Details
Stereochemistry | ACHIRAL |
Molecular Formula | C22H26ClN7O2S.H2O |
Molecular Weight | 506.021 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
O.CC1=NC(NC2=NC=C(S2)C(=O)NC3=C(C)C=CC=C3Cl)=CC(=N1)N4CCN(CCO)CC4
InChI
InChIKey=XHXFZZNHDVTMLI-UHFFFAOYSA-N
InChI=1S/C22H26ClN7O2S.H2O/c1-14-4-3-5-16(23)20(14)28-21(32)17-13-24-22(33-17)27-18-12-19(26-15(2)25-18)30-8-6-29(7-9-30)10-11-31;/h3-5,12-13,31H,6-11H2,1-2H3,(H,28,32)(H,24,25,26,27);1H2
Molecular Formula | C22H26ClN7O2S |
Molecular Weight | 488.006 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
Molecular Formula | H2O |
Molecular Weight | 18.0153 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
DescriptionCurator's Comment: description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/16542059
Curator's Comment: description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/16542059
Dasatinib [BMS 354825] is an orally active, small molecule, dual inhibitor of both SRC and ABL kinases that is under development with Bristol-Myers Squibb for the treatment of patients with chronic myelogenous leukaemia (CML) and imatinib-acquired resistance/intolerance. It’s used for the treatment of adults with chronic, accelerated, or myeloid or lymphoid blast phase chronic myeloid leukemia with resistance or intolerance to prior therapy. Also indicated for the treatment of adults with Philadelphia chromosome-positive acute lymphoblastic leukemia with resistance or intolerance to prior therapy. While imatinib remains a frontline therapy for CML, patients with advanced disease frequently develop resistance to imatinib therapy through multiple mechanisms. Dasatinib is also undergoing preclinical evaluation for its potential as a therapy against multiple myeloma. Bristol-Myers Squibb has a composition-of-matter patent covering this research approach that will expire in 2020. Dasatinib, at nanomolar concentrations, inhibits the following kinases: BCR-ABL, SRC family (SRC, LCK, YES, FYN), c-KIT, EPHA2, and PDGFRβ. Based on modeling studies, dasatinib is predicted to bind to multiple conformations of the ABL kinase.
CNS Activity
Originator
Sources: https://www.ncbi.nlm.nih.gov/pubmed/16542059
Curator's Comment: # Bristol-Myers Squibb
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL2363074 Sources: https://www.ncbi.nlm.nih.gov/pubmed/17701954 |
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Target ID: CHEMBL1936 Sources: https://www.ncbi.nlm.nih.gov/pubmed/17701954 |
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Target ID: CHEMBL2068 Sources: https://www.ncbi.nlm.nih.gov/pubmed/17701954 |
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Target ID: CHEMBL1913 Sources: https://www.ncbi.nlm.nih.gov/pubmed/17701954 |
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Target ID: CHEMBL1862 Sources: https://www.ncbi.nlm.nih.gov/pubmed/17701954 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | SPRYCEL Approved UseSPRYCEL® (dasatinib) is indicated for the treatment of adults with newly diagnosed Philadelphia chromosome-positive (Ph+) chronic myeloid leukemia (CML) in chronic phase. The effectiveness of SPRYCEL is based on cytogenetic response and major molecular response rates [see Clinical Studies (14.1) Launch Date2006 |
|||
Primary | SPRYCEL Approved UseSPRYCEL® (dasatinib) is indicated for the treatment of adults with newly diagnosed Philadelphia chromosome-positive (Ph+) chronic myeloid leukemia (CML) in chronic phase. The effectiveness of SPRYCEL is based on cytogenetic response and major molecular response rates [see Clinical Studies (14.1) Launch Date2006 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
139.65 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/37789147/ |
140 mg single, oral dose: 140 mg route of administration: Oral experiment type: SINGLE co-administered: |
DASATINIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
82.2 ng/mL |
100 mg 1 times / day steady-state, oral dose: 100 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
DASATINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
499.45 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/37789147/ |
140 mg single, oral dose: 140 mg route of administration: Oral experiment type: SINGLE co-administered: |
DASATINIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
397 ng × h/mL |
100 mg 1 times / day steady-state, oral dose: 100 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
DASATINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
5 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/37789147/ |
140 mg single, oral dose: 140 mg route of administration: Oral experiment type: SINGLE co-administered: |
DASATINIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
3 h |
100 mg 1 times / day steady-state, oral dose: 100 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
DASATINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
Funbound
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
6% EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/17429625 |
DASATINIB plasma | Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
Doses
Dose | Population | Adverse events |
---|---|---|
90 mg 2 times / day steady, oral Higher than recommended Dose: 90 mg, 2 times / day Route: oral Route: steady Dose: 90 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
DLT: Dehydration, Hyponatremia... Other AEs: Fatigue, Nausea... Dose limiting toxicities: Dehydration (grade 3, 1 patient) Other AEs:Hyponatremia (grade 3, 1 patient) Fatigue (grade 1-2, 3 patients) Sources: Nausea (grade 1-2, 1 patient) Diarrhea (grade 1-2, 1 patient) Anorexia (grade 1-2, 1 patient) Lethargy (grade 1-2, 2 patients) Headache (grade 1-2, 1 patient) |
160 mg 2 times / day steady, oral Highest studied dose Dose: 160 mg, 2 times / day Route: oral Route: steady Dose: 160 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
DLT: Rash, Lethargy... Other AEs: Nausea, Fatigue... Dose limiting toxicities: Rash (grade 2, 3 patients) Other AEs:Lethargy (grade 3, 3 patients) Bleeding time prolonged (grade 3, 1 patient) Hypocalcemia (grade 3, 1 patient) Nausea (grade 1-2, 4 patients) Sources: Fatigue (grade 1-2, 1 patient) Diarrhea (grade 1-2, 3 patients) Vomiting (grade 1-2, 2 patients) Anorexia (grade 1-2, 2 patients) Lethargy (grade 1-2, 2 patients) Headache (grade 1-2, 1 patient) Pyrexia (grade 1-2, 1 patient) Chills (grade 1-2, 3 patients) Proteinuria (grade 1-2, 2 patients) Anorexia (grade 3-4, 1 patient) Lethargy (grade 3-4, 1 patient) Proteinuria (grade 3-4, 1 patient) |
