Details
Stereochemistry | ACHIRAL |
Molecular Formula | C29H32N6O4S.2ClH |
Molecular Weight | 633.589 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.Cl.CC(C)(C)C1=CC(NC(=O)NC2=CC=C(C=C2)C3=CN4C(SC5=CC(OCCN6CCOCC6)=CC=C45)=N3)=NO1
InChI
InChIKey=DHYPGRVMIOATAE-UHFFFAOYSA-N
InChI=1S/C29H32N6O4S.2ClH/c1-29(2,3)25-17-26(33-39-25)32-27(36)30-20-6-4-19(5-7-20)22-18-35-23-9-8-21(16-24(23)40-28(35)31-22)38-15-12-34-10-13-37-14-11-34;;/h4-9,16-18H,10-15H2,1-3H3,(H2,30,32,33,36);2*1H
Molecular Formula | C29H32N6O4S |
Molecular Weight | 560.667 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
Molecular Formula | ClH |
Molecular Weight | 36.461 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
DescriptionSources: http://adisinsight.springer.com/drugs/800025852Curator's Comment: Description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/19654408 | https://www.ncbi.nlm.nih.gov/pubmed/23497317
Sources: http://adisinsight.springer.com/drugs/800025852
Curator's Comment: Description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/19654408 | https://www.ncbi.nlm.nih.gov/pubmed/23497317
Quizartinib (AC220) is an orally bioavailable, small molecule receptor tyrosine kinase inhibitor that is being developed by Daiichi Sankyo Company (previously Ambit Biosciences) and Astellas Pharma as a treatment for acute myeloid leukaemia (AML), acute lymphoblastic leukaemia (ALL) and advanced solid tumours. The highest affinity target identified for Quizartinib was FLT3. The only other kinases with binding constants within 10-fold that for FLT3 were the closely related receptor tyrosine kinases KIT, PDGFRA, PDGFRB, RET, and CSF1R. Kinase inhibition of (mutant) KIT, PDGFR and FLT3 isoforms by quizartinib leads to potent inhibition of cellular proliferation and induction of apoptosis in in vitro leukemia models as well as in native leukemia blasts treated ex vivo.
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
1.6 nM [Kd] | |||
Target ID: CHEMBL1936 |
4.8 nM [Kd] | ||
Target ID: CHEMBL2007 |
11.0 nM [Kd] | ||
Target ID: CHEMBL1913 Sources: https://www.ncbi.nlm.nih.gov/pubmed/19654408 |
7.7 nM [Kd] | ||
Target ID: CHEMBL2041 Sources: https://www.ncbi.nlm.nih.gov/pubmed/19654408 |
9.9 nM [Kd] | ||
Target ID: CHEMBL1844 Sources: https://www.ncbi.nlm.nih.gov/pubmed/19654408 |
12.0 nM [Kd] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | Unknown Approved UseUnknown |
|||
Primary | Unknown Approved UseUnknown |
|||
Primary | Unknown Approved UseUnknown |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
400 ng × eq/g EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/27460866 |
60 mg single, oral dose: 60 mg route of administration: Oral experiment type: SINGLE co-administered: |
QUIZARTINIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
10000 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/24002496 |
300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered: |
QUIZARTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
1.5 day EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/24002496 |
300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered: |
QUIZARTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
Doses
Dose | Population | Adverse events |
---|---|---|
90 mg 1 times / day multiple, oral MTD Dose: 90 mg, 1 times / day Route: oral Route: multiple Dose: 90 mg, 1 times / day Sources: |
unhealthy, Median age 49.5 years n = 8 Health Status: unhealthy Condition: solid tumors Age Group: Median age 49.5 years Sex: M+F Population Size: 8 Sources: |
Other AEs: Hyperglycemia, Fatigue... Other AEs: Hyperglycemia (25%) Sources: Fatigue (62.5%) Dysgeusia (25%) Nausea (37.5%) Vomiting (25%) Edema peripheral (25%) Peripheral sensory neuropathy (12.5%) Anemia (25%) Neutropenia (25%) Electrocardiogram QT prolonged (12.5%) Tumor pain (12.5%) Abdominal distension (12.5%) Leukopenia (12.5%) Thrombocytopenia (12.5%) Dyspnea (12.5%) Pain in extremity (12.5%) |
250 mg 1 times / day multiple, oral (mean) Dose: 250 mg, 1 times / day Route: oral Route: multiple Dose: 250 mg, 1 times / day Sources: |
unhealthy, Median age 52 years n = 25 Health Status: unhealthy Condition: acute myeloid leukemia Age Group: Median age 52 years Sex: M+F Population Size: 25 Sources: |
Other AEs: Fatigue, Photosensitivity... Other AEs: Fatigue (grade 3, 4%) Sources: Photosensitivity (grade 3, 4%) Thrombocytopenia (grade 3, 4%) |
300 mg 1 times / day multiple, oral Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: |
unhealthy, Median age 52 years n = 8 Health Status: unhealthy Condition: acute myeloid leukemia Age Group: Median age 52 years Sex: M+F Population Size: 8 Sources: |
DLT: Electrocardiogram QTc interval prolonged... Dose limiting toxicities: Electrocardiogram QTc interval prolonged (grade 3, 38%) Sources: |
200 mg 1 times / day multiple, oral MTD Dose: 200 mg, 1 times / day Route: oral Route: multiple Dose: 200 mg, 1 times / day Sources: |
unhealthy, Median age 52.4 years n = 17 Health Status: unhealthy Condition: acute myeloid leukemia Age Group: Median age 52.4 years Sex: M+F Population Size: 17 Sources: |
DLT: Electrocardiogram QTc interval prolonged... Dose limiting toxicities: Electrocardiogram QTc interval prolonged (grade 3, 24%) Sources: |
60 mg 1 times / day multiple, oral Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, Median age 55 years n = 241 Health Status: unhealthy Condition: acute myeloid leukaemia Age Group: Median age 55 years Sex: M+F Population Size: 241 Sources: |
