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Details

Stereochemistry ACHIRAL
Molecular Formula C22H26ClN7O2S.H2O
Molecular Weight 506.0227
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of DASATINIB

SMILES

Cc1cccc(c1N=C(c2cnc(Nc3cc(nc(C)n3)N4CCN(CC4)CCO)s2)O)Cl.O

InChI

InChIKey=XHXFZZNHDVTMLI-UHFFFAOYSA-N
InChI=1S/C22H26ClN7O2S.H2O/c1-14-4-3-5-16(23)20(14)28-21(32)17-13-24-22(33-17)27-18-12-19(26-15(2)25-18)30-8-6-29(7-9-30)10-11-31;/h3-5,12-13,31H,6-11H2,1-2H3,(H,28,32)(H,24,25,26,27);1H2

HIDE SMILES / InChI

Molecular Formula C22H26ClN7O2S
Molecular Weight 488.0074
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Molecular Formula H2O
Molecular Weight 18.0153
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

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

1.15145284E12
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

1.15145284E12
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
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
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
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: Page: Table 3
unhealthy, 32-81 years
n = 6
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 6
Sources: Page: Table 3
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: Page: Table 3
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: Page: Table 3
unhealthy, 32-81 years
n = 4
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 4
Sources: Page: Table 3
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: Page: Table 3
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: Page: Table 3
unhealthy, 32-81 years
n = 9
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 9
Sources: Page: Table 3
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: Page: Table 3
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: Page: Table 4
unhealthy, 32-81 years
n = 5
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 5
Sources: Page: Table 4
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: Page: Table 4
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: Page: Table 3
unhealthy, 32-81 years
n = 3
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 3
Sources: Page: Table 3
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: Page: Table 3
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: Page: Table 3
unhealthy, 32-81 years
n = 4
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 4
Sources: Page: Table 3
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: Page: Table 3
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: Page: Table 4
unhealthy, 32-81 years
n = 13
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 13
Sources: Page: Table 4
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: Page: Table 4
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: Page: Table 4
unhealthy, 32-81 years
n = 17
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 17
Sources: Page: Table 4
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: Page: Table 4
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: Page: Table 4
unhealthy, 32-81 years
n = 4
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 4
Sources: Page: Table 4
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: Page: Table 4
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: Page: Table 4
unhealthy, 32-81 years
n = 5
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 5
Sources: Page: Table 4
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: Page: Table 4
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: Page: Table 3
unhealthy, 32-81 years
n = 7
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 7
Sources: Page: Table 3
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: Page: Table 3
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: Page: Table 4
unhealthy, 32-81 years
n = 7
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 7
Sources: Page: Table 4
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: Page: Table 4
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: Page: Table 3
unhealthy, 32-81 years
n = 6
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 6
Sources: Page: Table 3
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: Page: Table 3
unhealthy, 32-81 years
n = 6
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 6
Sources: Page: Table 3
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: Page: Table 3
unhealthy, 32-81 years
n = 6
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 6
Sources: Page: Table 3
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: Page: Table 3
unhealthy, 32-81 years
n = 6
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 6
Sources: Page: Table 3
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: Page: Table 3
unhealthy, 32-81 years
n = 6
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 6
Sources: Page: Table 3
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: Page: Table 3
unhealthy, 32-81 years
n = 6
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 6
Sources: Page: Table 3
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: Page: Table 3
unhealthy, 32-81 years
n = 6
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 6
Sources: Page: Table 3
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: Page: Table 3
unhealthy, 32-81 years
n = 6
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 6
Sources: Page: Table 3
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: Page: Table 3
unhealthy, 32-81 years
n = 4
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 4
Sources: Page: Table 3
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: Page: Table 3
unhealthy, 32-81 years
n = 4
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 4
Sources: Page: Table 3
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: Page: Table 3
unhealthy, 32-81 years
n = 4
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 4
Sources: Page: Table 3
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: Page: Table 3
unhealthy, 32-81 years
n = 4
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 4
Sources: Page: Table 3
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: Page: Table 3
unhealthy, 32-81 years
n = 4
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 4
Sources: Page: Table 3
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: Page: Table 3
unhealthy, 32-81 years
n = 4
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 4
Sources: Page: Table 3
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: Page: Table 3
unhealthy, 32-81 years
n = 4
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 4
Sources: Page: Table 3
