accompanied by histone hypoacetylation and CpG island-localized changes in chromatin architecture.
2002 Feb 15
Reduced expression of insulin-like growth factor binding protein-3 and its promoter hypermethylation in human hepatocellular carcinoma.
2002 Feb 25
Novel agents for the therapy of acute leukemia.
2002 Jan
Characterization of XAGE-1b, a short major transcript of cancer/testis-associated gene XAGE-1, induced in melanoma metastasis.
2002 Jan 10
Aberrant methylation and histone deacetylation of cyclooxygenase 2 in gastric cancer.
2002 Jan 20
Combined restriction landmark genomic scanning and virtual genome scans identify a novel human homeobox gene, ALX3, that is hypermethylated in neuroblastoma.
2002 Mar
Patents

Sample Use Guides

Regimen 1: administer decitabine (Dacogen) at a dose of 15 mg/m2 by continuous intravenous infusion over 3 hours repeated every 8 hours for 3 days. Repeat cycle every 6 weeks. Regimen 2: administer decitabine at a dose of 20 mg/m2 by continuous intravenous infusion over 1 hour repeated daily for 5 days. Repeat cycle every 4 weeks.
Route of Administration: Intravenous
In Vitro Use Guide
Sources: www.ncbi.nlm.nih.gov/pubmed/20126405
AML cells were treated daily with serial dilutions (0.02–50 uM) of freshlyprepared decitabine and incubated at 37 degree Celsius, 5% CO2 for 72 hours.
Name Type Language
DECITABINE
INN   MART.   MI   ORANGE BOOK   USAN   VANDF   WHO-DD  
INN   USAN  
Official Name English
1,3,5-TRIAZIN-2(1H)-ONE, 4-AMINO-1-(2-DEOXY-.BETA.-D-ERYTHRO-PENTOFURANOSYL)-
Common Name English
ASTX-727 COMPONENT DECITABINE
Common Name English
4-AMINO-1-(2-DEOXY-.BETA.-D-ERYTHRO-PENTOFURANOSYL)-S-TRIAZIN-2(1H)-ONE
Common Name English
DACOGEN
Brand Name English
DECITABINE [VANDF]
Common Name English
ASTX727 COMPONENT DECITABINE
Common Name English
NSC-127716
Code English
5-AZA-2'-DEOXYCYTIDINE
Systematic Name English
INQOVI COMPONENT DECITABINE
Brand Name English
5-AZA-DEOXYCYTIDINE
Systematic Name English
DECITABINE COMPONENT OF INQOVI
Brand Name English
DECITABINE [WHO-DD]
Common Name English
DECITABINE [INN]
Common Name English
DAC
Common Name English
2'-DEOXY-5-AZACYTIDINE
Common Name English
DECITABINE [MART.]
Common Name English
DECITABINE [USAN]
Common Name English
DECITABINE [MI]
Common Name English
DECITABINE [ORANGE BOOK]
Common Name English
Classification Tree Code System Code
FDA ORPHAN DRUG 555916
Created by admin on Sat Jun 26 00:22:15 UTC 2021 , Edited by admin on Sat Jun 26 00:22:15 UTC 2021
NCI_THESAURUS C1557
Created by admin on Sat Jun 26 00:22:15 UTC 2021 , Edited by admin on Sat Jun 26 00:22:15 UTC 2021
FDA ORPHAN DRUG 697019
Created by admin on Sat Jun 26 00:22:15 UTC 2021 , Edited by admin on Sat Jun 26 00:22:15 UTC 2021
FDA ORPHAN DRUG 227106
Created by admin on Sat Jun 26 00:22:15 UTC 2021 , Edited by admin on Sat Jun 26 00:22:15 UTC 2021
FDA ORPHAN DRUG 159702
Created by admin on Sat Jun 26 00:22:15 UTC 2021 , Edited by admin on Sat Jun 26 00:22:15 UTC 2021
NDF-RT N0000000233
Created by admin on Sat Jun 26 00:22:15 UTC 2021 , Edited by admin on Sat Jun 26 00:22:15 UTC 2021
FDA ORPHAN DRUG 122298
Created by admin on Sat Jun 26 00:22:15 UTC 2021 , Edited by admin on Sat Jun 26 00:22:15 UTC 2021
NCI_THESAURUS C2083
Created by admin on Sat Jun 26 00:22:15 UTC 2021 , Edited by admin on Sat Jun 26 00:22:15 UTC 2021
