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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
Structure of Dasatinib Laurylsulfate

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)

HIDE SMILES / InChI

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

Description
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.

Originator

Curator's Comment: # Bristol-Myers Squibb

Approval Year

TargetsConditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
SPRYCEL

Approved Use

SPRYCEL® (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 Date

2006
Primary
SPRYCEL

Approved Use

SPRYCEL® (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 Date

2006
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
139.65 ng/mL
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

AUC

ValueDoseCo-administeredAnalytePopulation
499.45 ng × h/mL
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

T1/2

ValueDoseCo-administeredAnalytePopulation
5 h
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

Funbound

ValueDoseCo-administeredAnalytePopulation
6%
DASATINIB plasma
Homo sapiens
population: UNKNOWN
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse 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)
Hyponatremia (grade 3, 1 patient)
Other AEs:
Fatigue (grade 1-2, 3 patients)
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)
Sources:
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)
Lethargy (grade 3, 3 patients)
Bleeding time prolonged (grade 3, 1 patient)
Hypocalcemia (grade 3, 1 patient)
Other AEs:
Nausea (grade 1-2, 4 patients)
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)
Sources:
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)
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)
Sources:
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)
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)
Sources:
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)
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)
Sources:
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)
Fatigue (grade 1-2, 3 patients)
Diarrhea (grade 1-2, 1 patient)
Anorexia (grade 1-2, 2 patients)
Sources:
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)
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)
Sources:
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)
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)
Sources:
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)
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)
Sources:
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)
Fatigue (grade 3, 3 patients)
Rash (grade 3, 1 patient)
Proteinuria (grade 2, 1 patient)
Sources:
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)
Dehydration (grade 3, 1 patient)
Other AEs:
Nausea (grade 1-2, 4 patients)
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)
Sources:
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)
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)
Sources:
AEs

AEs

AESignificanceDosePopulation
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:
OverviewDrug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
no [IC50 >50 uM]
no [IC50 >50 uM]
no [IC50 >50 uM]
no [IC50 >50 uM]
no [IC50 >50 uM]
no
no
no
no
no
no
no
weak [Ki 1.9 uM]
yes [IC50 12 uM]
yes [IC50 35 uM]
yes [IC50 50 uM]
yes
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
yes
yes
yes (co-administration study)
Comment: rifampin decreased AUC by 80%; ketoconazole increased dasatinib Cmax by 4-fold and AUC by 5-fold
Page: 6, 8
Tox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
PubMed

PubMed

TitleDatePubMed
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
Patents

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
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 Wed Apr 02 05:37:13 GMT 2025
Edited
by admin
on Wed Apr 02 05:37:13 GMT 2025
Record UNII
FY77PS0C4O
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
Dasatinib Laurylsulfate
USAN  
Official Name English
Sulfuric acid, monododecyl ester, compd. with N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4-pyrimidinyl]amino]-5-thiazolecarboxamide (1:1)
Preferred Name English
DASATINIB LAURYLSULFATE [USAN]
Common Name English
C078D
Code English
N-(2-Chloro-6-methylphenyl)-2-({6-[4-(2-hydroxyethyl)piperazin-1-yl]-2-methylpyrimidin-4-yl}amino)thiazole-5-carboxamide dodecyl sulfate
Systematic Name English
DASATINIB MONOLAURYL SULFATE
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
CAS
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
FDA UNII
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
SMS_ID
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
USAN
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
NCI_THESAURUS
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
PUBCHEM
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