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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

2006
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
77 ng/mL
15 mg/m² 3 times / day 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
155 ng/mL
20 mg/m² 1 times / day multiple, intravenous
dose: 20 mg/m²
route of administration: Intravenous
experiment type: MULTIPLE
co-administered:
DECITABINE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status:
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
158 ng × h/mL
15 mg/m² 3 times / day 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
802.81 ng × h/mL
20 mg/m² 1 times / day multiple, intravenous
dose: 20 mg/m²
route of administration: Intravenous
experiment type: MULTIPLE
co-administered:
DECITABINE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
750.82 ng × h/mL
35 mg 1 times / day multiple, oral
dose: 35 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered: CEDAZURIDINE
DECITABINE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
150 ng × h/mL
20 mg/m² 1 times / day multiple, intravenous
dose: 20 mg/m²
route of administration: Intravenous
experiment type: MULTIPLE
co-administered:
DECITABINE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status:
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
0.78 h
15 mg/m² 3 times / day 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
0.2 h
20 mg/m² 1 times / day multiple, intravenous
dose: 20 mg/m²
route of administration: Intravenous
experiment type: MULTIPLE
co-administered:
DECITABINE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status:
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)
Health Status: unhealthy
Age Group: 52 years (range: 23 - 78 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 59 years (range: 42–79 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 61 years (range: 32–82 years)
Sex: M+F
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
Health Status: unhealthy
Age Group: 65 years
Sex: M+F
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)
Health Status: unhealthy
Age Group: 70 years (range: 65-76 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 72 years (range: 68–75 years)
Sex: M+F
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
Health Status: unhealthy
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
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:
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)
Health Status: unhealthy
Age Group: 59 years (range: 42–79 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 59 years (range: 42–79 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 59 years (range: 42–79 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 59 years (range: 42–79 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 59 years (range: 42–79 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 61 years (range: 32–82 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 61 years (range: 32–82 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 70 years (range: 65-76 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 70 years (range: 65-76 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 70 years (range: 65-76 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 70 years (range: 65-76 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 70 years (range: 65-76 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 70 years (range: 65-76 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 70 years (range: 65-76 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 72 years (range: 68–75 years)
Sex: M+F
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:
unhealthy
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:
unhealthy
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:
unhealthy
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:
unhealthy
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:
unhealthy
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:
unhealthy
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:
unhealthy
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:
unhealthy
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:
unhealthy
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:
unhealthy
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:
unhealthy
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:
unhealthy
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:
unhealthy
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:
unhealthy
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:
unhealthy
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:
unhealthy
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:
unhealthy
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:
unhealthy
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:
unhealthy
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:
unhealthy
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:
unhealthy
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:
unhealthy
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:
unhealthy
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:
unhealthy
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:
unhealthy
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:
unhealthy
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:
unhealthy
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:
unhealthy
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:
unhealthy
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:
unhealthy
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:
unhealthy
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:
unhealthy
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:
unhealthy
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:
unhealthy
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:
unhealthy
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:
unhealthy
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:
unhealthy
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:
unhealthy
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:
unhealthy
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:
unhealthy
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:
unhealthy
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:
unhealthy
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:
unhealthy
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:
unhealthy
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:
unhealthy
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:
unhealthy
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
Hypermethylation of the cpG island of Ras association domain family 1A (RASSF1A), a putative tumor suppressor gene from the 3p21.3 locus, occurs in a large percentage of human breast cancers.
2001 Apr 1
Unnatural enantiomers of 5-azacytidine analogues: syntheses and enzymatic properties.
2001 Apr-Jul
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
[Chemotherapy and radiation therapy].
2001 Dec
Identification of a novel member of the snail/Gfi-1 repressor family, mlt 1, which is methylated and silenced in liver tumors of SV40 T antigen transgenic mice.
2001 Feb 1
Unbalanced expression of HLA-A and -B antigens: a specific feature of cutaneous melanoma and other non-hemopoietic malignancies reverted by IFN-gamma.
2001 Feb 15
Induction of MAGE-3 expression in lung and esophageal cancer cells.
2001 Jan
Hypermethylation leads to silencing of the SYK gene in human breast cancer.
2001 Jul 15
Transcriptional silencing of Cyclooxygenase-2 by hyper-methylation of the 5' CpG island in human gastric carcinoma cells.
2001 Jun 1
Pharmacologic induction of fetal hemoglobin: raising the therapeutic bar in sickle cell disease.
2001 Mar
Elevation of breast carcinoma Nm23-H1 metastasis suppressor gene expression and reduced motility by DNA methylation inhibition.