120 mg 2 times / day steady, oral MTD Dose: 120 mg, 2 times / day Route: oral Route: steady Dose: 120 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
DLT: Tumor lysis syndrome... Other AEs: Nausea, Fatigue... Dose limiting toxicities: Tumor lysis syndrome (grade 3, 1 patient) Other AEs:Nausea (grade 1-2, 7 patients) Sources: Fatigue (grade 1-2, 2 patients) Diarrhea (grade 1-2, 4 patients) Vomiting (grade 1-2, 4 patients) Anorexia (grade 1-2, 1 patient) Lethargy (grade 1-2, 2 patients) Headache (grade 1-2, 2 patients) Pyrexia (grade 1-2, 1 patient) Chills (grade 1-2, 1 patient) Proteinuria (grade 1-2, 1 patient) Nausea (grade 3-4, 1 patient) Vomiting (grade 3-4, 1 patient) |
70 mg 2 times / day steady, oral MTD Dose: 70 mg, 2 times / day Route: oral Route: steady Dose: 70 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Other AEs: Nausea, Anorexia... Other AEs: Nausea (grade 1-2, 2 patients) Sources: Anorexia (grade 1-2, 4 patients) Fatigue (grade 1-2, 1 patient) Diarrhea (grade 1-2, 1 patient) Lethargy (grade 1-2, 2 patients) Vomiting (grade 1-2, 1 patient) Headache (grade 1-2, 2 patients) |
50 mg 2 times / day steady, oral Recommended Dose: 50 mg, 2 times / day Route: oral Route: steady Dose: 50 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Other AEs: Nausea, Fatigue... Other AEs: Nausea (grade 1-2, 1 patient) Sources: Fatigue (grade 1-2, 2 patients) Diarrhea (grade 1-2, 1 patient) Vomiting (grade 1-2, 1 patient) Anorexia (grade 1-2, 1 patient) Lethargy (grade 1-2, 1 patient) Pyrexia (grade 1-2, 1 patient) |
70 mg 2 times / day steady, oral Recommended Dose: 70 mg, 2 times / day Route: oral Route: steady Dose: 70 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Other AEs: Nausea, Fatigue... Other AEs: Nausea (grade 1-2, 3 patients) Sources: Fatigue (grade 1-2, 3 patients) Diarrhea (grade 1-2, 1 patient) Anorexia (grade 1-2, 2 patients) |
100 mg 2 times / day steady, oral Studied dose Dose: 100 mg, 2 times / day Route: oral Route: steady Dose: 100 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Other AEs: Nausea, Anorexia... Other AEs: Nausea (grade 1-2, 7 patients) Sources: Anorexia (grade 1-2, 9 patients) Fatigue (grade 1-2, 8 patients) Diarrhea (grade 1-2, 6 patients) Lethargy (grade 1-2, 2 patients) Vomiting (grade 1-2, 3 patients) Headache (grade 1-2, 3 patients) Proteinuria (grade 1-2, 4 patients) Rash (grade 1-2, 3 patients) Pruritus (grade 1-2, 2 patients) Anemia (grade 1-2, 2 patients) Dyspnea (grade 1-2, 2 patients) Fatigue (grade 3-4, 1 patient) Lethargy (grade 3-4, 1 patient) Dyspnea (grade 3-4, 1 patient) |
100 mg 2 times / day steady, oral Studied dose Dose: 100 mg, 2 times / day Route: oral Route: steady Dose: 100 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
DLT: Toxic myocarditis, T wave inversion... Dose limiting toxicities: Toxic myocarditis (grade 2, 1 patient) Sources: T wave inversion (grade 2, 1 patient) Cardiac troponin increased (grade 4, 1 patient) Dyspnea (grade 3, 6 patients) Constipation (grade 3, 6 patients) Proteinuria (grade 2, 6 patients) Fatigue (grade 4, 6 patients) Lethargy (grade 3, 6 patients) |
120 mg 2 times / day steady, oral Studied dose Dose: 120 mg, 2 times / day Route: oral Route: steady Dose: 120 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Other AEs: Nausea, Anorexia... Other AEs: Nausea (grade 1-2, 2 patients) Sources: Anorexia (grade 1-2, 2 patients) Fatigue (grade 1-2, 2 patients) Diarrhea (grade 1-2, 1 patient) Headache (grade 1-2, 1 patient) Proteinuria (grade 1-2, 1 patient) Pruritus (grade 1-2, 1 patient) Anemia (grade 1-2, 1 patient) Nausea (grade 3-4, 1 patient) Rash (grade 3-4, 1 patient) Fatigue (grade 3-4, 1 patient) |
120 mg 2 times / day steady, oral Studied dose Dose: 120 mg, 2 times / day Route: oral Route: steady Dose: 120 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
DLT: Nausea, Fatigue... Dose limiting toxicities: Nausea (grade 3, 3 patients) Sources: Fatigue (grade 3, 3 patients) Rash (grade 3, 1 patient) Proteinuria (grade 2, 1 patient) |
35 mg 2 times / day steady, oral Studied dose Dose: 35 mg, 2 times / day Route: oral Route: steady Dose: 35 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
DLT: Anorexia, Dehydration... Other AEs: Nausea, Fatigue... Dose limiting toxicities: Anorexia (grade 3, 1 patient) Other AEs:Dehydration (grade 3, 1 patient) Nausea (grade 1-2, 4 patients) Sources: Fatigue (grade 1-2, 3 patients) Diarrhea (grade 1-2, 3 patients) Vomiting (grade 1-2, 2 patients) Headache (grade 1-2, 1 patient) Pyrexia (grade 1-2, 1 patient) Diarrhea (grade 3-4, 1 patient) Anorexia (grade 3-4, 1 patient) |
90 mg 2 times / day steady, oral Studied dose Dose: 90 mg, 2 times / day Route: oral Route: steady Dose: 90 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Other AEs: Nausea, Anorexia... Other AEs: Nausea (grade 1-2, 4 patients) Sources: Anorexia (grade 1-2, 4 patients) Fatigue (grade 1-2, 2 patients) Diarrhea (grade 1-2, 3 patients) Lethargy (grade 1-2, 3 patients) Vomiting (grade 1-2, 3 patients) Rash (grade 1-2, 2 patients) Pruritus (grade 1-2, 1 patient) Anemia (grade 1-2, 1 patient) Dyspnea (grade 1-2, 1 patient) Proteinuria (grade 3-4, 1 patient) |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Anorexia | grade 1-2, 1 patient | 90 mg 2 times / day steady, oral Higher than recommended Dose: 90 mg, 2 times / day Route: oral Route: steady Dose: 90 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Diarrhea | grade 1-2, 1 patient | 90 mg 2 times / day steady, oral Higher than recommended Dose: 90 mg, 2 times / day Route: oral Route: steady Dose: 90 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Headache | grade 1-2, 1 patient | 90 mg 2 times / day steady, oral Higher than recommended Dose: 90 mg, 2 times / day Route: oral Route: steady Dose: 90 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Nausea | grade 1-2, 1 patient | 90 mg 2 times / day steady, oral Higher than recommended Dose: 90 mg, 2 times / day Route: oral Route: steady Dose: 90 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Lethargy | grade 1-2, 2 patients | 90 mg 2 times / day steady, oral Higher than recommended Dose: 90 mg, 2 times / day Route: oral Route: steady Dose: 90 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Fatigue | grade 1-2, 3 patients | 90 mg 2 times / day steady, oral Higher than recommended Dose: 90 mg, 2 times / day Route: oral Route: steady Dose: 90 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Dehydration | grade 3, 1 patient DLT |
