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
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
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 |
DescriptionSources: https://clinicaltrials.gov/ct2/show/NCT02907359 | https://www.ncbi.nlm.nih.gov/pubmed/31060979 | https://clinicaltrials.gov/ct2/show/NCT02348489 | https://www.businesswire.com/news/home/20151006006636/en/Astex-Pharmaceuticals-Announces-Orphan-Drug-Designation-Guadecitabine | https://astx.com/research-development/clinical-pipeline/guadecitabine-sgi-110-dnmt-inhibitor-solid-tumors/https://www.ncbi.nlm.nih.gov/pubmed/23369223Curator'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
Sources: https://clinicaltrials.gov/ct2/show/NCT02907359 | https://www.ncbi.nlm.nih.gov/pubmed/31060979 | https://clinicaltrials.gov/ct2/show/NCT02348489 | https://www.businesswire.com/news/home/20151006006636/en/Astex-Pharmaceuticals-Announces-Orphan-Drug-Designation-Guadecitabine | https://astx.com/research-development/clinical-pipeline/guadecitabine-sgi-110-dnmt-inhibitor-solid-tumors/https://www.ncbi.nlm.nih.gov/pubmed/23369223
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).
CNS Activity
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL2311221 |
|||
Target ID: CHEMBL1993 Sources: www.ncbi.nlm.nih.gov/pubmed/20501800 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | DACOGEN Approved UseDacogen 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 Date2006 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
77 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/17564707 |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/22816487/ |
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
158 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/17564707 |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/32285126/ |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/32285126/ |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/22816487/ |
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
0.78 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/17564707 |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/22816487/ |
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
99% |
DECITABINE plasma | Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
Doses
Dose | Population | Adverse 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%) Sources: Lymphopenia (grade 2, 17%) Neutropenia (grade 2, 17%) Leucopenia (grade 1, 17%) Thrombocytopaenia (grade 1, 17%) |
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) Sources: Thrombocytopenia (2 patients) |
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) Other AEs:Neutropenia (grade 5, 6 patients) Thrombocytopenia (grade 5, 6 patients) Neutropenia (grade 3-4, 87%) Sources: Thrombocytopenia (grade 3-4, 85%) Febrile neutropenia (grade 3-4, 23%) Leukopenia (grade 3-4, 22%) |
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 |
|
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 Health Status: unhealthy Sources: |
Other AEs: Neutropenia, Thrombocytopenia... Other AEs: Neutropenia (all grades, 83%) Sources: 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%) |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Other Inhibitor | Other Substrate | Other Inducer |
---|---|---|
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021790s000_Dacogen_BioPharmR.pdf#page=20 Page: 20.0 |
no | |||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
weak | ||||
Sources: https://pdf.hres.ca/dpd_pm/00049298.PDF#page=19 Page: 19.0 |
yes |
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
weak |
Tox targets
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
PubMed
Title | Date | PubMed |
---|---|---|
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
In Vivo Use Guide
Sources: https://clinicaltrials.gov/ct2/show/NCT02907359
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
Substance Class |
Chemical
Created
by
admin
on
Edited
Wed Apr 02 07:04:39 GMT 2025
by
admin
on
Wed Apr 02 07:04:39 GMT 2025
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Record UNII |
776B62CQ27
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Record Status |
Validated (UNII)
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Record Version |
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Classification Tree | Code System | Code | ||
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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
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NCI_THESAURUS |
C1557
Created by
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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
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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
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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
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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
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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
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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
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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
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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
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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
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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
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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
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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
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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
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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
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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
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Code System | Code | Type | Description | ||
---|---|---|---|---|---|
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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
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PRIMARY | |||
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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
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PRIMARY | |||
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DB01262
Created by
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PRIMARY | |||
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776B62CQ27
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PRIMARY | |||
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SUB06932MIG
Created by
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PRIMARY | |||
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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
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PRIMARY | Merck Index | ||
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CHEMBL1201129
Created by
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PRIMARY | |||
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50131
Created by
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PRIMARY | |||
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15657
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PRIMARY | RxNorm | ||
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790
Created by
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PRIMARY | |||
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6805
Created by
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PRIMARY | |||
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776B62CQ27
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PRIMARY | |||
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2353-33-5
Created by
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PRIMARY | |||
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1165204
Created by
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PRIMARY | |||
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451668
Created by
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PRIMARY | |||
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C014347
Created by
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PRIMARY | |||
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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
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PRIMARY | |||
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6374
Created by
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PRIMARY | |||
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100000083471
Created by
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PRIMARY | |||
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DTXSID7030432
Created by
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PRIMARY | |||
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AA-24
Created by
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PRIMARY | |||
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219-089-4
Created by
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PRIMARY | |||
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127716
Created by
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PRIMARY |
Related Record | Type | Details | ||
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SOLVATE->ANHYDROUS | |||
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BINDER->LIGAND |
BINDING
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EXCRETED UNCHANGED |
According to the limited data in the study by van Groeningen et al. (1986), decitabine is not excreted unchanged in urine.
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TARGET -> INHIBITOR |
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SALT/SOLVATE -> PARENT |
Related Record | Type | Details | ||
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METABOLITE INACTIVE -> PARENT | |||
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PRODRUG -> METABOLITE ACTIVE |
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METABOLITE -> PARENT | |||
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METABOLITE -> PARENT | |||
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METABOLITE -> PARENT |
Related Record | Type | Details | ||
---|---|---|---|---|
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ACTIVE MOIETY |
|
Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
---|---|---|---|---|---|---|
Biological Half-life | PHARMACOKINETIC |
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Tmax | PHARMACOKINETIC |
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ONCE DAILY |
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