Disc. AE: Pneumonia, Intracranial haemorrhage... Other AEs: Nausea, Fatigue... AEs leading to discontinuation/dose reduction: Pneumonia (2%) Other AEs:Intracranial haemorrhage (2%) Graft versus host disease (2%) Septic shock (2%) QT interval prolonged (grade 2, 1%) QT interval prolonged (5%) QT interval prolonged (9%) Nausea (grade 3, 2%) Sources: Fatigue (grade 3, 8%) Thrombocytopenia (grade 3, 5%) Thrombocytopenia (grade 4, 30%) Thrombocytopenia (grade 5, <1%) Pyrexia (grade 3, 2%) Musculoskeletal pain (grade 3, 4%) Anaemia (grade 3, 29%) Anaemia (grade 4, 1%) Febrile neutropenia (grade 3, 28%) Febrile neutropenia (grade 4, 2%) Neutropenia (grade 3, 5%) Neutropenia (grade 4, 27%) Vomiting (grade 3, 3%) Hypokalaemia (grade 3, 11%) Hypokalaemia (grade 4, 1%) Diarrhoea (grade 3, 2%) Electrocardiogram QT prolonged (grade 3, 4%) Cough (grade 3, <1%) Rash (grade 3, 2%) Abdominal pain (grade 3, 2%) Headache (grade 3, <1%) Septic shock (grade 3, 11%) Septic shock (grade 4, 6%) Septic shock (grade 5, 2%) Oedema peripheral (grade 3, 3%) Decreased appetite (grade 3, 2%) Dyspnoea (grade 3, 5%) Dyspnoea (grade 4, <1%) White blood cell count decreased (grade 3, 5%) White blood cell count decreased (grade 4, 12%) Stomatitis (grade 3, 2%) Stomatitis (grade 4, <1%) Pneumonia (grade 3, 7%) Pneumonia (grade 4, 1%) Pneumonia (grade 5, 4%) ALT increased (grade 3, 4%) Hypotension (grade 3, 3%) Hypotension (grade 4, <1%) Graft versus host disease (grade 3, 3%) Graft versus host disease (grade 4, 1%) Graft versus host disease (grade 5, 1%) Hypocalcaemia (grade 3, <1%) Petechiae (grade 3, 1%) Weight decreased (grade 3, 1%) Hypophosphataemia (grade 3, 4%) Hypophosphataemia (grade 4, <1%) Hyponatremia (grade 3, 3%) Hyponatremia (grade 4, <1%) Urinary tract infection (grade 3, 4%) Urinary tract infection (grade 4, <1%) Upper respiratory tract infection (grade 3, 2%) Cellulitis (grade 3, 3%) Hyperglycaemia (grade 3, 1%) Hyperglycaemia (grade 4, 1%) Leukocytosis (grade 3, 2%) Leukocytosis (grade 4, 1%) Leukocytosis (grade 5, <1%) Acute renal failure (grade 3, 1%) Acute renal failure (grade 4, <1%) Acute renal failure (grade 5) Pancytopenia (grade 3, 5%) Syncope (grade 3, 4%) Clostridioides difficile infection (grade 3, 2%) Clostridioides difficile infection (grade 4, <1%) Device related infection (grade 3, 3%) Lymphocyte count decreased (grade 3, 2%) Lymphocyte count decreased (grade 4, 1%) Intracranial haemorrhage (grade 4, 1%) Intracranial haemorrhage (grade 5, 2%) Pneumonia fungal (grade 3, 2%) Respiratory distress (grade 3, 1%) Respiratory distress (grade 4, <1%) Respiratory distress (grade 5, 1%) |
135 mg 1 times / day multiple, oral Dose: 135 mg, 1 times / day Route: oral Route: multiple Dose: 135 mg, 1 times / day Sources: |
unhealthy, Median age 56 years n = 5 Health Status: unhealthy Condition: solid tumors Age Group: Median age 56 years Sex: M+F Population Size: 5 Sources: |
DLT: Pancytopenia, Electrocardiogram QT prolonged... Dose limiting toxicities: Pancytopenia (grade 3, 20%) Sources: Electrocardiogram QT prolonged (grade 3, 20%) Febrile neutropenia (20%) |
450 mg 1 times / day multiple, oral Highest studied dose Dose: 450 mg, 1 times / day Route: oral Route: multiple Dose: 450 mg, 1 times / day Sources: |
unhealthy, Median age 57.8 years n = 6 Health Status: unhealthy Condition: acute myeloid leukemia Age Group: Median age 57.8 years Sex: M+F Population Size: 6 Sources: |
Other AEs: Electrocardiogram QTc interval prolonged... Other AEs: Electrocardiogram QTc interval prolonged (33.3%) Sources: |
73.5 mg 1 times / day multiple, oral (mean) Dose: 73.5 mg, 1 times / day Route: oral Route: multiple Dose: 73.5 mg, 1 times / day Sources: |
unhealthy, Median age 64 years n = 35 Health Status: unhealthy Condition: acute myeloid leukemia Age Group: Median age 64 years Sex: M+F Population Size: 35 Sources: |
Other AEs: Vomiting, Anorexia... Other AEs: Vomiting (grade 3, 3%) Sources: Anorexia (grade 3, 3%) Fatigue (grade 3, 3%) Anemia (grade 3, 6%) Hypocalcemia (grade 3, 3%) Pyrexia (grade 3, 3%) Pancytopenia (grade 3, 3%) |
316.7 mg 1 times / day multiple, oral (mean) Dose: 316.7 mg, 1 times / day Route: oral Route: multiple Dose: 316.7 mg, 1 times / day Sources: |
unhealthy n = 16 Health Status: unhealthy Condition: acute myeloid leukemia Sex: M+F Population Size: 16 Sources: |
Other AEs: Anemia, Eyelid edema... Other AEs: Anemia (grade 3, 6%) Sources: Eyelid edema (grade 3, 6%) Hypoalbuminemia (grade 3, 6%) Lung infection (grade 3, 6%) |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Abdominal distension | 12.5% | 90 mg 1 times / day multiple, oral MTD Dose: 90 mg, 1 times / day Route: oral Route: multiple Dose: 90 mg, 1 times / day Sources: |
unhealthy, Median age 49.5 years n = 8 Health Status: unhealthy Condition: solid tumors Age Group: Median age 49.5 years Sex: M+F Population Size: 8 Sources: |
Dyspnea | 12.5% | 90 mg 1 times / day multiple, oral MTD Dose: 90 mg, 1 times / day Route: oral Route: multiple Dose: 90 mg, 1 times / day Sources: |
unhealthy, Median age 49.5 years n = 8 Health Status: unhealthy Condition: solid tumors Age Group: Median age 49.5 years Sex: M+F Population Size: 8 Sources: |
Electrocardiogram QT prolonged | 12.5% | 90 mg 1 times / day multiple, oral MTD Dose: 90 mg, 1 times / day Route: oral Route: multiple Dose: 90 mg, 1 times / day Sources: |
unhealthy, Median age 49.5 years n = 8 Health Status: unhealthy Condition: solid tumors Age Group: Median age 49.5 years Sex: M+F Population Size: 8 Sources: |
Leukopenia | 12.5% | 90 mg 1 times / day multiple, oral MTD Dose: 90 mg, 1 times / day Route: oral Route: multiple Dose: 90 mg, 1 times / day Sources: |
unhealthy, Median age 49.5 years n = 8 Health Status: unhealthy Condition: solid tumors Age Group: Median age 49.5 years Sex: M+F Population Size: 8 Sources: |
Pain in extremity | 12.5% | 90 mg 1 times / day multiple, oral MTD Dose: 90 mg, 1 times / day Route: oral Route: multiple Dose: 90 mg, 1 times / day Sources: |
unhealthy, Median age 49.5 years n = 8 Health Status: unhealthy Condition: solid tumors Age Group: Median age 49.5 years Sex: M+F Population Size: 8 Sources: |
Peripheral sensory neuropathy | 12.5% | 90 mg 1 times / day multiple, oral MTD Dose: 90 mg, 1 times / day Route: oral Route: multiple Dose: 90 mg, 1 times / day Sources: |
unhealthy, Median age 49.5 years n = 8 Health Status: unhealthy Condition: solid tumors Age Group: Median age 49.5 years Sex: M+F Population Size: 8 Sources: |
Thrombocytopenia | 12.5% | 90 mg 1 times / day multiple, oral MTD Dose: 90 mg, 1 times / day Route: oral Route: multiple Dose: 90 mg, 1 times / day Sources: |
unhealthy, Median age 49.5 years n = 8 Health Status: unhealthy Condition: solid tumors Age Group: Median age 49.5 years Sex: M+F Population Size: 8 Sources: |
Tumor pain | 12.5% | 90 mg 1 times / day multiple, oral MTD Dose: 90 mg, 1 times / day Route: oral Route: multiple Dose: 90 mg, 1 times / day Sources: |
unhealthy, Median age 49.5 years n = 8 Health Status: unhealthy Condition: solid tumors Age Group: Median age 49.5 years Sex: M+F Population Size: 8 Sources: |