90 mg 2 times / day steady, oral Higher than recommended Dose: 90 mg, 2 times / day Route: oral Route: steady Dose: 90 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Hyponatremia | grade 3, 1 patient DLT |
90 mg 2 times / day steady, oral Higher than recommended Dose: 90 mg, 2 times / day Route: oral Route: steady Dose: 90 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Fatigue | grade 1-2, 1 patient | 160 mg 2 times / day steady, oral Highest studied dose Dose: 160 mg, 2 times / day Route: oral Route: steady Dose: 160 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Headache | grade 1-2, 1 patient | 160 mg 2 times / day steady, oral Highest studied dose Dose: 160 mg, 2 times / day Route: oral Route: steady Dose: 160 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Pyrexia | grade 1-2, 1 patient | 160 mg 2 times / day steady, oral Highest studied dose Dose: 160 mg, 2 times / day Route: oral Route: steady Dose: 160 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Anorexia | grade 1-2, 2 patients | 160 mg 2 times / day steady, oral Highest studied dose Dose: 160 mg, 2 times / day Route: oral Route: steady Dose: 160 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Lethargy | grade 1-2, 2 patients | 160 mg 2 times / day steady, oral Highest studied dose Dose: 160 mg, 2 times / day Route: oral Route: steady Dose: 160 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Proteinuria | grade 1-2, 2 patients | 160 mg 2 times / day steady, oral Highest studied dose Dose: 160 mg, 2 times / day Route: oral Route: steady Dose: 160 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Vomiting | grade 1-2, 2 patients | 160 mg 2 times / day steady, oral Highest studied dose Dose: 160 mg, 2 times / day Route: oral Route: steady Dose: 160 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Chills | grade 1-2, 3 patients | 160 mg 2 times / day steady, oral Highest studied dose Dose: 160 mg, 2 times / day Route: oral Route: steady Dose: 160 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Diarrhea | grade 1-2, 3 patients | 160 mg 2 times / day steady, oral Highest studied dose Dose: 160 mg, 2 times / day Route: oral Route: steady Dose: 160 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Nausea | grade 1-2, 4 patients | 160 mg 2 times / day steady, oral Highest studied dose Dose: 160 mg, 2 times / day Route: oral Route: steady Dose: 160 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Rash | grade 2, 3 patients DLT |
160 mg 2 times / day steady, oral Highest studied dose Dose: 160 mg, 2 times / day Route: oral Route: steady Dose: 160 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Bleeding time prolonged | grade 3, 1 patient DLT |
160 mg 2 times / day steady, oral Highest studied dose Dose: 160 mg, 2 times / day Route: oral Route: steady Dose: 160 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Hypocalcemia | grade 3, 1 patient DLT |
160 mg 2 times / day steady, oral Highest studied dose Dose: 160 mg, 2 times / day Route: oral Route: steady Dose: 160 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Lethargy | grade 3, 3 patients DLT |
160 mg 2 times / day steady, oral Highest studied dose Dose: 160 mg, 2 times / day Route: oral Route: steady Dose: 160 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Anorexia | grade 3-4, 1 patient | 160 mg 2 times / day steady, oral Highest studied dose Dose: 160 mg, 2 times / day Route: oral Route: steady Dose: 160 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Lethargy | grade 3-4, 1 patient | 160 mg 2 times / day steady, oral Highest studied dose Dose: 160 mg, 2 times / day Route: oral Route: steady Dose: 160 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Proteinuria | grade 3-4, 1 patient | 160 mg 2 times / day steady, oral Highest studied dose Dose: 160 mg, 2 times / day Route: oral Route: steady Dose: 160 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Anorexia | grade 1-2, 1 patient | 120 mg 2 times / day steady, oral MTD Dose: 120 mg, 2 times / day Route: oral Route: steady Dose: 120 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Chills | grade 1-2, 1 patient | 120 mg 2 times / day steady, oral MTD Dose: 120 mg, 2 times / day Route: oral Route: steady Dose: 120 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Proteinuria | grade 1-2, 1 patient | 120 mg 2 times / day steady, oral MTD Dose: 120 mg, 2 times / day Route: oral Route: steady Dose: 120 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Pyrexia | grade 1-2, 1 patient | 120 mg 2 times / day steady, oral MTD Dose: 120 mg, 2 times / day Route: oral Route: steady Dose: 120 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Fatigue | grade 1-2, 2 patients | 120 mg 2 times / day steady, oral MTD Dose: 120 mg, 2 times / day Route: oral Route: steady Dose: 120 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Headache | grade 1-2, 2 patients | 120 mg 2 times / day steady, oral MTD Dose: 120 mg, 2 times / day Route: oral Route: steady Dose: 120 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Lethargy | grade 1-2, 2 patients | 120 mg 2 times / day steady, oral MTD Dose: 120 mg, 2 times / day Route: oral Route: steady Dose: 120 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Diarrhea | grade 1-2, 4 patients | 120 mg 2 times / day steady, oral MTD Dose: 120 mg, 2 times / day Route: oral Route: steady Dose: 120 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Vomiting | grade 1-2, 4 patients | 120 mg 2 times / day steady, oral MTD Dose: 120 mg, 2 times / day Route: oral Route: steady Dose: 120 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Nausea | grade 1-2, 7 patients | 120 mg 2 times / day steady, oral MTD Dose: 120 mg, 2 times / day Route: oral Route: steady Dose: 120 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Tumor lysis syndrome | grade 3, 1 patient DLT |
