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Details

Stereochemistry ABSOLUTE
Molecular Formula C8H12N4O4
Molecular Weight 228.2053
Optical Activity UNSPECIFIED
Defined Stereocenters 3 / 3
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of DECITABINE

SMILES

NC1=NC(=O)N(C=N1)[C@H]2C[C@H](O)[C@@H](CO)O2

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

Molecular Formula C8H12N4O4
Molecular Weight 228.2053
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 3 / 3
E/Z Centers 0
Optical Activity UNSPECIFIED

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
Unnatural enantiomers of 5-azacytidine analogues: syntheses and enzymatic properties.
2000 Nov
Demethylation by 5-aza-2'-deoxycytidine (5-azadC) of p16INK4A gene results in downregulation of vascular endothelial growth factor expression in human lung cancer cell lines.
2001
Applications of microarray technology in breast cancer research.
2001
Changes in DNA methylation in neoplasia: pathophysiology and therapeutic implications.
2001 Apr 3
Unnatural enantiomers of 5-azacytidine analogues: syntheses and enzymatic properties.
2001 Apr-Jul
Activation of the maternally preset program of apoptosis by microinjection of 5-aza-2'-deoxycytidine and 5-methyl-2'-deoxycytidine-5'-triphosphate in Xenopus laevis embryos.
2001 Aug
[Chemotherapy and radiation therapy].
2001 Dec
Reexpression of a cluster of silenced transgenes is associated with their rearrangement.
2001 Dec
Identification and characterization of differentially methylated CpG islands in pancreatic carcinoma.
2001 Dec 1
Resistance to tumor necrosis factor-related apoptosis-inducing ligand (TRAIL)-induced apoptosis in neuroblastoma cells correlates with a loss of caspase-8 expression.
2001 Feb 15
Progesterone receptor B gene inactivation and CpG hypermethylation in human uterine endometrial cancer.
2001 Jan 1
Inactivation of the apoptosis effector Apaf-1 in malignant melanoma.
2001 Jan 11
Evidence that silencing of the HPRT promoter by DNA methylation is mediated by critical CpG sites.
2001 Jan 5
Aberrant methylation of the adenomatous polyposis coli (APC) gene promoter 1A in breast and lung carcinomas.
2001 Jul
Transcription regulation and protein subcellular localization of the truncated basic hair keratin hHb1-DeltaN in human breast cancer cells.
2001 Jun 22
Association of acetylated histones with paternally expressed genes in the Prader--Willi deletion region.
2001 Mar 15
Reduced expression of syndecan-1 affects metastatic potential and clinical outcome in patients with colorectal cancer.
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
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
CpG hypermethylation of the promoter region inactivates the estrogen receptor-beta gene in patients with prostate carcinoma.
2001 Oct 15
Methylation-dependent silencing of the reduced folate carrier gene in inherently methotrexate-resistant human breast cancer cells.
2001 Oct 26
Methylation status in the promoter region of the human PGP9.5 gene in cancer and normal tissues.
2001 Sep 10
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
Patents