Anemia | 25% | 90 mg 1 times / day multiple, oral MTD Dose: 90 mg, 1 times / day Route: oral Route: multiple Dose: 90 mg, 1 times / day Sources: |
unhealthy, Median age 49.5 years n = 8 Health Status: unhealthy Condition: solid tumors Age Group: Median age 49.5 years Sex: M+F Population Size: 8 Sources: |
Dysgeusia | 25% | 90 mg 1 times / day multiple, oral MTD Dose: 90 mg, 1 times / day Route: oral Route: multiple Dose: 90 mg, 1 times / day Sources: |
unhealthy, Median age 49.5 years n = 8 Health Status: unhealthy Condition: solid tumors Age Group: Median age 49.5 years Sex: M+F Population Size: 8 Sources: |
Edema peripheral | 25% | 90 mg 1 times / day multiple, oral MTD Dose: 90 mg, 1 times / day Route: oral Route: multiple Dose: 90 mg, 1 times / day Sources: |
unhealthy, Median age 49.5 years n = 8 Health Status: unhealthy Condition: solid tumors Age Group: Median age 49.5 years Sex: M+F Population Size: 8 Sources: |
Hyperglycemia | 25% | 90 mg 1 times / day multiple, oral MTD Dose: 90 mg, 1 times / day Route: oral Route: multiple Dose: 90 mg, 1 times / day Sources: |
unhealthy, Median age 49.5 years n = 8 Health Status: unhealthy Condition: solid tumors Age Group: Median age 49.5 years Sex: M+F Population Size: 8 Sources: |
Neutropenia | 25% | 90 mg 1 times / day multiple, oral MTD Dose: 90 mg, 1 times / day Route: oral Route: multiple Dose: 90 mg, 1 times / day Sources: |
unhealthy, Median age 49.5 years n = 8 Health Status: unhealthy Condition: solid tumors Age Group: Median age 49.5 years Sex: M+F Population Size: 8 Sources: |
Vomiting | 25% | 90 mg 1 times / day multiple, oral MTD Dose: 90 mg, 1 times / day Route: oral Route: multiple Dose: 90 mg, 1 times / day Sources: |
unhealthy, Median age 49.5 years n = 8 Health Status: unhealthy Condition: solid tumors Age Group: Median age 49.5 years Sex: M+F Population Size: 8 Sources: |
Nausea | 37.5% | 90 mg 1 times / day multiple, oral MTD Dose: 90 mg, 1 times / day Route: oral Route: multiple Dose: 90 mg, 1 times / day Sources: |
unhealthy, Median age 49.5 years n = 8 Health Status: unhealthy Condition: solid tumors Age Group: Median age 49.5 years Sex: M+F Population Size: 8 Sources: |
Fatigue | 62.5% | 90 mg 1 times / day multiple, oral MTD Dose: 90 mg, 1 times / day Route: oral Route: multiple Dose: 90 mg, 1 times / day Sources: |
unhealthy, Median age 49.5 years n = 8 Health Status: unhealthy Condition: solid tumors Age Group: Median age 49.5 years Sex: M+F Population Size: 8 Sources: |
Fatigue | grade 3, 4% | 250 mg 1 times / day multiple, oral (mean) Dose: 250 mg, 1 times / day Route: oral Route: multiple Dose: 250 mg, 1 times / day Sources: |
unhealthy, Median age 52 years n = 25 Health Status: unhealthy Condition: acute myeloid leukemia Age Group: Median age 52 years Sex: M+F Population Size: 25 Sources: |
Photosensitivity | grade 3, 4% | 250 mg 1 times / day multiple, oral (mean) Dose: 250 mg, 1 times / day Route: oral Route: multiple Dose: 250 mg, 1 times / day Sources: |
unhealthy, Median age 52 years n = 25 Health Status: unhealthy Condition: acute myeloid leukemia Age Group: Median age 52 years Sex: M+F Population Size: 25 Sources: |
Thrombocytopenia | grade 3, 4% | 250 mg 1 times / day multiple, oral (mean) Dose: 250 mg, 1 times / day Route: oral Route: multiple Dose: 250 mg, 1 times / day Sources: |
unhealthy, Median age 52 years n = 25 Health Status: unhealthy Condition: acute myeloid leukemia Age Group: Median age 52 years Sex: M+F Population Size: 25 Sources: |
Electrocardiogram QTc interval prolonged | grade 3, 38% DLT |
300 mg 1 times / day multiple, oral Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: |
unhealthy, Median age 52 years n = 8 Health Status: unhealthy Condition: acute myeloid leukemia Age Group: Median age 52 years Sex: M+F Population Size: 8 Sources: |
Electrocardiogram QTc interval prolonged | grade 3, 24% DLT |
200 mg 1 times / day multiple, oral MTD Dose: 200 mg, 1 times / day Route: oral Route: multiple Dose: 200 mg, 1 times / day Sources: |
unhealthy, Median age 52.4 years n = 17 Health Status: unhealthy Condition: acute myeloid leukemia Age Group: Median age 52.4 years Sex: M+F Population Size: 17 Sources: |
Graft versus host disease | 2% Disc. AE |
60 mg 1 times / day multiple, oral Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, Median age 55 years n = 241 Health Status: unhealthy Condition: acute myeloid leukaemia Age Group: Median age 55 years Sex: M+F Population Size: 241 Sources: |
Intracranial haemorrhage | 2% Disc. AE |
60 mg 1 times / day multiple, oral Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, Median age 55 years n = 241 Health Status: unhealthy Condition: acute myeloid leukaemia Age Group: Median age 55 years Sex: M+F Population Size: 241 Sources: |
Pneumonia | 2% Disc. AE |
60 mg 1 times / day multiple, oral Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, Median age 55 years n = 241 Health Status: unhealthy Condition: acute myeloid leukaemia Age Group: Median age 55 years Sex: M+F Population Size: 241 Sources: |
Septic shock | 2% Disc. AE |
60 mg 1 times / day multiple, oral Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, Median age 55 years n = 241 Health Status: unhealthy Condition: acute myeloid leukaemia Age Group: Median age 55 years Sex: M+F Population Size: 241 Sources: |
QT interval prolonged | 5% Disc. AE |
60 mg 1 times / day multiple, oral Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, Median age 55 years n = 241 Health Status: unhealthy Condition: acute myeloid leukaemia Age Group: Median age 55 years Sex: M+F Population Size: 241 Sources: |
QT interval prolonged | 9% Disc. AE |
60 mg 1 times / day multiple, oral Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, Median age 55 years n = 241 Health Status: unhealthy Condition: acute myeloid leukaemia Age Group: Median age 55 years Sex: M+F Population Size: 241 Sources: |
QT interval prolonged | grade 2, 1% Disc. AE |
60 mg 1 times / day multiple, oral Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, Median age 55 years n = 241 Health Status: unhealthy Condition: acute myeloid leukaemia Age Group: Median age 55 years Sex: M+F Population Size: 241 Sources: |
