Details
Stereochemistry | ACHIRAL |
Molecular Formula | C22H26ClN7O2S |
Molecular Weight | 488.006 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CC1=NC(NC2=NC=C(S2)C(=O)NC3=C(C)C=CC=C3Cl)=CC(=N1)N4CCN(CCO)CC4
InChI
InChIKey=ZBNZXTGUTAYRHI-UHFFFAOYSA-N
InChI=1S/C22H26ClN7O2S/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)
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 |
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 |
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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 |
---|---|---|
Two new agents effective in Gleevec-resistant CML. | 2004 Dec |
|
Chronic myelogenous leukemia. | 2005 Oct |
|
[Tyrosine kinase inhibitors in the therapy of chronic myeloid leukaemia]. | 2006 |
|
Cancer and kinases: reports from the front line. | 2006 |
|
Dasatinib: BMS 354825. | 2006 |
|
Glivec and beyond. | 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 |
|
Dasatinib induces a response in malignant thymoma. | 2006 Dec 1 |
|
In vitro and in vivo activity of SKI-606, a novel Src-Abl inhibitor, against imatinib-resistant Bcr-Abl+ neoplastic cells. | 2006 Dec 1 |
|
Novel treatment strategies for chronic myeloid leukemia. | 2006 Dec 1 |
|
Molecular pathogenesis and therapy of polycythemia induced in mice by JAK2 V617F. | 2006 Dec 20 |
|
Dasatinib (BMS-354825) inhibits KITD816V, an imatinib-resistant activating mutation that triggers neoplastic growth in most patients with systemic mastocytosis. | 2006 Jul 1 |
|
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 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 |
|
Emerging drugs in chronic myelogenous leukaemia. | 2006 Nov |
|
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 |
|
Presence or the emergence of a F317L BCR-ABL mutation may be associated with resistance to dasatinib in Philadelphia chromosome-positive leukemia. | 2006 Nov 20 |
|
BCR and its mutants, the reciprocal t(9;22)-associated ABL/BCR fusion proteins, differentially regulate the cytoskeleton and cell motility. | 2006 Nov 7 |
|
The FDA approves new leukemia drug; expands use of current drug. | 2006 Nov-Dec |
|
Gateways to clinical trials. | 2006 Oct |
|
New tyrosine kinase inhibitors in the treatment of chronic myeloid leukemia. | 2006 Oct |
|
Cotreatment with vorinostat (suberoylanilide hydroxamic acid) enhances activity of dasatinib (BMS-354825) against imatinib mesylate-sensitive or imatinib mesylate-resistant chronic myelogenous leukemia cells. | 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 |
|
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 |
|
With targeted drugs, chronic myelogenous leukemia therapy may follow HIV's model. | 2007 Feb 7 |
|
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 |
|
BCR-ABL mutant kinetics in CML patients treated with dasatinib. | 2007 Jun |
|
Identification and functional signature of genes regulated by structurally different ABL kinase inhibitors. | 2007 Jun 14 |
|
Resistance to dasatinib in Philadelphia-positive leukemia patients and the presence or the selection of mutations at residues 315 and 317 in the BCR-ABL kinase domain. | 2007 Mar |
|
Second-line treatment with dasatinib in patients resistant to imatinib can select novel inhibitor-specific BCR-ABL mutants in Ph+ ALL. | 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 induces notable hematologic and cytogenetic responses in chronic-phase chronic myeloid leukemia after failure of imatinib therapy. | 2007 Mar 15 |
|
MEK1/2 inhibitors sensitize Bcr/Abl+ human leukemia cells to the dual Abl/Src inhibitor BMS-354/825. | 2007 May 1 |
|
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 18:28:12 GMT 2025
by
admin
on
Mon Mar 31 18:28:12 GMT 2025
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Record UNII |
X78UG0A0RN
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Record Status |
Validated (UNII)
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Record Version |
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-
Download
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Common Name | English | ||
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Preferred Name | English | ||
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Code | English | ||
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Systematic Name | English | ||
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Common Name | English | ||
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Common Name | English |
Classification Tree | Code System | Code | ||
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NCI_THESAURUS |
C155700
Created by
admin on Mon Mar 31 18:28:12 GMT 2025 , Edited by admin on Mon Mar 31 18:28:12 GMT 2025
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NCI_THESAURUS |
C1967
Created by
admin on Mon Mar 31 18:28:12 GMT 2025 , Edited by admin on Mon Mar 31 18:28:12 GMT 2025
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NDF-RT |
N0000175605
Created by
admin on Mon Mar 31 18:28:12 GMT 2025 , Edited by admin on Mon Mar 31 18:28:12 GMT 2025
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WHO-ATC |
L01XE06
Created by
admin on Mon Mar 31 18:28:12 GMT 2025 , Edited by admin on Mon Mar 31 18:28:12 GMT 2025
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NDF-RT |
N0000175076
Created by
admin on Mon Mar 31 18:28:12 GMT 2025 , Edited by admin on Mon Mar 31 18:28:12 GMT 2025
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Code System | Code | Type | Description | ||
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1546019
Created by
admin on Mon Mar 31 18:28:12 GMT 2025 , Edited by admin on Mon Mar 31 18:28:12 GMT 2025
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PRIMARY | RxNorm | ||