2001 Mar 1
Regulation of CD21 expression by DNA methylation and histone deacetylation.
2001 May
Methylation in hMLH1 promoter interferes with its binding to transcription factor CBF and inhibits gene expression.
2001 Oct 25
Hypermethylation of the tumor necrosis factor receptor superfamily 6 (APT1, Fas, CD95/Apo-1) gene promoter at rel/nuclear factor kappaB sites in prostatic carcinoma.
2001 Sep
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
Reduced expression of insulin-like growth factor binding protein-3 and its promoter hypermethylation in human hepatocellular carcinoma.
2002 Feb 25
The 5-lipoxygenase promoter is regulated by DNA methylation.
2002 Feb 8
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
Immunomodulatory activity of SGI-110, a 5-aza-2'-deoxycytidine-containing demethylating dinucleotide.
2013 Mar
TGF-β induces global changes in DNA methylation during the epithelial-to-mesenchymal transition in ovarian cancer cells.
2014 Nov
Guadecitabine (SGI-110) in patients with intermediate or high-risk myelodysplastic syndromes: phase 2 results from a multicentre, open-label, randomised, phase 1/2 trial.
2019 Jun
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 Wed Apr 02 07:04:39 GMT 2025
Edited
by admin
on Wed Apr 02 07:04:39 GMT 2025
Record UNII
776B62CQ27
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
DACOGEN
Preferred Name English
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
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 [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 Wed Apr 02 07:04:39 GMT 2025 , Edited by admin on Wed Apr 02 07:04:39 GMT 2025
NCI_THESAURUS C1557
Created by admin on Wed Apr 02 07:04:39 GMT 2025 , Edited by admin on Wed Apr 02 07:04:39 GMT 2025
FDA ORPHAN DRUG 227106
Created by admin on Wed Apr 02 07:04:39 GMT 2025 , Edited by admin on Wed Apr 02 07:04:39 GMT 2025
FDA ORPHAN DRUG 159702
Created by admin on Wed Apr 02 07:04:39 GMT 2025 , Edited by admin on Wed Apr 02 07:04:39 GMT 2025
NDF-RT N0000000233
Created by admin on Wed Apr 02 07:04:39 GMT 2025 , Edited by admin on Wed Apr 02 07:04:39 GMT 2025
FDA ORPHAN DRUG 122298
Created by admin on Wed Apr 02 07:04:39 GMT 2025 , Edited by admin on Wed Apr 02 07:04:39 GMT 2025
NCI_THESAURUS C2083
Created by admin on Wed Apr 02 07:04:39 GMT 2025 , Edited by admin on Wed Apr 02 07:04:39 GMT 2025
FDA ORPHAN DRUG 123399
Created by admin on Wed Apr 02 07:04:39 GMT 2025 , Edited by admin on Wed Apr 02 07:04:39 GMT 2025
FDA ORPHAN DRUG 537716
Created by admin on Wed Apr 02 07:04:39 GMT 2025 , Edited by admin on Wed Apr 02 07:04:39 GMT 2025
WHO-VATC QL01BC08
Created by admin on Wed Apr 02 07:04:39 GMT 2025 , Edited by admin on Wed Apr 02 07:04:39 GMT 2025
EU-Orphan Drug EU/3/17/1881
Created by admin on Wed Apr 02 07:04:39 GMT 2025 , Edited by admin on Wed Apr 02 07:04:39 GMT 2025
EMA ASSESSMENT REPORTS DACOGEN (AUTHORIZED: LEUKEMIA, MYELOID)
Created by admin on Wed Apr 02 07:04:39 GMT 2025 , Edited by admin on Wed Apr 02 07:04:39 GMT 2025
FDA ORPHAN DRUG 697019
Created by admin on Wed Apr 02 07:04:39 GMT 2025 , Edited by admin on Wed Apr 02 07:04:39 GMT 2025
LIVERTOX NBK548668
Created by admin on Wed Apr 02 07:04:39 GMT 2025 , Edited by admin on Wed Apr 02 07:04:39 GMT 2025
NDF-RT N0000175595