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: Page: Table 3
unhealthy, 32-81 years
n = 4
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 4
Sources: Page: Table 3
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: Page: Table 3
unhealthy, 32-81 years
n = 4
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 4
Sources: Page: Table 3
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: Page: Table 3
unhealthy, 32-81 years
n = 4
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 4
Sources: Page: Table 3
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: Page: Table 3
unhealthy, 32-81 years
n = 4
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 4
Sources: Page: Table 3
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: Page: Table 3
unhealthy, 32-81 years
n = 4
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 4
Sources: Page: Table 3
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: Page: Table 3
unhealthy, 32-81 years
n = 4
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 4
Sources: Page: Table 3
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: Page: Table 3
unhealthy, 32-81 years
n = 4
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 4
Sources: Page: Table 3
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: Page: Table 3
unhealthy, 32-81 years
n = 4
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 4
Sources: Page: Table 3
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: Page: Table 3
unhealthy, 32-81 years
n = 4
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 4
Sources: Page: Table 3
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: Page: Table 3
unhealthy, 32-81 years
n = 4
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 4
Sources: Page: Table 3
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: Page: Table 3
unhealthy, 32-81 years
n = 9
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 9
Sources: Page: Table 3
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: Page: Table 3
unhealthy, 32-81 years
n = 9
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 9
Sources: Page: Table 3
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: Page: Table 3
unhealthy, 32-81 years
n = 9
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 9
Sources: Page: Table 3
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: Page: Table 3
unhealthy, 32-81 years
n = 9
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 9
Sources: Page: Table 3
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: Page: Table 3
unhealthy, 32-81 years
n = 9
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 9
Sources: Page: Table 3
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: Page: Table 3
unhealthy, 32-81 years
n = 9
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 9
Sources: Page: Table 3
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: Page: Table 3
unhealthy, 32-81 years
n = 9
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 9
Sources: Page: Table 3
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: Page: Table 3
unhealthy, 32-81 years
n = 9
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 9
Sources: Page: Table 3
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: Page: Table 3
unhealthy, 32-81 years
n = 9
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 9
Sources: Page: Table 3
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: Page: Table 3
unhealthy, 32-81 years
n = 9
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 9
Sources: Page: Table 3
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: Page: Table 3
unhealthy, 32-81 years
n = 9
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 9
Sources: Page: Table 3
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: Page: Table 3
unhealthy, 32-81 years
n = 9
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 9
Sources: Page: Table 3
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: Page: Table 3
unhealthy, 32-81 years
n = 9
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 9
Sources: Page: Table 3
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: Page: Table 4
unhealthy, 32-81 years
n = 5
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 5
Sources: Page: Table 4
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: Page: Table 4
unhealthy, 32-81 years
n = 5
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 5
Sources: Page: Table 4
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: Page: Table 4
unhealthy, 32-81 years
n = 5
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 5
Sources: Page: Table 4
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: Page: Table 4
unhealthy, 32-81 years
n = 5
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 5
Sources: Page: Table 4
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: Page: Table 4
unhealthy, 32-81 years
n = 5
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 5
Sources: Page: Table 4
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: Page: Table 4
unhealthy, 32-81 years
n = 5
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 5
Sources: Page: Table 4
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: Page: Table 4
unhealthy, 32-81 years
n = 5
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 5
Sources: Page: Table 4
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: Page: Table 3
unhealthy, 32-81 years
n = 3
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 3
Sources: Page: Table 3
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: Page: Table 3
unhealthy, 32-81 years
n = 3
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 3
Sources: Page: Table 3
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: Page: Table 3
unhealthy, 32-81 years
n = 3
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 3
Sources: Page: Table 3
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: Page: Table 3
unhealthy, 32-81 years
n = 3
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 3
Sources: Page: Table 3
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: Page: Table 3
unhealthy, 32-81 years
n = 3
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 3
Sources: Page: Table 3
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: Page: Table 3
unhealthy, 32-81 years
n = 3
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 3
Sources: Page: Table 3
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: Page: Table 3
unhealthy, 32-81 years
n = 3
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 3
Sources: Page: Table 3
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: Page: Table 3
unhealthy, 32-81 years
n = 4