Acute renal failure | grade 3, 1% | 60 mg 1 times / day multiple, oral Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, Median age 55 years n = 241 Health Status: unhealthy Condition: acute myeloid leukaemia Age Group: Median age 55 years Sex: M+F Population Size: 241 Sources: |
Hyperglycaemia | grade 3, 1% | 60 mg 1 times / day multiple, oral Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, Median age 55 years n = 241 Health Status: unhealthy Condition: acute myeloid leukaemia Age Group: Median age 55 years Sex: M+F Population Size: 241 Sources: |
Petechiae | grade 3, 1% | 60 mg 1 times / day multiple, oral Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, Median age 55 years n = 241 Health Status: unhealthy Condition: acute myeloid leukaemia Age Group: Median age 55 years Sex: M+F Population Size: 241 Sources: |
Respiratory distress | grade 3, 1% | 60 mg 1 times / day multiple, oral Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, Median age 55 years n = 241 Health Status: unhealthy Condition: acute myeloid leukaemia Age Group: Median age 55 years Sex: M+F Population Size: 241 Sources: |
Weight decreased | grade 3, 1% | 60 mg 1 times / day multiple, oral Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, Median age 55 years n = 241 Health Status: unhealthy Condition: acute myeloid leukaemia Age Group: Median age 55 years Sex: M+F Population Size: 241 Sources: |
Hypokalaemia | grade 3, 11% | 60 mg 1 times / day multiple, oral Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, Median age 55 years n = 241 Health Status: unhealthy Condition: acute myeloid leukaemia Age Group: Median age 55 years Sex: M+F Population Size: 241 Sources: |
Septic shock | grade 3, 11% | 60 mg 1 times / day multiple, oral Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, Median age 55 years n = 241 Health Status: unhealthy Condition: acute myeloid leukaemia Age Group: Median age 55 years Sex: M+F Population Size: 241 Sources: |
Abdominal pain | grade 3, 2% | 60 mg 1 times / day multiple, oral Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, Median age 55 years n = 241 Health Status: unhealthy Condition: acute myeloid leukaemia Age Group: Median age 55 years Sex: M+F Population Size: 241 Sources: |
Clostridioides difficile infection | grade 3, 2% | 60 mg 1 times / day multiple, oral Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, Median age 55 years n = 241 Health Status: unhealthy Condition: acute myeloid leukaemia Age Group: Median age 55 years Sex: M+F Population Size: 241 Sources: |
Decreased appetite | grade 3, 2% | 60 mg 1 times / day multiple, oral Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, Median age 55 years n = 241 Health Status: unhealthy Condition: acute myeloid leukaemia Age Group: Median age 55 years Sex: M+F Population Size: 241 Sources: |
Diarrhoea | grade 3, 2% | 60 mg 1 times / day multiple, oral Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, Median age 55 years n = 241 Health Status: unhealthy Condition: acute myeloid leukaemia Age Group: Median age 55 years Sex: M+F Population Size: 241 Sources: |
Leukocytosis | grade 3, 2% | 60 mg 1 times / day multiple, oral Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, Median age 55 years n = 241 Health Status: unhealthy Condition: acute myeloid leukaemia Age Group: Median age 55 years Sex: M+F Population Size: 241 Sources: |
Lymphocyte count decreased | grade 3, 2% | 60 mg 1 times / day multiple, oral Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, Median age 55 years n = 241 Health Status: unhealthy Condition: acute myeloid leukaemia Age Group: Median age 55 years Sex: M+F Population Size: 241 Sources: |
Nausea | grade 3, 2% | 60 mg 1 times / day multiple, oral Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, Median age 55 years n = 241 Health Status: unhealthy Condition: acute myeloid leukaemia Age Group: Median age 55 years Sex: M+F Population Size: 241 Sources: |
Pneumonia fungal | grade 3, 2% | 60 mg 1 times / day multiple, oral Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, Median age 55 years n = 241 Health Status: unhealthy Condition: acute myeloid leukaemia Age Group: Median age 55 years Sex: M+F Population Size: 241 Sources: |
Pyrexia | grade 3, 2% | 60 mg 1 times / day multiple, oral Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, Median age 55 years n = 241 Health Status: unhealthy Condition: acute myeloid leukaemia Age Group: Median age 55 years Sex: M+F Population Size: 241 Sources: |
Rash | grade 3, 2% | 60 mg 1 times / day multiple, oral Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, Median age 55 years n = 241 Health Status: unhealthy Condition: acute myeloid leukaemia Age Group: Median age 55 years Sex: M+F Population Size: 241 Sources: |
Stomatitis | grade 3, 2% | 60 mg 1 times / day multiple, oral Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, Median age 55 years n = 241 Health Status: unhealthy Condition: acute myeloid leukaemia Age Group: Median age 55 years Sex: M+F Population Size: 241 Sources: |
Upper respiratory tract infection | grade 3, 2% | 60 mg 1 times / day multiple, oral Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, Median age 55 years n = 241 Health Status: unhealthy Condition: acute myeloid leukaemia Age Group: Median age 55 years Sex: M+F Population Size: 241 Sources: |
Febrile neutropenia | grade 3, 28% | 60 mg 1 times / day multiple, oral Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, Median age 55 years n = 241 Health Status: unhealthy Condition: acute myeloid leukaemia Age Group: Median age 55 years Sex: M+F Population Size: 241 Sources: |
Anaemia | grade 3, 29% | 60 mg 1 times / day multiple, oral Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, Median age 55 years n = 241 Health Status: unhealthy Condition: acute myeloid leukaemia Age Group: Median age 55 years Sex: M+F Population Size: 241 Sources: |
Cellulitis | grade 3, 3% | 60 mg 1 times / day multiple, oral Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, Median age 55 years n = 241 Health Status: unhealthy Condition: acute myeloid leukaemia Age Group: Median age 55 years Sex: M+F Population Size: 241 Sources: |
Device related infection | grade 3, 3% | 60 mg 1 times / day multiple, oral Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, Median age 55 years n = 241 Health Status: unhealthy Condition: acute myeloid leukaemia Age Group: Median age 55 years Sex: M+F Population Size: 241 Sources: |