120 mg 2 times / day steady, oral MTD Dose: 120 mg, 2 times / day Route: oral Route: steady Dose: 120 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Nausea | grade 3-4, 1 patient | 120 mg 2 times / day steady, oral MTD Dose: 120 mg, 2 times / day Route: oral Route: steady Dose: 120 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Vomiting | grade 3-4, 1 patient | 120 mg 2 times / day steady, oral MTD Dose: 120 mg, 2 times / day Route: oral Route: steady Dose: 120 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Diarrhea | grade 1-2, 1 patient | 70 mg 2 times / day steady, oral MTD Dose: 70 mg, 2 times / day Route: oral Route: steady Dose: 70 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Fatigue | grade 1-2, 1 patient | 70 mg 2 times / day steady, oral MTD Dose: 70 mg, 2 times / day Route: oral Route: steady Dose: 70 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Vomiting | grade 1-2, 1 patient | 70 mg 2 times / day steady, oral MTD Dose: 70 mg, 2 times / day Route: oral Route: steady Dose: 70 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Headache | grade 1-2, 2 patients | 70 mg 2 times / day steady, oral MTD Dose: 70 mg, 2 times / day Route: oral Route: steady Dose: 70 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Lethargy | grade 1-2, 2 patients | 70 mg 2 times / day steady, oral MTD Dose: 70 mg, 2 times / day Route: oral Route: steady Dose: 70 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Nausea | grade 1-2, 2 patients | 70 mg 2 times / day steady, oral MTD Dose: 70 mg, 2 times / day Route: oral Route: steady Dose: 70 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Anorexia | grade 1-2, 4 patients | 70 mg 2 times / day steady, oral MTD Dose: 70 mg, 2 times / day Route: oral Route: steady Dose: 70 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Anorexia | grade 1-2, 1 patient | 50 mg 2 times / day steady, oral Recommended Dose: 50 mg, 2 times / day Route: oral Route: steady Dose: 50 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Diarrhea | grade 1-2, 1 patient | 50 mg 2 times / day steady, oral Recommended Dose: 50 mg, 2 times / day Route: oral Route: steady Dose: 50 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Lethargy | grade 1-2, 1 patient | 50 mg 2 times / day steady, oral Recommended Dose: 50 mg, 2 times / day Route: oral Route: steady Dose: 50 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Nausea | grade 1-2, 1 patient | 50 mg 2 times / day steady, oral Recommended Dose: 50 mg, 2 times / day Route: oral Route: steady Dose: 50 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Pyrexia | grade 1-2, 1 patient | 50 mg 2 times / day steady, oral Recommended Dose: 50 mg, 2 times / day Route: oral Route: steady Dose: 50 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Vomiting | grade 1-2, 1 patient | 50 mg 2 times / day steady, oral Recommended Dose: 50 mg, 2 times / day Route: oral Route: steady Dose: 50 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Fatigue | grade 1-2, 2 patients | 50 mg 2 times / day steady, oral Recommended Dose: 50 mg, 2 times / day Route: oral Route: steady Dose: 50 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Diarrhea | grade 1-2, 1 patient | 70 mg 2 times / day steady, oral Recommended Dose: 70 mg, 2 times / day Route: oral Route: steady Dose: 70 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Anorexia | grade 1-2, 2 patients | 70 mg 2 times / day steady, oral Recommended Dose: 70 mg, 2 times / day Route: oral Route: steady Dose: 70 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Fatigue | grade 1-2, 3 patients | 70 mg 2 times / day steady, oral Recommended Dose: 70 mg, 2 times / day Route: oral Route: steady Dose: 70 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Nausea | grade 1-2, 3 patients | 70 mg 2 times / day steady, oral Recommended Dose: 70 mg, 2 times / day Route: oral Route: steady Dose: 70 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Anemia | grade 1-2, 2 patients | 100 mg 2 times / day steady, oral Studied dose Dose: 100 mg, 2 times / day Route: oral Route: steady Dose: 100 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Dyspnea | grade 1-2, 2 patients | 100 mg 2 times / day steady, oral Studied dose Dose: 100 mg, 2 times / day Route: oral Route: steady Dose: 100 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Lethargy | grade 1-2, 2 patients | 100 mg 2 times / day steady, oral Studied dose Dose: 100 mg, 2 times / day Route: oral Route: steady Dose: 100 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Pruritus | grade 1-2, 2 patients | 100 mg 2 times / day steady, oral Studied dose Dose: 100 mg, 2 times / day Route: oral Route: steady Dose: 100 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Headache | grade 1-2, 3 patients | 100 mg 2 times / day steady, oral Studied dose Dose: 100 mg, 2 times / day Route: oral Route: steady Dose: 100 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Rash | grade 1-2, 3 patients | 100 mg 2 times / day steady, oral Studied dose Dose: 100 mg, 2 times / day Route: oral Route: steady Dose: 100 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Vomiting | grade 1-2, 3 patients | 100 mg 2 times / day steady, oral Studied dose Dose: 100 mg, 2 times / day Route: oral Route: steady Dose: 100 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Proteinuria | grade 1-2, 4 patients | 100 mg 2 times / day steady, oral Studied dose Dose: 100 mg, 2 times / day Route: oral Route: steady Dose: 100 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Diarrhea | grade 1-2, 6 patients | 100 mg 2 times / day steady, oral Studied dose Dose: 100 mg, 2 times / day Route: oral Route: steady Dose: 100 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Nausea | grade 1-2, 7 patients | 100 mg 2 times / day steady, oral Studied dose Dose: 100 mg, 2 times / day Route: oral Route: steady Dose: 100 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Fatigue | grade 1-2, 8 patients | 100 mg 2 times / day steady, oral Studied dose Dose: 100 mg, 2 times / day Route: oral Route: steady Dose: 100 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Anorexia | grade 1-2, 9 patients | 100 mg 2 times / day steady, oral Studied dose Dose: 100 mg, 2 times / day Route: oral Route: steady Dose: 100 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Dyspnea | grade 3-4, 1 patient | 100 mg 2 times / day steady, oral Studied dose Dose: 100 mg, 2 times / day Route: oral Route: steady Dose: 100 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Fatigue | grade 3-4, 1 patient | 100 mg 2 times / day steady, oral Studied dose Dose: 100 mg, 2 times / day Route: oral Route: steady Dose: 100 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Lethargy | grade 3-4, 1 patient | 100 mg 2 times / day steady, oral Studied dose Dose: 100 mg, 2 times / day Route: oral Route: steady Dose: 100 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
T wave inversion | grade 2, 1 patient DLT |
100 mg 2 times / day steady, oral Studied dose Dose: 100 mg, 2 times / day Route: oral Route: steady Dose: 100 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Toxic myocarditis | grade 2, 1 patient DLT |