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 4
Sources: Page: Table 3
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: Page: Table 3
unhealthy, 32-81 years
n = 4
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 4
Sources: Page: Table 3
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: Page: Table 3
unhealthy, 32-81 years
n = 4
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 4
Sources: Page: Table 3
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: Page: Table 3
unhealthy, 32-81 years
n = 4
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 4
Sources: Page: Table 3
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: Page: Table 4
unhealthy, 32-81 years
n = 13
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 13
Sources: Page: Table 4
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: Page: Table 4
unhealthy, 32-81 years
n = 13
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 13
Sources: Page: Table 4
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: Page: Table 4
unhealthy, 32-81 years
n = 13
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 13
Sources: Page: Table 4
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: Page: Table 4
unhealthy, 32-81 years
n = 13
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 13
Sources: Page: Table 4
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: Page: Table 4
unhealthy, 32-81 years
n = 13
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 13
Sources: Page: Table 4
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: Page: Table 4
unhealthy, 32-81 years
n = 13
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 13
Sources: Page: Table 4
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: Page: Table 4
unhealthy, 32-81 years
n = 13
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 13
Sources: Page: Table 4
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: Page: Table 4
unhealthy, 32-81 years
n = 13
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 13
Sources: Page: Table 4
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: Page: Table 4
unhealthy, 32-81 years
n = 17
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 17
Sources: Page: Table 4
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: Page: Table 4
unhealthy, 32-81 years
n = 17
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 17
Sources: Page: Table 4
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: Page: Table 4
unhealthy, 32-81 years
n = 17
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 17
Sources: Page: Table 4
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: Page: Table 4
unhealthy, 32-81 years
n = 17
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 17
Sources: Page: Table 4
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: Page: Table 4
unhealthy, 32-81 years
n = 17
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 17
Sources: Page: Table 4
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: Page: Table 4
unhealthy, 32-81 years
n = 17
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 17
Sources: Page: Table 4
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: Page: Table 4
unhealthy, 32-81 years
n = 17
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 17
Sources: Page: Table 4
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: Page: Table 4
unhealthy, 32-81 years
n = 17
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 17
Sources: Page: Table 4
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: Page: Table 4
unhealthy, 32-81 years
n = 17
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 17
Sources: Page: Table 4
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: Page: Table 4
unhealthy, 32-81 years
n = 17
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 17
Sources: Page: Table 4
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: Page: Table 4
unhealthy, 32-81 years
n = 17
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 17
Sources: Page: Table 4
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: Page: Table 4
unhealthy, 32-81 years
n = 17
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 17
Sources: Page: Table 4
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: Page: Table 4
unhealthy, 32-81 years
n = 17
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 17
Sources: Page: Table 4
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: Page: Table 4
unhealthy, 32-81 years
n = 17
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 17
Sources: Page: Table 4
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: Page: Table 4
unhealthy, 32-81 years
n = 17
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 17
Sources: Page: Table 4
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: Page: Table 4
unhealthy, 32-81 years
n = 4
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 4
Sources: Page: Table 4
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: Page: Table 4
unhealthy, 32-81 years
n = 4
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 4
Sources: Page: Table 4
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: Page: Table 4
unhealthy, 32-81 years
n = 4
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 4
Sources: Page: Table 4
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: Page: Table 4
unhealthy, 32-81 years
n = 4
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 4
Sources: Page: Table 4
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: Page: Table 4
unhealthy, 32-81 years
n = 5
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 5
Sources: Page: Table 4
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: Page: Table 4
unhealthy, 32-81 years
n = 5
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 5
Sources: Page: Table 4
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: Page: Table 4
unhealthy, 32-81 years
n = 5
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 5
Sources: Page: Table 4
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: Page: Table 4
unhealthy, 32-81 years
n = 5
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 5
Sources: Page: Table 4
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: Page: Table 4
unhealthy, 32-81 years
n = 5
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 5
Sources: Page: Table 4
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: Page: Table 4
unhealthy, 32-81 years
n = 5
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 5
Sources: Page: Table 4
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: Page: Table 4
unhealthy, 32-81 years
n = 5
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 5
Sources: Page: Table 4