Graft versus host disease | grade 3, 3% | 60 mg 1 times / day multiple, oral Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, Median age 55 years n = 241 Health Status: unhealthy Condition: acute myeloid leukaemia Age Group: Median age 55 years Sex: M+F Population Size: 241 Sources: |
Hyponatremia | grade 3, 3% | 60 mg 1 times / day multiple, oral Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, Median age 55 years n = 241 Health Status: unhealthy Condition: acute myeloid leukaemia Age Group: Median age 55 years Sex: M+F Population Size: 241 Sources: |
Hypotension | grade 3, 3% | 60 mg 1 times / day multiple, oral Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, Median age 55 years n = 241 Health Status: unhealthy Condition: acute myeloid leukaemia Age Group: Median age 55 years Sex: M+F Population Size: 241 Sources: |
Oedema peripheral | grade 3, 3% | 60 mg 1 times / day multiple, oral Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, Median age 55 years n = 241 Health Status: unhealthy Condition: acute myeloid leukaemia Age Group: Median age 55 years Sex: M+F Population Size: 241 Sources: |
Vomiting | grade 3, 3% | 60 mg 1 times / day multiple, oral Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, Median age 55 years n = 241 Health Status: unhealthy Condition: acute myeloid leukaemia Age Group: Median age 55 years Sex: M+F Population Size: 241 Sources: |
ALT increased | grade 3, 4% | 60 mg 1 times / day multiple, oral Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, Median age 55 years n = 241 Health Status: unhealthy Condition: acute myeloid leukaemia Age Group: Median age 55 years Sex: M+F Population Size: 241 Sources: |
Electrocardiogram QT prolonged | grade 3, 4% | 60 mg 1 times / day multiple, oral Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, Median age 55 years n = 241 Health Status: unhealthy Condition: acute myeloid leukaemia Age Group: Median age 55 years Sex: M+F Population Size: 241 Sources: |
Hypophosphataemia | grade 3, 4% | 60 mg 1 times / day multiple, oral Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, Median age 55 years n = 241 Health Status: unhealthy Condition: acute myeloid leukaemia Age Group: Median age 55 years Sex: M+F Population Size: 241 Sources: |
Musculoskeletal pain | grade 3, 4% | 60 mg 1 times / day multiple, oral Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, Median age 55 years n = 241 Health Status: unhealthy Condition: acute myeloid leukaemia Age Group: Median age 55 years Sex: M+F Population Size: 241 Sources: |
Syncope | grade 3, 4% | 60 mg 1 times / day multiple, oral Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, Median age 55 years n = 241 Health Status: unhealthy Condition: acute myeloid leukaemia Age Group: Median age 55 years Sex: M+F Population Size: 241 Sources: |
Urinary tract infection | grade 3, 4% | 60 mg 1 times / day multiple, oral Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, Median age 55 years n = 241 Health Status: unhealthy Condition: acute myeloid leukaemia Age Group: Median age 55 years Sex: M+F Population Size: 241 Sources: |
Dyspnoea | grade 3, 5% | 60 mg 1 times / day multiple, oral Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, Median age 55 years n = 241 Health Status: unhealthy Condition: acute myeloid leukaemia Age Group: Median age 55 years Sex: M+F Population Size: 241 Sources: |
Neutropenia | grade 3, 5% | 60 mg 1 times / day multiple, oral Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, Median age 55 years n = 241 Health Status: unhealthy Condition: acute myeloid leukaemia Age Group: Median age 55 years Sex: M+F Population Size: 241 Sources: |
Pancytopenia | grade 3, 5% | 60 mg 1 times / day multiple, oral Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, Median age 55 years n = 241 Health Status: unhealthy Condition: acute myeloid leukaemia Age Group: Median age 55 years Sex: M+F Population Size: 241 Sources: |
Thrombocytopenia | grade 3, 5% | 60 mg 1 times / day multiple, oral Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, Median age 55 years n = 241 Health Status: unhealthy Condition: acute myeloid leukaemia Age Group: Median age 55 years Sex: M+F Population Size: 241 Sources: |
White blood cell count decreased | grade 3, 5% | 60 mg 1 times / day multiple, oral Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, Median age 55 years n = 241 Health Status: unhealthy Condition: acute myeloid leukaemia Age Group: Median age 55 years Sex: M+F Population Size: 241 Sources: |
Pneumonia | grade 3, 7% | 60 mg 1 times / day multiple, oral Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, Median age 55 years n = 241 Health Status: unhealthy Condition: acute myeloid leukaemia Age Group: Median age 55 years Sex: M+F Population Size: 241 Sources: |
Fatigue | grade 3, 8% | 60 mg 1 times / day multiple, oral Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, Median age 55 years n = 241 Health Status: unhealthy Condition: acute myeloid leukaemia Age Group: Median age 55 years Sex: M+F Population Size: 241 Sources: |
Cough | grade 3, <1% | 60 mg 1 times / day multiple, oral Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, Median age 55 years n = 241 Health Status: unhealthy Condition: acute myeloid leukaemia Age Group: Median age 55 years Sex: M+F Population Size: 241 Sources: |
Headache | grade 3, <1% | 60 mg 1 times / day multiple, oral Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, Median age 55 years n = 241 Health Status: unhealthy Condition: acute myeloid leukaemia Age Group: Median age 55 years Sex: M+F Population Size: 241 Sources: |
Hypocalcaemia | grade 3, <1% | 60 mg 1 times / day multiple, oral Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, Median age 55 years n = 241 Health Status: unhealthy Condition: acute myeloid leukaemia Age Group: Median age 55 years Sex: M+F Population Size: 241 Sources: |
Anaemia | grade 4, 1% | 60 mg 1 times / day multiple, oral Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, Median age 55 years n = 241 Health Status: unhealthy Condition: acute myeloid leukaemia Age Group: Median age 55 years Sex: M+F Population Size: 241 Sources: |