100 mg 2 times / day steady, oral Studied dose Dose: 100 mg, 2 times / day Route: oral Route: steady Dose: 100 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Proteinuria | grade 2, 6 patients DLT |
100 mg 2 times / day steady, oral Studied dose Dose: 100 mg, 2 times / day Route: oral Route: steady Dose: 100 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Constipation | grade 3, 6 patients DLT |
100 mg 2 times / day steady, oral Studied dose Dose: 100 mg, 2 times / day Route: oral Route: steady Dose: 100 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Dyspnea | grade 3, 6 patients DLT |
100 mg 2 times / day steady, oral Studied dose Dose: 100 mg, 2 times / day Route: oral Route: steady Dose: 100 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Lethargy | grade 3, 6 patients DLT |
100 mg 2 times / day steady, oral Studied dose Dose: 100 mg, 2 times / day Route: oral Route: steady Dose: 100 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Cardiac troponin increased | grade 4, 1 patient DLT |
100 mg 2 times / day steady, oral Studied dose Dose: 100 mg, 2 times / day Route: oral Route: steady Dose: 100 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Fatigue | grade 4, 6 patients DLT |
100 mg 2 times / day steady, oral Studied dose Dose: 100 mg, 2 times / day Route: oral Route: steady Dose: 100 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Anemia | grade 1-2, 1 patient | 120 mg 2 times / day steady, oral Studied dose Dose: 120 mg, 2 times / day Route: oral Route: steady Dose: 120 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Diarrhea | grade 1-2, 1 patient | 120 mg 2 times / day steady, oral Studied dose Dose: 120 mg, 2 times / day Route: oral Route: steady Dose: 120 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Headache | grade 1-2, 1 patient | 120 mg 2 times / day steady, oral Studied dose Dose: 120 mg, 2 times / day Route: oral Route: steady Dose: 120 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Proteinuria | grade 1-2, 1 patient | 120 mg 2 times / day steady, oral Studied dose Dose: 120 mg, 2 times / day Route: oral Route: steady Dose: 120 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Pruritus | grade 1-2, 1 patient | 120 mg 2 times / day steady, oral Studied dose Dose: 120 mg, 2 times / day Route: oral Route: steady Dose: 120 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Anorexia | grade 1-2, 2 patients | 120 mg 2 times / day steady, oral Studied dose Dose: 120 mg, 2 times / day Route: oral Route: steady Dose: 120 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Fatigue | grade 1-2, 2 patients | 120 mg 2 times / day steady, oral Studied dose Dose: 120 mg, 2 times / day Route: oral Route: steady Dose: 120 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Nausea | grade 1-2, 2 patients | 120 mg 2 times / day steady, oral Studied dose Dose: 120 mg, 2 times / day Route: oral Route: steady Dose: 120 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Fatigue | grade 3-4, 1 patient | 120 mg 2 times / day steady, oral Studied dose Dose: 120 mg, 2 times / day Route: oral Route: steady Dose: 120 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Nausea | grade 3-4, 1 patient | 120 mg 2 times / day steady, oral Studied dose Dose: 120 mg, 2 times / day Route: oral Route: steady Dose: 120 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Rash | grade 3-4, 1 patient | 120 mg 2 times / day steady, oral Studied dose Dose: 120 mg, 2 times / day Route: oral Route: steady Dose: 120 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Proteinuria | grade 2, 1 patient DLT |
120 mg 2 times / day steady, oral Studied dose Dose: 120 mg, 2 times / day Route: oral Route: steady Dose: 120 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Rash | grade 3, 1 patient DLT |
120 mg 2 times / day steady, oral Studied dose Dose: 120 mg, 2 times / day Route: oral Route: steady Dose: 120 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Fatigue | grade 3, 3 patients DLT |
120 mg 2 times / day steady, oral Studied dose Dose: 120 mg, 2 times / day Route: oral Route: steady Dose: 120 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Nausea | grade 3, 3 patients DLT |
120 mg 2 times / day steady, oral Studied dose Dose: 120 mg, 2 times / day Route: oral Route: steady Dose: 120 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Headache | grade 1-2, 1 patient | 35 mg 2 times / day steady, oral Studied dose Dose: 35 mg, 2 times / day Route: oral Route: steady Dose: 35 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Pyrexia | grade 1-2, 1 patient | 35 mg 2 times / day steady, oral Studied dose Dose: 35 mg, 2 times / day Route: oral Route: steady Dose: 35 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Vomiting | grade 1-2, 2 patients | 35 mg 2 times / day steady, oral Studied dose Dose: 35 mg, 2 times / day Route: oral Route: steady Dose: 35 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Diarrhea | grade 1-2, 3 patients | 35 mg 2 times / day steady, oral Studied dose Dose: 35 mg, 2 times / day Route: oral Route: steady Dose: 35 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Fatigue | grade 1-2, 3 patients | 35 mg 2 times / day steady, oral Studied dose Dose: 35 mg, 2 times / day Route: oral Route: steady Dose: 35 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Nausea | grade 1-2, 4 patients | 35 mg 2 times / day steady, oral Studied dose Dose: 35 mg, 2 times / day Route: oral Route: steady Dose: 35 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Anorexia | grade 3, 1 patient DLT |
35 mg 2 times / day steady, oral Studied dose Dose: 35 mg, 2 times / day Route: oral Route: steady Dose: 35 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Dehydration | grade 3, 1 patient DLT |
