Details
Stereochemistry | ACHIRAL |
Molecular Formula | C22H26ClN7O2S.C12H26O4S |
Molecular Weight | 754.403 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CCCCCCCCCCCCOS(O)(=O)=O.CC1=NC(NC2=NC=C(S2)C(=O)NC3=C(C)C=CC=C3Cl)=CC(=N1)N4CCN(CCO)CC4
InChI
InChIKey=SWMPKFFMQAIAEW-UHFFFAOYSA-N
InChI=1S/C22H26ClN7O2S.C12H26O4S/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;1-2-3-4-5-6-7-8-9-10-11-12-16-17(13,14)15/h3-5,12-13,31H,6-11H2,1-2H3,(H,28,32)(H,24,25,26,27);2-12H2,1H3,(H,13,14,15)
Molecular Formula | C12H26O4S |
Molecular Weight | 266.397 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
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 |
|||
Target ID: CHEMBL1936 Sources: https://www.ncbi.nlm.nih.gov/pubmed/17701954 |
|||
Target ID: CHEMBL2068 Sources: https://www.ncbi.nlm.nih.gov/pubmed/17701954 |
|||
Target ID: CHEMBL1913 Sources: https://www.ncbi.nlm.nih.gov/pubmed/17701954 |
|||
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 |
---|---|---|
Cancer. Gleevec, chapter two: new leukemia drug aims to overcome resistance. | 2004 Jul 16 |
|
A single nucleotide polymorphism in the coding region of ABL and its effects on sensitivity to imatinib. | 2005 Nov |
|
[Novel inhibitors of Bcr-Abl]. | 2006 |
|
Cancer and kinases: reports from the front line. | 2006 |
|
Glivec and beyond. | 2006 Aug |
|
Tyrosine kinase inhibitors: the next generation. | 2006 Aug |
|
Molecular pathogenesis and therapy of polycythemia induced in mice by JAK2 V617F. | 2006 Dec 20 |
|
Gateways to clinical trials. | 2006 Jul-Aug |
|
Dasatinib in imatinib-resistant Philadelphia chromosome-positive leukemias. | 2006 Jun 15 |
|
Kinase inhibitors in chronic myelogenous leukemia. | 2006 May |
|
Potent inhibition of platelet-derived growth factor-induced responses in vascular smooth muscle cells by BMS-354825 (dasatinib). | 2006 May |
|
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 |
|
The FDA approves new leukemia drug; expands use of current drug. | 2006 Nov-Dec |
|
Novel approaches in the treatment of systemic mastocytosis. | 2006 Oct 1 |
|
Pharmacy benefit spending on oral chemotherapy drugs. | 2006 Sep |
|
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 |
|
Nonreceptor tyrosine kinases in prostate cancer. | 2007 Feb |
|
[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 |
|
Important therapeutic targets in chronic myelogenous leukemia. | 2007 Feb 15 |
|
L576P KIT mutation in anal melanomas correlates with KIT protein expression and is sensitive to specific kinase inhibition. | 2007 Jul 15 |
|
Dasatinib or high-dose imatinib for chronic-phase chronic myeloid leukemia after failure of first-line imatinib: a randomized phase 2 trial. | 2007 Jun 15 |
|
Emerging therapeutic options for Philadelphia-positive acute lymphocytic leukemia. | 2007 Mar |
|
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 |
|
Identification of candidate molecular markers predicting sensitivity in solid tumors to dasatinib: rationale for patient selection. | 2007 Mar 1 |
|
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, an orally active small molecule inhibitor of both the src and abl kinases, selectively inhibits growth of basal-type/"triple-negative" breast cancer cell lines growing in vitro. | 2007 Nov |
|
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
Wed Apr 02 05:37:13 GMT 2025
by
admin
on
Wed Apr 02 05:37:13 GMT 2025
|
Record UNII |
FY77PS0C4O
|
Record Status |
Validated (UNII)
|
Record Version |
|
-
Download
Name | Type | Language | ||
---|---|---|---|---|
|
Official Name | English | ||
|
Preferred Name | English | ||
|
Common Name | English | ||
|
Code | English | ||
|
Systematic Name | English | ||
|
Common Name | English |
Classification Tree | Code System | Code | ||
---|---|---|---|---|
|
FDA ORPHAN DRUG |
888722
Created by
admin on Wed Apr 02 05:37:13 GMT 2025 , Edited by admin on Wed Apr 02 05:37:13 GMT 2025
|
||
|
FDA ORPHAN DRUG |
869722
Created by
admin on Wed Apr 02 05:37:13 GMT 2025 , Edited by admin on Wed Apr 02 05:37:13 GMT 2025
|
Code System | Code | Type | Description | ||
---|---|---|---|---|---|
|
2398469-56-0
Created by
admin on Wed Apr 02 05:37:13 GMT 2025 , Edited by admin on Wed Apr 02 05:37:13 GMT 2025
|
PRIMARY | |||
|
FY77PS0C4O
Created by
admin on Wed Apr 02 05:37:13 GMT 2025 , Edited by admin on Wed Apr 02 05:37:13 GMT 2025
|
PRIMARY | |||
|
300000051136
Created by
admin on Wed Apr 02 05:37:13 GMT 2025 , Edited by admin on Wed Apr 02 05:37:13 GMT 2025
|
PRIMARY | |||
|
LM-189
Created by
admin on Wed Apr 02 05:37:13 GMT 2025 , Edited by admin on Wed Apr 02 05:37:13 GMT 2025
|
PRIMARY | |||
|
C203070
Created by
admin on Wed Apr 02 05:37:13 GMT 2025 , Edited by admin on Wed Apr 02 05:37:13 GMT 2025
|
PRIMARY | |||
|
146048051
Created by
admin on Wed Apr 02 05:37:13 GMT 2025 , Edited by admin on Wed Apr 02 05:37:13 GMT 2025
|
PRIMARY |
Related Record | Type | Details | ||
---|---|---|---|---|
|
PARENT -> SALT/SOLVATE |
|
Related Record | Type | Details | ||
---|---|---|---|---|
|
ACTIVE MOIETY |
|