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: Page: Table 4
unhealthy, 32-81 years
n = 5
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 5
Sources: Page: Table 4
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: Page: Table 4
unhealthy, 32-81 years
n = 5
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 5
Sources: Page: Table 4
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: Page: Table 4
unhealthy, 32-81 years
n = 5
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 5
Sources: Page: Table 4
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: Page: Table 4
unhealthy, 32-81 years
n = 5
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 5
Sources: Page: Table 4
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: Page: Table 3
unhealthy, 32-81 years
n = 7
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 7
Sources: Page: Table 3
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: Page: Table 3
unhealthy, 32-81 years
n = 7
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 7
Sources: Page: Table 3
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: Page: Table 3
unhealthy, 32-81 years
n = 7
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 7
Sources: Page: Table 3
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: Page: Table 3
unhealthy, 32-81 years
n = 7
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 7
Sources: Page: Table 3
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: Page: Table 3
unhealthy, 32-81 years
n = 7
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 7
Sources: Page: Table 3
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: Page: Table 3
unhealthy, 32-81 years
n = 7
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 7
Sources: Page: Table 3
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: Page: Table 3
unhealthy, 32-81 years
n = 7
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 7
Sources: Page: Table 3
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: Page: Table 3
unhealthy, 32-81 years
n = 7
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 7
Sources: Page: Table 3
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: Page: Table 3
unhealthy, 32-81 years
n = 7
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 7
Sources: Page: Table 3
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: Page: Table 3
unhealthy, 32-81 years
n = 7
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 7
Sources: Page: Table 3
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: Page: Table 4
unhealthy, 32-81 years
n = 7
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 7
Sources: Page: Table 4
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: Page: Table 4
unhealthy, 32-81 years
n = 7
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 7
Sources: Page: Table 4
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: Page: Table 4
unhealthy, 32-81 years
n = 7
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 7
Sources: Page: Table 4
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: Page: Table 4
unhealthy, 32-81 years
n = 7
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 7
Sources: Page: Table 4
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: Page: Table 4
unhealthy, 32-81 years
n = 7
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 7
Sources: Page: Table 4
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: Page: Table 4
unhealthy, 32-81 years
n = 7
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 7
Sources: Page: Table 4
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: Page: Table 4
unhealthy, 32-81 years
n = 7
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 7
Sources: Page: Table 4
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: Page: Table 4
unhealthy, 32-81 years
n = 7
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 7
Sources: Page: Table 4
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: Page: Table 4
unhealthy, 32-81 years
n = 7
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 7
Sources: Page: Table 4
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: Page: Table 4
unhealthy, 32-81 years
n = 7
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 7
Sources: Page: Table 4
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: Page: Table 4
unhealthy, 32-81 years
n = 7
Health Status: unhealthy
Condition: metastatic solid tumors
Age Group: 32-81 years
Sex: M+F
Population Size: 7
Sources: Page: Table 4
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
Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays.
2004 Dec 30
Overriding imatinib resistance with a novel ABL kinase inhibitor.
2004 Jul 16
New generation leukaemia drugs are on their way.
2004 Sep 1
In vitro activity of Bcr-Abl inhibitors AMN107 and BMS-354825 against clinically relevant imatinib-resistant Abl kinase domain mutants.
2005 Jun 1
[Tyrosine kinase inhibitors in the therapy of chronic myeloid leukaemia].
2006
Dasatinib: BMS 354825.
2006
Glivec and beyond.
2006 Aug
Identification of potential biomarkers for measuring inhibition of Src kinase activity in colon cancer cells following treatment with dasatinib.
2006 Dec
Dasatinib (BMS-354825), a dual SRC/ABL kinase inhibitor, inhibits the kinase activity of wild-type, juxtamembrane, and activation loop mutant KIT isoforms associated with human malignancies.
2006 Jan 1
Gateways to clinical trials.
2006 Jul-Aug
Gateways to clinical trials.
2006 Jun
Dasatinib in imatinib-resistant Philadelphia chromosome-positive leukemias.
2006 Jun 15
AMN107 (nilotinib): a novel and selective inhibitor of BCR-ABL.
2006 Jun 19
Inhibition of SRC expression and activity inhibits tumor progression and metastasis of human pancreatic adenocarcinoma cells in an orthotopic nude mouse model.
2006 Mar
Kinase inhibitors in chronic myelogenous leukemia.
2006 May
New assignments for multitasking signal transduction inhibitors.
2006 May
Emerging drugs in chronic myelogenous leukaemia.
2006 Nov
2-aminothiazole as a novel kinase inhibitor template. Structure-activity relationship studies toward the discovery of N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1- piperazinyl)]-2-methyl-4-pyrimidinyl]amino)]-1,3-thiazole-5-carboxamide (dasatinib, BMS-354825) as a potent pan-Src kinase inhibitor.
2006 Nov 16
New tyrosine kinase inhibitors in the treatment of chronic myeloid leukemia.
2006 Oct
Cotreatment with vorinostat (suberoylanilide hydroxamic acid) enhances activity of dasatinib (BMS-354825) against imatinib mesylate-sensitive or imatinib mesylate-resistant chronic myelogenous leukemia cells.
2006 Oct 1
Dasatinib.
2006 Sep
Pharmacy benefit spending on oral chemotherapy drugs.