35 mg 2 times / day steady, oral Studied dose Dose: 35 mg, 2 times / day Route: oral Route: steady Dose: 35 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Anorexia | grade 3-4, 1 patient | 35 mg 2 times / day steady, oral Studied dose Dose: 35 mg, 2 times / day Route: oral Route: steady Dose: 35 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Diarrhea | grade 3-4, 1 patient | 35 mg 2 times / day steady, oral Studied dose Dose: 35 mg, 2 times / day Route: oral Route: steady Dose: 35 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Anemia | grade 1-2, 1 patient | 90 mg 2 times / day steady, oral Studied dose Dose: 90 mg, 2 times / day Route: oral Route: steady Dose: 90 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Dyspnea | grade 1-2, 1 patient | 90 mg 2 times / day steady, oral Studied dose Dose: 90 mg, 2 times / day Route: oral Route: steady Dose: 90 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Pruritus | grade 1-2, 1 patient | 90 mg 2 times / day steady, oral Studied dose Dose: 90 mg, 2 times / day Route: oral Route: steady Dose: 90 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Fatigue | grade 1-2, 2 patients | 90 mg 2 times / day steady, oral Studied dose Dose: 90 mg, 2 times / day Route: oral Route: steady Dose: 90 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Rash | grade 1-2, 2 patients | 90 mg 2 times / day steady, oral Studied dose Dose: 90 mg, 2 times / day Route: oral Route: steady Dose: 90 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Diarrhea | grade 1-2, 3 patients | 90 mg 2 times / day steady, oral Studied dose Dose: 90 mg, 2 times / day Route: oral Route: steady Dose: 90 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Lethargy | grade 1-2, 3 patients | 90 mg 2 times / day steady, oral Studied dose Dose: 90 mg, 2 times / day Route: oral Route: steady Dose: 90 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Vomiting | grade 1-2, 3 patients | 90 mg 2 times / day steady, oral Studied dose Dose: 90 mg, 2 times / day Route: oral Route: steady Dose: 90 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Anorexia | grade 1-2, 4 patients | 90 mg 2 times / day steady, oral Studied dose Dose: 90 mg, 2 times / day Route: oral Route: steady Dose: 90 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Nausea | grade 1-2, 4 patients | 90 mg 2 times / day steady, oral Studied dose Dose: 90 mg, 2 times / day Route: oral Route: steady Dose: 90 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Proteinuria | grade 3-4, 1 patient | 90 mg 2 times / day steady, oral Studied dose Dose: 90 mg, 2 times / day Route: oral Route: steady Dose: 90 mg, 2 times / day Sources: |
unhealthy, 32-81 years Health Status: unhealthy Age Group: 32-81 years Sex: M+F Sources: |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Other Inhibitor | Other Substrate | Other Inducer |
---|---|---|
Drug as perpetrator
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021986s000_Sprycel__ClinPharmR.pdf Page: 6.0 |
yes | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021986s000_Sprycel__ClinPharmR.pdf Page: 6, 8 |
yes | yes (co-administration study) Comment: rifampin decreased AUC by 80%; ketoconazole increased dasatinib Cmax by 4-fold and AUC by 5-fold Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021986s000_Sprycel__ClinPharmR.pdf Page: 6, 8 |
Tox targets
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Page: 34.0 |
PubMed
Title | Date | PubMed |
---|---|---|
[Novel inhibitors of Bcr-Abl]. | 2006 |
|
[Tyrosine kinase inhibitors in the therapy of chronic myeloid leukaemia]. | 2006 |
|
Cancer and kinases: reports from the front line. | 2006 |
|
[State of the art in the treatment of chronic leukemias]. | 2006 Apr |
|
Glivec and beyond. | 2006 Aug |
|
KIT mutations in mastocytosis and their potential as therapeutic targets. | 2006 Aug |
|
Tyrosine kinase inhibitors: the next generation. | 2006 Aug |
|
Leukemogenesis induced by wild-type and STI571-resistant BCR/ABL is potently suppressed by C/EBPalpha. | 2006 Aug 15 |
|
Targeting ABL and SRC kinases in chronic myeloid leukemia: experience with dasatinib. | 2006 Dec |
|
Molecular pathogenesis and therapy of polycythemia induced in mice by JAK2 V617F. | 2006 Dec 20 |
|
Gateways to clinical trials. | 2006 Jul-Aug |
|
Gateways to clinical trials. | 2006 Jun |
|
Dasatinib-related alveolar pneumonia responsive to corticosteroids. | 2006 Jun |
|
Impact of genetic diagnostics on drug development strategy. | 2006 Jun |
|
The structure of Dasatinib (BMS-354825) bound to activated ABL kinase domain elucidates its inhibitory activity against imatinib-resistant ABL mutants. | 2006 Jun 1 |
|
Dasatinib (BMS-354825) selectively induces apoptosis in lung cancer cells dependent on epidermal growth factor receptor signaling for survival. | 2006 Jun 1 |
|
Complete regression of cutaneous lesions of refractory Ph+ ALL after 4 weeks of treatment with BMS-354825. | 2006 Jun 1 |
|
Panniculitis during dasatinib therapy for imatinib-resistant chronic myelogenous leukemia. | 2006 Jun 15 |
|
Circumventing resistance to kinase-inhibitor therapy. | 2006 Jun 15 |
|
Dasatinib in imatinib-resistant Philadelphia chromosome-positive leukemias. | 2006 Jun 15 |
|
AMN107 (nilotinib): a novel and selective inhibitor of BCR-ABL. | 2006 Jun 19 |
|
Clinical development of SRC tyrosine kinase inhibitors in lung cancer. | 2006 May |
|
The second generation of BCR-ABL tyrosine kinase inhibitors. | 2006 May |
|
Kinase inhibitors in chronic myelogenous leukemia. | 2006 May |
|
Novel tyrosine kinase inhibitors in chronic myelogenous leukemia. | 2006 Nov |
|
2-aminothiazole as a novel kinase inhibitor template. Structure-activity relationship studies toward the discovery of N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1- piperazinyl)]-2-methyl-4-pyrimidinyl]amino)]-1,3-thiazole-5-carboxamide (dasatinib, BMS-354825) as a potent pan-Src kinase inhibitor. | 2006 Nov 16 |
|
Gateways to clinical trials. | 2006 Oct |
|
Novel approaches in the treatment of systemic mastocytosis. | 2006 Oct 1 |
|
Comparison of imatinib mesylate, dasatinib (BMS-354825), and nilotinib (AMN107) in an N-ethyl-N-nitrosourea (ENU)-based mutagenesis screen: high efficacy of drug combinations. | 2006 Oct 1 |
|
ReSETting PP2A tumour suppressor activity in blast crisis and imatinib-resistant chronic myelogenous leukaemia. | 2006 Oct 9 |
|
Dasatinib. | 2006 Sep |
|
Pharmacy benefit spending on oral chemotherapy drugs. | 2006 Sep |
|
Sequential emergence of ABL-kinase mutations with loss of unmutated BCR-ABL allele during targeted therapies of CML. | 2006 Sep 1 |
|
Dasatinib in chronic myelogenous leukemia. | 2006 Sep 7 |
|
Dasatinib in chronic myelogenous leukemia. | 2006 Sep 7 |
|
Outcome of patients with Philadelphia chromosome-positive chronic myelogenous leukemia post-imatinib mesylate failure. | 2007 Apr 15 |
|
Dasatinib induces complete hematologic and cytogenetic responses in patients with imatinib-resistant or -intolerant chronic myeloid leukemia in blast crisis. | 2007 Apr 15 |
|
[Innovation of clinical trials for anti-cancer drugs in Japan--proposals from academia with special reference to the development of novel Bcr-Abl/Lyn tyrosine kinase inhibitor INNO-406 (NS-187) for imatinib-resistant chronic myelogenous leukemia]. | 2007 Feb |
|
Dasatinib. | 2007 Jan |
|
[Molecular targeting therapy for chronic myeloid leukemia]. | 2007 Jan |
|