Graft versus host disease | grade 4, 1% | 60 mg 1 times / day multiple, oral Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, Median age 55 years n = 241 Health Status: unhealthy Condition: acute myeloid leukaemia Age Group: Median age 55 years Sex: M+F Population Size: 241 Sources: |
Hyperglycaemia | grade 4, 1% | 60 mg 1 times / day multiple, oral Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, Median age 55 years n = 241 Health Status: unhealthy Condition: acute myeloid leukaemia Age Group: Median age 55 years Sex: M+F Population Size: 241 Sources: |
Hypokalaemia | grade 4, 1% | 60 mg 1 times / day multiple, oral Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, Median age 55 years n = 241 Health Status: unhealthy Condition: acute myeloid leukaemia Age Group: Median age 55 years Sex: M+F Population Size: 241 Sources: |
Intracranial haemorrhage | grade 4, 1% | 60 mg 1 times / day multiple, oral Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, Median age 55 years n = 241 Health Status: unhealthy Condition: acute myeloid leukaemia Age Group: Median age 55 years Sex: M+F Population Size: 241 Sources: |
Leukocytosis | grade 4, 1% | 60 mg 1 times / day multiple, oral Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, Median age 55 years n = 241 Health Status: unhealthy Condition: acute myeloid leukaemia Age Group: Median age 55 years Sex: M+F Population Size: 241 Sources: |
Lymphocyte count decreased | grade 4, 1% | 60 mg 1 times / day multiple, oral Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, Median age 55 years n = 241 Health Status: unhealthy Condition: acute myeloid leukaemia Age Group: Median age 55 years Sex: M+F Population Size: 241 Sources: |
Pneumonia | grade 4, 1% | 60 mg 1 times / day multiple, oral Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, Median age 55 years n = 241 Health Status: unhealthy Condition: acute myeloid leukaemia Age Group: Median age 55 years Sex: M+F Population Size: 241 Sources: |
White blood cell count decreased | grade 4, 12% | 60 mg 1 times / day multiple, oral Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, Median age 55 years n = 241 Health Status: unhealthy Condition: acute myeloid leukaemia Age Group: Median age 55 years Sex: M+F Population Size: 241 Sources: |
Febrile neutropenia | grade 4, 2% | 60 mg 1 times / day multiple, oral Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, Median age 55 years n = 241 Health Status: unhealthy Condition: acute myeloid leukaemia Age Group: Median age 55 years Sex: M+F Population Size: 241 Sources: |
Neutropenia | grade 4, 27% | 60 mg 1 times / day multiple, oral Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, Median age 55 years n = 241 Health Status: unhealthy Condition: acute myeloid leukaemia Age Group: Median age 55 years Sex: M+F Population Size: 241 Sources: |
Thrombocytopenia | grade 4, 30% | 60 mg 1 times / day multiple, oral Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, Median age 55 years n = 241 Health Status: unhealthy Condition: acute myeloid leukaemia Age Group: Median age 55 years Sex: M+F Population Size: 241 Sources: |
Septic shock | grade 4, 6% | 60 mg 1 times / day multiple, oral Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, Median age 55 years n = 241 Health Status: unhealthy Condition: acute myeloid leukaemia Age Group: Median age 55 years Sex: M+F Population Size: 241 Sources: |
Acute renal failure | grade 4, <1% | 60 mg 1 times / day multiple, oral Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, Median age 55 years n = 241 Health Status: unhealthy Condition: acute myeloid leukaemia Age Group: Median age 55 years Sex: M+F Population Size: 241 Sources: |
Clostridioides difficile infection | grade 4, <1% | 60 mg 1 times / day multiple, oral Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, Median age 55 years n = 241 Health Status: unhealthy Condition: acute myeloid leukaemia Age Group: Median age 55 years Sex: M+F Population Size: 241 Sources: |
Dyspnoea | grade 4, <1% | 60 mg 1 times / day multiple, oral Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, Median age 55 years n = 241 Health Status: unhealthy Condition: acute myeloid leukaemia Age Group: Median age 55 years Sex: M+F Population Size: 241 Sources: |
Hyponatremia | grade 4, <1% | 60 mg 1 times / day multiple, oral Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, Median age 55 years n = 241 Health Status: unhealthy Condition: acute myeloid leukaemia Age Group: Median age 55 years Sex: M+F Population Size: 241 Sources: |
Hypophosphataemia | grade 4, <1% | 60 mg 1 times / day multiple, oral Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, Median age 55 years n = 241 Health Status: unhealthy Condition: acute myeloid leukaemia Age Group: Median age 55 years Sex: M+F Population Size: 241 Sources: |
Hypotension | grade 4, <1% | 60 mg 1 times / day multiple, oral Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, Median age 55 years n = 241 Health Status: unhealthy Condition: acute myeloid leukaemia Age Group: Median age 55 years Sex: M+F Population Size: 241 Sources: |
Respiratory distress | grade 4, <1% | 60 mg 1 times / day multiple, oral Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, Median age 55 years n = 241 Health Status: unhealthy Condition: acute myeloid leukaemia Age Group: Median age 55 years Sex: M+F Population Size: 241 Sources: |
Stomatitis | grade 4, <1% | 60 mg 1 times / day multiple, oral Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, Median age 55 years n = 241 Health Status: unhealthy Condition: acute myeloid leukaemia Age Group: Median age 55 years Sex: M+F Population Size: 241 Sources: |
Urinary tract infection | grade 4, <1% | 60 mg 1 times / day multiple, oral Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, Median age 55 years n = 241 Health Status: unhealthy Condition: acute myeloid leukaemia Age Group: Median age 55 years Sex: M+F Population Size: 241 Sources: |
Acute renal failure | grade 5 | 60 mg 1 times / day multiple, oral Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, Median age 55 years n = 241 Health Status: unhealthy Condition: acute myeloid leukaemia Age Group: Median age 55 years Sex: M+F Population Size: 241 Sources: |