2006 Sep
Dasatinib in chronic myelogenous leukemia.
2006 Sep 7
Dasatinib in chronic myelogenous leukemia.
2006 Sep 7
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
Important therapeutic targets in chronic myelogenous leukemia.
2007 Feb 15
New targeted therapies for chronic myelogenous leukemia: opportunities to overcome imatinib resistance.
2007 Jan
BCR-ABL mutant kinetics in CML patients treated with dasatinib.
2007 Jun
Identification and functional signature of genes regulated by structurally different ABL kinase inhibitors.
2007 Jun 14
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
MEK1/2 inhibitors sensitize Bcr/Abl+ human leukemia cells to the dual Abl/Src inhibitor BMS-354/825.
2007 May 1
Dasatinib induces significant hematologic and cytogenetic responses in patients with imatinib-resistant or -intolerant chronic myeloid leukemia in accelerated phase.
2007 May 15
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 Fri Jun 25 21:58:19 UTC 2021
Edited
by admin
on Fri Jun 25 21:58:19 UTC 2021
Record UNII
RBZ1571X5H
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
DASATINIB
EMA EPAR   ORANGE BOOK   USAN   VANDF  
USAN  
Official Name English
DASATINIB MONOHYDRATE
WHO-DD  
Common Name English
BMS-354825 HYDRATE
Code English
SPRYCEL
Brand Name English
N-(2-CHLORO-6-METHYLPHENYL)-2-((6-(4-(2-HYDROXYETHYL)PIPERAZIN-1-YL)-2-METHYLPYRIMIDIN-4-YL)AMINO)THIAZOLE-5-CARBOXAMIDE HYDRATE
Systematic Name English
DASATINIB HYDRATE
JAN  
Common Name English
DASATINIB MONOHYDRATE [WHO-DD]
Common Name English
DASATINIB [ORANGE BOOK]
Common Name English
DASATINIB [VANDF]
Common Name English
DASATINIB [EMA EPAR]
Common Name English
NSC-759877
Code English
DASATINIB [USAN]
Common Name English
DASATINIB HYDRATE [JAN]
Common Name English
BMS-354825-03
Code English
5-THIAZOLECARBOXAMIDE, N-(2-CHLORO-6-METHYLPHENYL)-2-((6-(4-(2-HYDROXYETHYL)-1-PIPERAZINYL)-2-METHYL-4-PYRIMIDINYL)AMINO)-, MONOHYDRATE
Systematic Name English
Classification Tree Code System Code
WHO-VATC QL01XE06
Created by admin on Fri Jun 25 21:58:19 UTC 2021 , Edited by admin on Fri Jun 25 21:58:19 UTC 2021
EMA ASSESSMENT REPORTS SPRYCEL (AUTHORIZED: PRECURSOR CELL LYMPHOBLASTIC LEUKEMIA-LYMPHOMA)
Created by admin on Fri Jun 25 21:58:19 UTC 2021 , Edited by admin on Fri Jun 25 21:58:19 UTC 2021
NCI_THESAURUS C155700
Created by admin on Fri Jun 25 21:58:19 UTC 2021 , Edited by admin on Fri Jun 25 21:58:19 UTC 2021
NDF-RT N0000175605
Created by admin on Fri Jun 25 21:58:19 UTC 2021 , Edited by admin on Fri Jun 25 21:58:19 UTC 2021
NCI_THESAURUS C129825
Created by admin on Fri Jun 25 21:58:19 UTC 2021 , Edited by admin on Fri Jun 25 21:58:19 UTC 2021
EU-Orphan Drug EU/3/05/338
Created by admin on Fri Jun 25 21:58:19 UTC 2021 , Edited by admin on Fri Jun 25 21:58:19 UTC 2021
WHO-ATC L01XE06
Created by admin on Fri Jun 25 21:58:19 UTC 2021 , Edited by admin on Fri Jun 25 21:58:19 UTC 2021
FDA ORPHAN DRUG 214605
Created by admin on Fri Jun 25 21:58:19 UTC 2021 , Edited by admin on Fri Jun 25 21:58:19 UTC 2021
FDA ORPHAN DRUG 212405