New targeted therapies for chronic myelogenous leukemia: opportunities to overcome imatinib resistance. | 2007 Jan |
|
Chronic Myeloid Leukaemia in The 21st Century. | 2007 Jan |
|
MK-0457, a novel kinase inhibitor, is active in patients with chronic myeloid leukemia or acute lymphocytic leukemia with the T315I BCR-ABL mutation. | 2007 Jan 15 |
|
Dasatinib (BMS-354825) is active in Philadelphia chromosome-positive chronic myelogenous leukemia after imatinib and nilotinib (AMN107) therapy failure. | 2007 Jan 15 |
|
L576P KIT mutation in anal melanomas correlates with KIT protein expression and is sensitive to specific kinase inhibition. | 2007 Jul 15 |
|
Identification and functional signature of genes regulated by structurally different ABL kinase inhibitors. | 2007 Jun 14 |
|
Emerging therapeutic options for Philadelphia-positive acute lymphocytic leukemia. | 2007 Mar |
|
In silico profiling of tyrosine kinases binding specificity and drug resistance using Monte Carlo simulations with the ensembles of protein kinase crystal structures. | 2007 Mar |
|
Dasatinib inhibits migration and invasion in diverse human sarcoma cell lines and induces apoptosis in bone sarcoma cells dependent on SRC kinase for survival. | 2007 Mar 15 |
|
Dasatinib may also inhibit c-Kit in triple negative breast cancer cell lines. | 2008 Jan |
Sample Use Guides
The recommended starting dosage of SPRYCEL (dasatinib) for chronic phase CML is 100 mg administered orally once daily. The recommended starting dosage of SPRYCEL for accelerated phase CML, myeloid or lymphoid blast phase CML, or Ph+ ALL is 140 mg administered orally once daily. SPRYCEL can be taken with or without a meal, either in the morning or in the evening.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/26548624
Curator's Comment: Dasatinib modulates myofibroblast differentiation through Src-SRF pathway. Thus, dasatinib could potentially be a therapeutic option in fibrotic diseases
Unknown
Substance Class |
Chemical
Created
by
admin
on
Edited
Mon Mar 31 18:05:15 GMT 2025
by
admin
on
Mon Mar 31 18:05:15 GMT 2025
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Record UNII |
RBZ1571X5H
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Record Status |
Validated (UNII)
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Record Version |
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Common Name | English | ||
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Common Name | English | ||
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Code | English | ||
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Systematic Name | English |
Classification Tree | Code System | Code | ||
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WHO-VATC |
QL01XE06
Created by
admin on Mon Mar 31 18:05:15 GMT 2025 , Edited by admin on Mon Mar 31 18:05:15 GMT 2025
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FDA ORPHAN DRUG |
809221
Created by
admin on Mon Mar 31 18:05:15 GMT 2025 , Edited by admin on Mon Mar 31 18:05:15 GMT 2025
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EMA ASSESSMENT REPORTS |
SPRYCEL (AUTHORIZED: PRECURSOR CELL LYMPHOBLASTIC LEUKEMIA-LYMPHOMA)
Created by
admin on Mon Mar 31 18:05:15 GMT 2025 , Edited by admin on Mon Mar 31 18:05:15 GMT 2025
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NCI_THESAURUS |
C155700
Created by
admin on Mon Mar 31 18:05:15 GMT 2025 , Edited by admin on Mon Mar 31 18:05:15 GMT 2025
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NDF-RT |
N0000175605
Created by
admin on Mon Mar 31 18:05:15 GMT 2025 , Edited by admin on Mon Mar 31 18:05:15 GMT 2025
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NCI_THESAURUS |
C129825
Created by
admin on Mon Mar 31 18:05:15 GMT 2025 , Edited by admin on Mon Mar 31 18:05:15 GMT 2025
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EU-Orphan Drug |
EU/3/05/338
Created by
admin on Mon Mar 31 18:05:15 GMT 2025 , Edited by admin on Mon Mar 31 18:05:15 GMT 2025
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WHO-ATC |
L01XE06
Created by
admin on Mon Mar 31 18:05:15 GMT 2025 , Edited by admin on Mon Mar 31 18:05:15 GMT 2025
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FDA ORPHAN DRUG |
214605
Created by
admin on Mon Mar 31 18:05:15 GMT 2025 , Edited by admin on Mon Mar 31 18:05:15 GMT 2025
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FDA ORPHAN DRUG |
775320
Created by
admin on Mon Mar 31 18:05:15 GMT 2025 , Edited by admin on Mon Mar 31 18:05:15 GMT 2025
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FDA ORPHAN DRUG |
212405
Created by
admin on Mon Mar 31 18:05:15 GMT 2025 , Edited by admin on Mon Mar 31 18:05:15 GMT 2025
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NCI_THESAURUS |
C1967
Created by
admin on Mon Mar 31 18:05:15 GMT 2025 , Edited by admin on Mon Mar 31 18:05:15 GMT 2025
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FDA ORPHAN DRUG |
750520
Created by
admin on Mon Mar 31 18:05:15 GMT 2025 , Edited by admin on Mon Mar 31 18:05:15 GMT 2025
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LIVERTOX |
NBK548780
Created by
admin on Mon Mar 31 18:05:15 GMT 2025 , Edited by admin on Mon Mar 31 18:05:15 GMT 2025
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EMA ASSESSMENT REPORTS |
SPRYCEL (AUTHORIZED: LEUKEMIA, MYELOGENOUS, CHRONIC, BCR-ABL POSITIVE)
Created by
admin on Mon Mar 31 18:05:15 GMT 2025 , Edited by admin on Mon Mar 31 18:05:15 GMT 2025
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FDA ORPHAN DRUG |
750420
Created by
admin on Mon Mar 31 18:05:15 GMT 2025 , Edited by admin on Mon Mar 31 18:05:15 GMT 2025
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Code System | Code | Type | Description | ||
---|---|---|---|---|---|
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RBZ1571X5H
Created by
admin on Mon Mar 31 18:05:15 GMT 2025 , Edited by admin on Mon Mar 31 18:05:15 GMT 2025
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PRIMARY | |||
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100000090154
Created by
admin on Mon Mar 31 18:05:15 GMT 2025 , Edited by admin on Mon Mar 31 18:05:15 GMT 2025
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PRIMARY | |||
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DB01254
Created by
admin on Mon Mar 31 18:05:15 GMT 2025 , Edited by admin on Mon Mar 31 18:05:15 GMT 2025
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PRIMARY | |||
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RBZ1571X5H
Created by
admin on Mon Mar 31 18:05:15 GMT 2025 , Edited by admin on Mon Mar 31 18:05:15 GMT 2025