Graft versus host disease | grade 5, 1% | 60 mg 1 times / day multiple, oral Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, Median age 55 years n = 241 Health Status: unhealthy Condition: acute myeloid leukaemia Age Group: Median age 55 years Sex: M+F Population Size: 241 Sources: |
Respiratory distress | grade 5, 1% | 60 mg 1 times / day multiple, oral Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, Median age 55 years n = 241 Health Status: unhealthy Condition: acute myeloid leukaemia Age Group: Median age 55 years Sex: M+F Population Size: 241 Sources: |
Intracranial haemorrhage | grade 5, 2% | 60 mg 1 times / day multiple, oral Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, Median age 55 years n = 241 Health Status: unhealthy Condition: acute myeloid leukaemia Age Group: Median age 55 years Sex: M+F Population Size: 241 Sources: |
Septic shock | grade 5, 2% | 60 mg 1 times / day multiple, oral Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, Median age 55 years n = 241 Health Status: unhealthy Condition: acute myeloid leukaemia Age Group: Median age 55 years Sex: M+F Population Size: 241 Sources: |
Pneumonia | grade 5, 4% | 60 mg 1 times / day multiple, oral Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, Median age 55 years n = 241 Health Status: unhealthy Condition: acute myeloid leukaemia Age Group: Median age 55 years Sex: M+F Population Size: 241 Sources: |
Leukocytosis | grade 5, <1% | 60 mg 1 times / day multiple, oral Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, Median age 55 years n = 241 Health Status: unhealthy Condition: acute myeloid leukaemia Age Group: Median age 55 years Sex: M+F Population Size: 241 Sources: |
Thrombocytopenia | grade 5, <1% | 60 mg 1 times / day multiple, oral Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, Median age 55 years n = 241 Health Status: unhealthy Condition: acute myeloid leukaemia Age Group: Median age 55 years Sex: M+F Population Size: 241 Sources: |
Febrile neutropenia | 20% DLT |
135 mg 1 times / day multiple, oral Dose: 135 mg, 1 times / day Route: oral Route: multiple Dose: 135 mg, 1 times / day Sources: |
unhealthy, Median age 56 years n = 5 Health Status: unhealthy Condition: solid tumors Age Group: Median age 56 years Sex: M+F Population Size: 5 Sources: |
Electrocardiogram QT prolonged | grade 3, 20% DLT, Disc. AE |
135 mg 1 times / day multiple, oral Dose: 135 mg, 1 times / day Route: oral Route: multiple Dose: 135 mg, 1 times / day Sources: |
unhealthy, Median age 56 years n = 5 Health Status: unhealthy Condition: solid tumors Age Group: Median age 56 years Sex: M+F Population Size: 5 Sources: |
Pancytopenia | grade 3, 20% DLT, Disc. AE |
135 mg 1 times / day multiple, oral Dose: 135 mg, 1 times / day Route: oral Route: multiple Dose: 135 mg, 1 times / day Sources: |
unhealthy, Median age 56 years n = 5 Health Status: unhealthy Condition: solid tumors Age Group: Median age 56 years Sex: M+F Population Size: 5 Sources: |
Electrocardiogram QTc interval prolonged | 33.3% | 450 mg 1 times / day multiple, oral Highest studied dose Dose: 450 mg, 1 times / day Route: oral Route: multiple Dose: 450 mg, 1 times / day Sources: |
unhealthy, Median age 57.8 years n = 6 Health Status: unhealthy Condition: acute myeloid leukemia Age Group: Median age 57.8 years Sex: M+F Population Size: 6 Sources: |
Anorexia | grade 3, 3% | 73.5 mg 1 times / day multiple, oral (mean) Dose: 73.5 mg, 1 times / day Route: oral Route: multiple Dose: 73.5 mg, 1 times / day Sources: |
unhealthy, Median age 64 years n = 35 Health Status: unhealthy Condition: acute myeloid leukemia Age Group: Median age 64 years Sex: M+F Population Size: 35 Sources: |
Fatigue | grade 3, 3% | 73.5 mg 1 times / day multiple, oral (mean) Dose: 73.5 mg, 1 times / day Route: oral Route: multiple Dose: 73.5 mg, 1 times / day Sources: |
unhealthy, Median age 64 years n = 35 Health Status: unhealthy Condition: acute myeloid leukemia Age Group: Median age 64 years Sex: M+F Population Size: 35 Sources: |
Hypocalcemia | grade 3, 3% | 73.5 mg 1 times / day multiple, oral (mean) Dose: 73.5 mg, 1 times / day Route: oral Route: multiple Dose: 73.5 mg, 1 times / day Sources: |
unhealthy, Median age 64 years n = 35 Health Status: unhealthy Condition: acute myeloid leukemia Age Group: Median age 64 years Sex: M+F Population Size: 35 Sources: |
Pancytopenia | grade 3, 3% | 73.5 mg 1 times / day multiple, oral (mean) Dose: 73.5 mg, 1 times / day Route: oral Route: multiple Dose: 73.5 mg, 1 times / day Sources: |
unhealthy, Median age 64 years n = 35 Health Status: unhealthy Condition: acute myeloid leukemia Age Group: Median age 64 years Sex: M+F Population Size: 35 Sources: |
Pyrexia | grade 3, 3% | 73.5 mg 1 times / day multiple, oral (mean) Dose: 73.5 mg, 1 times / day Route: oral Route: multiple Dose: 73.5 mg, 1 times / day Sources: |
unhealthy, Median age 64 years n = 35 Health Status: unhealthy Condition: acute myeloid leukemia Age Group: Median age 64 years Sex: M+F Population Size: 35 Sources: |
Vomiting | grade 3, 3% | 73.5 mg 1 times / day multiple, oral (mean) Dose: 73.5 mg, 1 times / day Route: oral Route: multiple Dose: 73.5 mg, 1 times / day Sources: |
unhealthy, Median age 64 years n = 35 Health Status: unhealthy Condition: acute myeloid leukemia Age Group: Median age 64 years Sex: M+F Population Size: 35 Sources: |
Anemia | grade 3, 6% | 73.5 mg 1 times / day multiple, oral (mean) Dose: 73.5 mg, 1 times / day Route: oral Route: multiple Dose: 73.5 mg, 1 times / day Sources: |
unhealthy, Median age 64 years n = 35 Health Status: unhealthy Condition: acute myeloid leukemia Age Group: Median age 64 years Sex: M+F Population Size: 35 Sources: |
Anemia | grade 3, 6% | 316.7 mg 1 times / day multiple, oral (mean) Dose: 316.7 mg, 1 times / day Route: oral Route: multiple Dose: 316.7 mg, 1 times / day Sources: |
unhealthy n = 16 Health Status: unhealthy Condition: acute myeloid leukemia Sex: M+F Population Size: 16 Sources: |
Eyelid edema | grade 3, 6% | 316.7 mg 1 times / day multiple, oral (mean) Dose: 316.7 mg, 1 times / day Route: oral Route: multiple Dose: 316.7 mg, 1 times / day Sources: |
unhealthy n = 16 Health Status: unhealthy Condition: acute myeloid leukemia Sex: M+F Population Size: 16 Sources: |
Hypoalbuminemia | grade 3, 6% | 316.7 mg 1 times / day multiple, oral (mean) Dose: 316.7 mg, 1 times / day Route: oral Route: multiple Dose: 316.7 mg, 1 times / day Sources: |