Created by admin on Fri Jun 25 21:58:19 UTC 2021 , Edited by admin on Fri Jun 25 21:58:19 UTC 2021
NCI_THESAURUS C1967
Created by admin on Fri Jun 25 21:58:19 UTC 2021 , Edited by admin on Fri Jun 25 21:58:19 UTC 2021
LIVERTOX 269
Created by admin on Fri Jun 25 21:58:19 UTC 2021 , Edited by admin on Fri Jun 25 21:58:19 UTC 2021
EMA ASSESSMENT REPORTS SPRYCEL (AUTHORIZED: LEUKEMIA, MYELOGENOUS, CHRONIC, BCR-ABL POSITIVE)
Created by admin on Fri Jun 25 21:58:19 UTC 2021 , Edited by admin on Fri Jun 25 21:58:19 UTC 2021
Code System Code Type Description
FDA UNII
RBZ1571X5H
Created by admin on Fri Jun 25 21:58:19 UTC 2021 , Edited by admin on Fri Jun 25 21:58:19 UTC 2021
PRIMARY
DRUG BANK
DB01254
Created by admin on Fri Jun 25 21:58:19 UTC 2021 , Edited by admin on Fri Jun 25 21:58:19 UTC 2021
PRIMARY
WIKIPEDIA
DASATINIB
Created by admin on Fri Jun 25 21:58:19 UTC 2021 , Edited by admin on Fri Jun 25 21:58:19 UTC 2021
PRIMARY
CAS
863127-77-9
Created by admin on Fri Jun 25 21:58:19 UTC 2021 , Edited by admin on Fri Jun 25 21:58:19 UTC 2021
PRIMARY
ChEMBL
CHEMBL1421
Created by admin on Fri Jun 25 21:58:19 UTC 2021 , Edited by admin on Fri Jun 25 21:58:19 UTC 2021
PRIMARY
DRUG CENTRAL
785
Created by admin on Fri Jun 25 21:58:19 UTC 2021 , Edited by admin on Fri Jun 25 21:58:19 UTC 2021
PRIMARY
LACTMED
Dasatinib
Created by admin on Fri Jun 25 21:58:19 UTC 2021 , Edited by admin on Fri Jun 25 21:58:19 UTC 2021
PRIMARY
IUPHAR
5678
Created by admin on Fri Jun 25 21:58:19 UTC 2021 , Edited by admin on Fri Jun 25 21:58:19 UTC 2021
PRIMARY
MESH
C488369
Created by admin on Fri Jun 25 21:58:19 UTC 2021 , Edited by admin on Fri Jun 25 21:58:19 UTC 2021
PRIMARY
PUBCHEM
11540687
Created by admin on Fri Jun 25 21:58:19 UTC 2021 , Edited by admin on Fri Jun 25 21:58:19 UTC 2021
PRIMARY
EPA CompTox
863127-77-9
Created by admin on Fri Jun 25 21:58:19 UTC 2021 , Edited by admin on Fri Jun 25 21:58:19 UTC 2021
PRIMARY
NDF-RT
N0000182141
Created by admin on Fri Jun 25 21:58:19 UTC 2021 , Edited by admin on Fri Jun 25 21:58:19 UTC 2021
PRIMARY Cytochrome P450 3A4 Inhibitors [MoA]
NCI_THESAURUS
C38713
Created by admin on Fri Jun 25 21:58:19 UTC 2021 , Edited by admin on Fri Jun 25 21:58:19 UTC 2021
PRIMARY
RXCUI
475342
Created by admin on Fri Jun 25 21:58:19 UTC 2021 , Edited by admin on Fri Jun 25 21:58:19 UTC 2021
PRIMARY RxNorm
EVMPD
SUB23159
Created by admin on Fri Jun 25 21:58:19 UTC 2021 , Edited by admin on Fri Jun 25 21:58:19 UTC 2021
PRIMARY
Related Record Type Details
TARGET -> INHIBITOR
TARGET -> INHIBITOR
TRANSPORTER -> INHIBITOR
BINDER->LIGAND
BINDING
TARGET -> INHIBITOR
TARGET -> INHIBITOR
Kd (pKd=9.1); Target: KIT
BINDING
TARGET -> INHIBITOR
TARGET -> INHIBITOR
TARGET -> INHIBITOR
TRANSPORTER -> SUBSTRATE
TARGET -> INHIBITOR
TRANSPORTER -> SUBSTRATE
TRANSPORTER -> SUBSTRATE
TARGET -> INHIBITOR
TARGET -> INHIBITOR
TRANSPORTER -> INHIBITOR
TRANSPORTER -> SUBSTRATE
TARGET -> INHIBITOR
TARGET -> INHIBITOR
INHIBITOR
TARGET -> INHIBITOR
PARENT -> SALT/SOLVATE
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Volume of Distribution PHARMACOKINETIC
Biological Half-life PHARMACOKINETIC