Created by admin on Wed Apr 02 07:04:39 GMT 2025 , Edited by admin on Wed Apr 02 07:04:39 GMT 2025
WHO-ATC L01BC08
Created by admin on Wed Apr 02 07:04:39 GMT 2025 , Edited by admin on Wed Apr 02 07:04:39 GMT 2025
FDA ORPHAN DRUG 20687
Created by admin on Wed Apr 02 07:04:39 GMT 2025 , Edited by admin on Wed Apr 02 07:04:39 GMT 2025
Code System Code Type Description
NCI_THESAURUS
C981
Created by admin on Wed Apr 02 07:04:39 GMT 2025 , Edited by admin on Wed Apr 02 07:04:39 GMT 2025
PRIMARY
WIKIPEDIA
DECITABINE
Created by admin on Wed Apr 02 07:04:39 GMT 2025 , Edited by admin on Wed Apr 02 07:04:39 GMT 2025
PRIMARY
DRUG BANK
DB01262
Created by admin on Wed Apr 02 07:04:39 GMT 2025 , Edited by admin on Wed Apr 02 07:04:39 GMT 2025
PRIMARY
FDA UNII
776B62CQ27
Created by admin on Wed Apr 02 07:04:39 GMT 2025 , Edited by admin on Wed Apr 02 07:04:39 GMT 2025
PRIMARY
EVMPD
SUB06932MIG
Created by admin on Wed Apr 02 07:04:39 GMT 2025 , Edited by admin on Wed Apr 02 07:04:39 GMT 2025
PRIMARY
MERCK INDEX
m4126
Created by admin on Wed Apr 02 07:04:39 GMT 2025 , Edited by admin on Wed Apr 02 07:04:39 GMT 2025
PRIMARY Merck Index
ChEMBL
CHEMBL1201129
Created by admin on Wed Apr 02 07:04:39 GMT 2025 , Edited by admin on Wed Apr 02 07:04:39 GMT 2025
PRIMARY
CHEBI
50131
Created by admin on Wed Apr 02 07:04:39 GMT 2025 , Edited by admin on Wed Apr 02 07:04:39 GMT 2025
PRIMARY
RXCUI
15657
Created by admin on Wed Apr 02 07:04:39 GMT 2025 , Edited by admin on Wed Apr 02 07:04:39 GMT 2025
PRIMARY RxNorm
DRUG CENTRAL
790
Created by admin on Wed Apr 02 07:04:39 GMT 2025 , Edited by admin on Wed Apr 02 07:04:39 GMT 2025
PRIMARY
IUPHAR
6805
Created by admin on Wed Apr 02 07:04:39 GMT 2025 , Edited by admin on Wed Apr 02 07:04:39 GMT 2025
PRIMARY
DAILYMED
776B62CQ27
Created by admin on Wed Apr 02 07:04:39 GMT 2025 , Edited by admin on Wed Apr 02 07:04:39 GMT 2025
PRIMARY
CAS
2353-33-5
Created by admin on Wed Apr 02 07:04:39 GMT 2025 , Edited by admin on Wed Apr 02 07:04:39 GMT 2025
PRIMARY
RS_ITEM_NUM
1165204
Created by admin on Wed Apr 02 07:04:39 GMT 2025 , Edited by admin on Wed Apr 02 07:04:39 GMT 2025
PRIMARY
PUBCHEM
451668
Created by admin on Wed Apr 02 07:04:39 GMT 2025 , Edited by admin on Wed Apr 02 07:04:39 GMT 2025
PRIMARY
MESH
C014347
Created by admin on Wed Apr 02 07:04:39 GMT 2025 , Edited by admin on Wed Apr 02 07:04:39 GMT 2025
PRIMARY
LACTMED
Decitabine
Created by admin on Wed Apr 02 07:04:39 GMT 2025 , Edited by admin on Wed Apr 02 07:04:39 GMT 2025
PRIMARY
INN
6374
Created by admin on Wed Apr 02 07:04:39 GMT 2025 , Edited by admin on Wed Apr 02 07:04:39 GMT 2025
PRIMARY
SMS_ID
100000083471
Created by admin on Wed Apr 02 07:04:39 GMT 2025 , Edited by admin on Wed Apr 02 07:04:39 GMT 2025
PRIMARY
EPA CompTox
DTXSID7030432
Created by admin on Wed Apr 02 07:04:39 GMT 2025 , Edited by admin on Wed Apr 02 07:04:39 GMT 2025
PRIMARY
USAN
AA-24
Created by admin on Wed Apr 02 07:04:39 GMT 2025 , Edited by admin on Wed Apr 02 07:04:39 GMT 2025
PRIMARY
ECHA (EC/EINECS)
219-089-4
Created by admin on Wed Apr 02 07:04:39 GMT 2025 , Edited by admin on Wed Apr 02 07:04:39 GMT 2025
PRIMARY
NSC
127716
Created by admin on Wed Apr 02 07:04:39 GMT 2025 , Edited by admin on Wed Apr 02 07:04:39 GMT 2025
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