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PRIMARY | |||
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DASATINIB
Created by
admin on Mon Mar 31 18:05:15 GMT 2025 , Edited by admin on Mon Mar 31 18:05:15 GMT 2025
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PRIMARY | |||
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SS-39
Created by
admin on Mon Mar 31 18:05:15 GMT 2025 , Edited by admin on Mon Mar 31 18:05:15 GMT 2025
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PRIMARY | |||
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863127-77-9
Created by
admin on Mon Mar 31 18:05:15 GMT 2025 , Edited by admin on Mon Mar 31 18:05:15 GMT 2025
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PRIMARY | |||
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49375
Created by
admin on Mon Mar 31 18:05:15 GMT 2025 , Edited by admin on Mon Mar 31 18:05:15 GMT 2025
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PRIMARY | |||
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70839
Created by
admin on Mon Mar 31 18:05:15 GMT 2025 , Edited by admin on Mon Mar 31 18:05:15 GMT 2025
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PRIMARY | |||
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CHEMBL1421
Created by
admin on Mon Mar 31 18:05:15 GMT 2025 , Edited by admin on Mon Mar 31 18:05:15 GMT 2025
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PRIMARY | |||
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785
Created by
admin on Mon Mar 31 18:05:15 GMT 2025 , Edited by admin on Mon Mar 31 18:05:15 GMT 2025
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PRIMARY | |||
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Dasatinib
Created by
admin on Mon Mar 31 18:05:15 GMT 2025 , Edited by admin on Mon Mar 31 18:05:15 GMT 2025
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PRIMARY | |||
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5678
Created by
admin on Mon Mar 31 18:05:15 GMT 2025 , Edited by admin on Mon Mar 31 18:05:15 GMT 2025
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PRIMARY | |||
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C488369
Created by
admin on Mon Mar 31 18:05:15 GMT 2025 , Edited by admin on Mon Mar 31 18:05:15 GMT 2025
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PRIMARY | |||
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11540687
Created by
admin on Mon Mar 31 18:05:15 GMT 2025 , Edited by admin on Mon Mar 31 18:05:15 GMT 2025
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PRIMARY | |||
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DTXSID50235486
Created by
admin on Mon Mar 31 18:05:15 GMT 2025 , Edited by admin on Mon Mar 31 18:05:15 GMT 2025
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PRIMARY | |||
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N0000182141
Created by
admin on Mon Mar 31 18:05:15 GMT 2025 , Edited by admin on Mon Mar 31 18:05:15 GMT 2025
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PRIMARY | Cytochrome P450 3A4 Inhibitors [MoA] | ||
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C38713
Created by
admin on Mon Mar 31 18:05:15 GMT 2025 , Edited by admin on Mon Mar 31 18:05:15 GMT 2025
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PRIMARY | |||
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759877
Created by
admin on Mon Mar 31 18:05:15 GMT 2025 , Edited by admin on Mon Mar 31 18:05:15 GMT 2025
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PRIMARY | |||
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475342
Created by
admin on Mon Mar 31 18:05:15 GMT 2025 , Edited by admin on Mon Mar 31 18:05:15 GMT 2025
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PRIMARY | RxNorm | ||
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SUB23159
Created by
admin on Mon Mar 31 18:05:15 GMT 2025 , Edited by admin on Mon Mar 31 18:05:15 GMT 2025
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PRIMARY |
Related Record | Type | Details | ||
---|---|---|---|---|
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SALT/SOLVATE -> PARENT |
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TARGET -> INHIBITOR | |||
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TARGET -> INHIBITOR | |||
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BINDER->LIGAND |
BINDING
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TARGET -> INHIBITOR | |||
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TARGET -> INHIBITOR | |||
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ANHYDROUS->SOLVATE | |||
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TARGET -> INHIBITOR | |||
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TARGET -> INHIBITOR | |||
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TARGET -> INHIBITOR | |||
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TRANSPORTER -> INHIBITOR | |||
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TARGET -> INHIBITOR | |||
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TRANSPORTER -> INHIBITOR | |||
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TARGET -> INHIBITOR | |||
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TARGET -> INHIBITOR | |||
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TRANSPORTER -> SUBSTRATE | |||
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TARGET -> INHIBITOR | |||
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SALT/SOLVATE -> PARENT |
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TARGET -> INHIBITOR | |||
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TARGET -> INHIBITOR | |||
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TRANSPORTER -> SUBSTRATE | |||
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TRANSPORTER -> SUBSTRATE | |||
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TRANSPORTER -> SUBSTRATE | |||
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PARENT -> SALT/SOLVATE |
Related Record | Type | Details | ||
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IMPURITY -> PARENT |
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Related Record | Type | Details | ||
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ACTIVE MOIETY |
Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
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Volume of Distribution | PHARMACOKINETIC |
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Biological Half-life | PHARMACOKINETIC |
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