Sample Use Guides

Guadecitabine 60 mg/m2 given subcutaneously daily on Days 1-5 in 28-day cycles. The total amount (in mg) of guadecitabine to be administered is determined by body surface area.
Route of Administration: Other
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.
Substance Class Chemical
Created
by admin
on Thu Jul 06 21:34:22 UTC 2023
Edited
by admin
on Thu Jul 06 21:34:22 UTC 2023
Record UNII
776B62CQ27
Record Status Validated (UNII)
Record Version
  • Download
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
Decitabine [WHO-DD]
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 [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 Thu Jul 06 21:34:24 UTC 2023 , Edited by admin on Thu Jul 06 21:34:24 UTC 2023
NCI_THESAURUS C1557
Created by admin on Thu Jul 06 21:34:24 UTC 2023 , Edited by admin on Thu Jul 06 21:34:24 UTC 2023
FDA ORPHAN DRUG 227106
Created by admin on Thu Jul 06 21:34:24 UTC 2023 , Edited by admin on Thu Jul 06 21:34:24 UTC 2023
FDA ORPHAN DRUG 159702
Created by admin on Thu Jul 06 21:34:24 UTC 2023 , Edited by admin on Thu Jul 06 21:34:24 UTC 2023
NDF-RT N0000000233
Created by admin on Thu Jul 06 21:34:24 UTC 2023 , Edited by admin on Thu Jul 06 21:34:24 UTC 2023
FDA ORPHAN DRUG 122298
Created by admin on Thu Jul 06 21:34:24 UTC 2023 , Edited by admin on Thu Jul 06 21:34:24 UTC 2023
NCI_THESAURUS C2083
Created by admin on Thu Jul 06 21:34:24 UTC 2023 , Edited by admin on Thu Jul 06 21:34:24 UTC 2023
FDA ORPHAN DRUG 123399
Created by admin on Thu Jul 06 21:34:24 UTC 2023 , Edited by admin on Thu Jul 06 21:34:24 UTC 2023
FDA ORPHAN DRUG 537716
Created by admin on Thu Jul 06 21:34:24 UTC 2023 , Edited by admin on Thu Jul 06 21:34:24 UTC 2023
WHO-VATC QL01BC08
Created by admin on Thu Jul 06 21:34:24 UTC 2023 , Edited by admin on Thu Jul 06 21:34:24 UTC 2023
EU-Orphan Drug EU/3/17/1881
Created by admin on Thu Jul 06 21:34:24 UTC 2023 , Edited by admin on Thu Jul 06 21:34:24 UTC 2023
EMA ASSESSMENT REPORTS DACOGEN (AUTHORIZED: LEUKEMIA, MYELOID)
Created by admin on Thu Jul 06 21:34:24 UTC 2023 , Edited by admin on Thu Jul 06 21:34:24 UTC 2023
FDA ORPHAN DRUG 697019
Created by admin on Thu Jul 06 21:34:24 UTC 2023 , Edited by admin on Thu Jul 06 21:34:24 UTC 2023
LIVERTOX NBK548668
Created by admin on Thu Jul 06 21:34:24 UTC 2023 , Edited by admin on Thu Jul 06 21:34:24 UTC 2023
NDF-RT N0000175595
Created by admin on Thu Jul 06 21:34:24 UTC 2023 , Edited by admin on Thu Jul 06 21:34:24 UTC 2023
WHO-ATC L01BC08
Created by admin on Thu Jul 06 21:34:24 UTC 2023 , Edited by admin on Thu Jul 06 21:34:24 UTC 2023
FDA ORPHAN DRUG 20687
Created by admin on Thu Jul 06 21:34:24 UTC 2023 , Edited by admin on Thu Jul 06 21:34:24 UTC 2023
Code System Code Type Description
NCI_THESAURUS
C981
Created by admin on Thu Jul 06 21:34:24 UTC 2023 , Edited by admin on Thu Jul 06 21:34:24 UTC 2023
PRIMARY
WIKIPEDIA
DECITABINE
Created by admin on Thu Jul 06 21:34:24 UTC 2023 , Edited by admin on Thu Jul 06 21:34:24 UTC 2023
PRIMARY
DRUG BANK