unhealthy n = 16 Health Status: unhealthy Condition: acute myeloid leukemia Sex: M+F Population Size: 16 Sources: |
Lung infection | grade 3, 6% | 316.7 mg 1 times / day multiple, oral (mean) Dose: 316.7 mg, 1 times / day Route: oral Route: multiple Dose: 316.7 mg, 1 times / day Sources: |
unhealthy n = 16 Health Status: unhealthy Condition: acute myeloid leukemia Sex: M+F Population Size: 16 Sources: |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Page: - |
yes | |||
Sources: https://www.fda.gov/media/124897/download#page=39 Page: - |
yes |
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Sources: https://www.fda.gov/media/124897/download#page=39 Page: - |
yes | |||
Sources: https://www.fda.gov/media/124897/download#page=39 Page: - |
yes | |||
Sources: https://www.fda.gov/media/124897/download#page=13 Page: - |
yes | yes (co-administration study) Comment: The PBPK results indicated that coadministration of rifampin, a strong CYP3A inducer, with quizartinib would result in an approximately 72% decrease in quizartinib exposure and an approximately 66% decrease in AC886 exposure (AUCinf) Sources: https://www.fda.gov/media/124897/download#page=13 Page: - |
||
Page: - |
yes | yes (co-administration study) Comment: Steady‐state PK simulation demonstrated ~2‐fold increase of both steady–state Cmax and AUC from time 0 to the end of the dosing interval when quizartinib was administered with ketoconazole due to accumulation of quizartinib at steady state. When administered with fluconazole, geometric mean ratios (90% confidence interval) for quizartinib Cmax and AUC from time 0 extrapolated to infinity were 111% (100%, 124%) and 120% (104%, 138%), respectively, vs quizartinib alone. Page: - |
Tox targets
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Sources: https://www.fda.gov/media/124897/download#page=39 Page: - |
PubMed
Title | Date | PubMed |
---|---|---|
Identification of N-(5-tert-butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea dihydrochloride (AC220), a uniquely potent, selective, and efficacious FMS-like tyrosine kinase-3 (FLT3) inhibitor. | 2009 Dec 10 |
|
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). | 2009 Oct 1 |
|
Activation state-dependent binding of small molecule kinase inhibitors: structural insights from biochemistry. | 2010 Nov 24 |
|
Design, synthesis, and evaluation of a novel dual FMS-like tyrosine kinase 3/stem cell factor receptor (FLT3/c-KIT) inhibitor for the treatment of acute myelogenous leukemia. | 2011 Oct 27 |
|
Comprehensive analysis of kinase inhibitor selectivity. | 2011 Oct 30 |
|
BET protein antagonist JQ1 is synergistically lethal with FLT3 tyrosine kinase inhibitor (TKI) and overcomes resistance to FLT3-TKI in AML cells expressing FLT-ITD. | 2014 Oct |
Sample Use Guides
60 mg daily was selected as the highest dose for continuous daily administration based on Phase 2 study data in relapsed or refractory acute myeloid leukaemia patients. Quizartinib was well tolerated at daily doses ≤ 200 mg/day in patients with relapsed or refractory acute myeloid leukaemia patients (Phase I study).
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/23412931
Both of the FLT3-ITD cell lines, MV4-11 and MOLM-14, were exquisitely sensitive to quizartinib treatment with cell viability IC50 values of 0.1 to 0.3 nmol/L measured at 72 hours. Interestingly, while an IC50 of 0.4 nmol/L could be measured after 72 hours in SEM-K2 cells, complete loss of viability required 5 to 7 days. In contrast, minimal or no loss of viability was observed in the FLT3-WT–expressing RS4;11 and THP-1 cells, even following 7 days of quizartinib treatment, consistent with reports that these lines are not dependent on FLT3 signaling for sustained cell growth
Substance Class |
Chemical
Created
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Fri Dec 15 19:47:05 GMT 2023
by
admin
on
Fri Dec 15 19:47:05 GMT 2023
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Record UNII |
WK7Q6ZIZ10
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Validated (UNII)
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Classification Tree | Code System | Code | ||
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EU-Orphan Drug |
MM Test
Created by
admin on Fri Dec 15 19:47:05 GMT 2023 , Edited by admin on Fri Dec 15 19:47:05 GMT 2023
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FDA ORPHAN DRUG |
277109
Created by
admin on Fri Dec 15 19:47:05 GMT 2023 , Edited by admin on Fri Dec 15 19:47:05 GMT 2023
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NCI_THESAURUS |
C1967
Created by
admin on Fri Dec 15 19:47:05 GMT 2023 , Edited by admin on Fri Dec 15 19:47:05 GMT 2023
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EU-Orphan Drug |
EU/3/09/622
Created by
admin on Fri Dec 15 19:47:05 GMT 2023 , Edited by admin on Fri Dec 15 19:47:05 GMT 2023
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25184035
Created by
admin on Fri Dec 15 19:47:05 GMT 2023 , Edited by admin on Fri Dec 15 19:47:05 GMT 2023
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DTXSID30150345
Created by
admin on Fri Dec 15 19:47:05 GMT 2023 , Edited by admin on Fri Dec 15 19:47:05 GMT 2023
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WK7Q6ZIZ10
Created by
admin on Fri Dec 15 19:47:05 GMT 2023 , Edited by admin on Fri Dec 15 19:47:05 GMT 2023
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C97272
Created by
admin on Fri Dec 15 19:47:05 GMT 2023 , Edited by admin on Fri Dec 15 19:47:05 GMT 2023
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XX-13
Created by
admin on Fri Dec 15 19:47:05 GMT 2023 , Edited by admin on Fri Dec 15 19:47:05 GMT 2023
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CHEMBL576982
Created by
admin on Fri Dec 15 19:47:05 GMT 2023 , Edited by admin on Fri Dec 15 19:47:05 GMT 2023
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1132827-21-4
Created by
admin on Fri Dec 15 19:47:05 GMT 2023 , Edited by admin on Fri Dec 15 19:47:05 GMT 2023
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100000178015
Created by
admin on Fri Dec 15 19:47:05 GMT 2023 , Edited by admin on Fri Dec 15 19:47:05 GMT 2023
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