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N0000182141
Created by
admin on Mon Mar 31 18:28:12 GMT 2025 , Edited by admin on Mon Mar 31 18:28:12 GMT 2025
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PRIMARY | Cytochrome P450 3A4 Inhibitors [MoA] | ||
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m4101
Created by
admin on Mon Mar 31 18:28:12 GMT 2025 , Edited by admin on Mon Mar 31 18:28:12 GMT 2025
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PRIMARY | Merck Index | ||
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C74556
Created by
admin on Mon Mar 31 18:28:12 GMT 2025 , Edited by admin on Mon Mar 31 18:28:12 GMT 2025
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PRIMARY | |||
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DTXSID4040979
Created by
admin on Mon Mar 31 18:28:12 GMT 2025 , Edited by admin on Mon Mar 31 18:28:12 GMT 2025
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SUB23322
Created by
admin on Mon Mar 31 18:28:12 GMT 2025 , Edited by admin on Mon Mar 31 18:28:12 GMT 2025
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49375
Created by
admin on Mon Mar 31 18:28:12 GMT 2025 , Edited by admin on Mon Mar 31 18:28:12 GMT 2025
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3062316
Created by
admin on Mon Mar 31 18:28:12 GMT 2025 , Edited by admin on Mon Mar 31 18:28:12 GMT 2025
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8712
Created by
admin on Mon Mar 31 18:28:12 GMT 2025 , Edited by admin on Mon Mar 31 18:28:12 GMT 2025
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DB01254
Created by
admin on Mon Mar 31 18:28:12 GMT 2025 , Edited by admin on Mon Mar 31 18:28:12 GMT 2025
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302962-49-8
Created by
admin on Mon Mar 31 18:28:12 GMT 2025 , Edited by admin on Mon Mar 31 18:28:12 GMT 2025
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PRIMARY | |||
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X78UG0A0RN
Created by
admin on Mon Mar 31 18:28:12 GMT 2025 , Edited by admin on Mon Mar 31 18:28:12 GMT 2025
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X78UG0A0RN
Created by
admin on Mon Mar 31 18:28:12 GMT 2025 , Edited by admin on Mon Mar 31 18:28:12 GMT 2025
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100000088015
Created by
admin on Mon Mar 31 18:28:12 GMT 2025 , Edited by admin on Mon Mar 31 18:28:12 GMT 2025
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PRIMARY |
Related Record | Type | Details | ||
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TARGET -> INHIBITOR |
IC50
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SOLVATE->ANHYDROUS |
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EXCRETED UNCHANGED |
URINE
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TARGET -> INHIBITOR |
IC50
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SOLVATE->ANHYDROUS | |||
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METABOLIC ENZYME -> SUBSTRATE | |||
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TARGET -> INHIBITOR |
IC50
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EXCRETED UNCHANGED |
FECAL
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BINDER->LIGAND |
with no concentration dependence over the range of 100–500 ng/mL
BINDING
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SOLVATE->ANHYDROUS |
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SALT/SOLVATE -> PARENT |
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RESISTANT TARGET->INHIBITOR | |||
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TARGET -> INHIBITOR |
IC50
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TARGET -> INHIBITOR |
IC50
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TARGET -> INHIBITOR |
IC50
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SALT/SOLVATE -> PARENT |
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METABOLIC ENZYME -> SUBSTRATE |
MAJOR
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TARGET -> INHIBITOR |
IC50
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METABOLIC ENZYME -> INHIBITOR |
In human liver microsomes, dasatinib was a weak time-dependent inhibitor of CYP3A4.
TIME-DEPENDENT INHIBITION
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TARGET -> INHIBITOR |
IC50
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Related Record | Type | Details | ||
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METABOLITE -> PARENT | |||
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METABOLITE ACTIVE -> PARENT |
Metabolite M4
was approximately equipotent to dasatinib
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METABOLITE ACTIVE -> PARENT |
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METABOLITE LESS ACTIVE -> PARENT |
M5 and M6 were 10-fold less active than dasatinib
MAJOR
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METABOLITE LESS ACTIVE -> PARENT | |||
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METABOLITE -> PARENT |
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Related Record | Type | Details | ||
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ACTIVE MOIETY |
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Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
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Tmax | PHARMACOKINETIC |
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ORAL ADMINISTRATION |
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Volume of Distribution | PHARMACOKINETIC |
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Biological Half-life | PHARMACOKINETIC |
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