DB01262
Created by admin on Thu Jul 06 21:34:24 UTC 2023 , Edited by admin on Thu Jul 06 21:34:24 UTC 2023
PRIMARY
FDA UNII
776B62CQ27
Created by admin on Thu Jul 06 21:34:24 UTC 2023 , Edited by admin on Thu Jul 06 21:34:24 UTC 2023
PRIMARY
EVMPD
SUB06932MIG
Created by admin on Thu Jul 06 21:34:24 UTC 2023 , Edited by admin on Thu Jul 06 21:34:24 UTC 2023
PRIMARY
MERCK INDEX
M4126
Created by admin on Thu Jul 06 21:34:24 UTC 2023 , Edited by admin on Thu Jul 06 21:34:24 UTC 2023
PRIMARY Merck Index
ChEMBL
CHEMBL1201129
Created by admin on Thu Jul 06 21:34:24 UTC 2023 , Edited by admin on Thu Jul 06 21:34:24 UTC 2023
PRIMARY
CHEBI
50131
Created by admin on Thu Jul 06 21:34:24 UTC 2023 , Edited by admin on Thu Jul 06 21:34:24 UTC 2023
PRIMARY
RXCUI
15657
Created by admin on Thu Jul 06 21:34:24 UTC 2023 , Edited by admin on Thu Jul 06 21:34:24 UTC 2023
PRIMARY RxNorm
DRUG CENTRAL
790
Created by admin on Thu Jul 06 21:34:24 UTC 2023 , Edited by admin on Thu Jul 06 21:34:24 UTC 2023
PRIMARY
IUPHAR
6805
Created by admin on Thu Jul 06 21:34:24 UTC 2023 , Edited by admin on Thu Jul 06 21:34:24 UTC 2023
PRIMARY
DAILYMED
776B62CQ27
Created by admin on Thu Jul 06 21:34:24 UTC 2023 , Edited by admin on Thu Jul 06 21:34:24 UTC 2023
PRIMARY
CAS
2353-33-5
Created by admin on Thu Jul 06 21:34:24 UTC 2023 , Edited by admin on Thu Jul 06 21:34:24 UTC 2023
PRIMARY
RS_ITEM_NUM
1165204
Created by admin on Thu Jul 06 21:34:24 UTC 2023 , Edited by admin on Thu Jul 06 21:34:24 UTC 2023
PRIMARY
PUBCHEM
451668
Created by admin on Thu Jul 06 21:34:24 UTC 2023 , Edited by admin on Thu Jul 06 21:34:24 UTC 2023
PRIMARY
MESH
C014347
Created by admin on Thu Jul 06 21:34:24 UTC 2023 , Edited by admin on Thu Jul 06 21:34:24 UTC 2023
PRIMARY
LACTMED
Decitabine
Created by admin on Thu Jul 06 21:34:24 UTC 2023 , Edited by admin on Thu Jul 06 21:34:24 UTC 2023
PRIMARY
INN
6374
Created by admin on Thu Jul 06 21:34:24 UTC 2023 , Edited by admin on Thu Jul 06 21:34:24 UTC 2023
PRIMARY
SMS_ID
100000083471
Created by admin on Thu Jul 06 21:34:24 UTC 2023 , Edited by admin on Thu Jul 06 21:34:24 UTC 2023
PRIMARY
EPA CompTox
DTXSID7030432
Created by admin on Thu Jul 06 21:34:24 UTC 2023 , Edited by admin on Thu Jul 06 21:34:24 UTC 2023
PRIMARY
USAN
AA-24
Created by admin on Thu Jul 06 21:34:24 UTC 2023 , Edited by admin on Thu Jul 06 21:34:24 UTC 2023
PRIMARY
ECHA (EC/EINECS)
219-089-4
Created by admin on Thu Jul 06 21:34:24 UTC 2023 , Edited by admin on Thu Jul 06 21:34:24 UTC 2023
PRIMARY
NSC
127716
Created by admin on Thu Jul 06 21:34:24 UTC 2023 , Edited by admin on Thu Jul 06 21:34:24 UTC 2023
PRIMARY
Related Record Type Details
SOLVATE->ANHYDROUS
BINDER->LIGAND
BINDING
EXCRETED UNCHANGED
According to the limited data in the study by van Groeningen et al. (1986), decitabine is not excreted unchanged in urine.
TARGET -> INHIBITOR
SALT/SOLVATE -> PARENT
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Biological Half-life PHARMACOKINETIC
Tmax PHARMACOKINETIC ONCE DAILY

ORAL ADMINISTRATION