FDA ORPHAN DRUG 123399
Created by admin on Sat Jun 26 00:22:15 UTC 2021 , Edited by admin on Sat Jun 26 00:22:15 UTC 2021
FDA ORPHAN DRUG 537716
Created by admin on Sat Jun 26 00:22:15 UTC 2021 , Edited by admin on Sat Jun 26 00:22:15 UTC 2021
WHO-VATC QL01BC08
Created by admin on Sat Jun 26 00:22:15 UTC 2021 , Edited by admin on Sat Jun 26 00:22:15 UTC 2021
EU-Orphan Drug EU/3/17/1881
Created by admin on Sat Jun 26 00:22:15 UTC 2021 , Edited by admin on Sat Jun 26 00:22:15 UTC 2021
EMA ASSESSMENT REPORTS DACOGEN (AUTHORIZED: LEUKEMIA, MYELOID)
Created by admin on Sat Jun 26 00:22:15 UTC 2021 , Edited by admin on Sat Jun 26 00:22:15 UTC 2021
LIVERTOX 271
Created by admin on Sat Jun 26 00:22:15 UTC 2021 , Edited by admin on Sat Jun 26 00:22:15 UTC 2021
NDF-RT N0000175595
Created by admin on Sat Jun 26 00:22:15 UTC 2021 , Edited by admin on Sat Jun 26 00:22:15 UTC 2021
WHO-ATC L01BC08
Created by admin on Sat Jun 26 00:22:15 UTC 2021 , Edited by admin on Sat Jun 26 00:22:15 UTC 2021
FDA ORPHAN DRUG 20687
Created by admin on Sat Jun 26 00:22:15 UTC 2021 , Edited by admin on Sat Jun 26 00:22:15 UTC 2021
Code System Code Type Description
NCI_THESAURUS
C981
Created by admin on Sat Jun 26 00:22:15 UTC 2021 , Edited by admin on Sat Jun 26 00:22:15 UTC 2021
PRIMARY
WIKIPEDIA
DECITABINE
Created by admin on Sat Jun 26 00:22:15 UTC 2021 , Edited by admin on Sat Jun 26 00:22:15 UTC 2021
PRIMARY
DRUG BANK
DB01262
Created by admin on Sat Jun 26 00:22:15 UTC 2021 , Edited by admin on Sat Jun 26 00:22:15 UTC 2021
PRIMARY
FDA UNII
776B62CQ27
Created by admin on Sat Jun 26 00:22:15 UTC 2021 , Edited by admin on Sat Jun 26 00:22:15 UTC 2021
PRIMARY
EVMPD
SUB06932MIG
Created by admin on Sat Jun 26 00:22:15 UTC 2021 , Edited by admin on Sat Jun 26 00:22:15 UTC 2021
PRIMARY
MERCK INDEX
M4126
Created by admin on Sat Jun 26 00:22:15 UTC 2021 , Edited by admin on Sat Jun 26 00:22:15 UTC 2021
PRIMARY Merck Index
ChEMBL
CHEMBL1201129
Created by admin on Sat Jun 26 00:22:15 UTC 2021 , Edited by admin on Sat Jun 26 00:22:15 UTC 2021
PRIMARY
RXCUI
15657
Created by admin on Sat Jun 26 00:22:15 UTC 2021 , Edited by admin on Sat Jun 26 00:22:15 UTC 2021
PRIMARY RxNorm
DRUG CENTRAL
790
Created by admin on Sat Jun 26 00:22:15 UTC 2021 , Edited by admin on Sat Jun 26 00:22:15 UTC 2021
PRIMARY
IUPHAR
6805
Created by admin on Sat Jun 26 00:22:15 UTC 2021 , Edited by admin on Sat Jun 26 00:22:15 UTC 2021
PRIMARY
CAS
2353-33-5
Created by admin on Sat Jun 26 00:22:15 UTC 2021 , Edited by admin on Sat Jun 26 00:22:15 UTC 2021
PRIMARY
PUBCHEM
451668
Created by admin on Sat Jun 26 00:22:15 UTC 2021 , Edited by admin on Sat Jun 26 00:22:15 UTC 2021
PRIMARY
MESH
C014347
Created by admin on Sat Jun 26 00:22:15 UTC 2021 , Edited by admin on Sat Jun 26 00:22:15 UTC 2021
PRIMARY
LACTMED
Decitabine
Created by admin on Sat Jun 26 00:22:15 UTC 2021 , Edited by admin on Sat Jun 26 00:22:15 UTC 2021
PRIMARY
INN
6374
Created by admin on Sat Jun 26 00:22:15 UTC 2021 , Edited by admin on Sat Jun 26 00:22:15 UTC 2021
PRIMARY
EPA CompTox
2353-33-5
Created by admin on Sat Jun 26 00:22:15 UTC 2021 , Edited by admin on Sat Jun 26 00:22:15 UTC 2021
PRIMARY
ECHA (EC/EINECS)
219-089-4
Created by admin on Sat Jun 26 00:22:15 UTC 2021 , Edited by admin on Sat Jun 26 00:22:15 UTC 2021
PRIMARY