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Details

Stereochemistry ACHIRAL
Molecular Formula C22H26ClN7O2S
Molecular Weight 488.006
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of DASATINIB ANHYDROUS

SMILES

CC1=NC(NC2=NC=C(S2)C(=O)NC3=C(Cl)C=CC=C3C)=CC(=N1)N4CCN(CCO)CC4

InChI

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

HIDE SMILES / InChI

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
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
Cancer. Gleevec, chapter two: new leukemia drug aims to overcome resistance.
2004 Jul 16
Loss of response to imatinib: mechanisms and management.
2005
BMS-354825: a novel drug with potential for the treatment of imatinib-resistant chronic myeloid leukaemia.
2005 Jan
Chronic myelogenous leukemia.
2005 Oct
[Novel inhibitors of Bcr-Abl].
2006
Cancer and kinases: reports from the front line.
2006
[State of the art in the treatment of chronic leukemias].
2006 Apr
KIT mutations in mastocytosis and their potential as therapeutic targets.
2006 Aug
Tyrosine kinase inhibitors: the next generation.
2006 Aug
Targeting ABL and SRC kinases in chronic myeloid leukemia: experience with dasatinib.
2006 Dec
Identification of potential biomarkers for measuring inhibition of Src kinase activity in colon cancer cells following treatment with dasatinib.
2006 Dec
Novel treatment strategies for chronic myeloid leukemia.
2006 Dec 1
Structure of the kinase domain of an imatinib-resistant Abl mutant in complex with the Aurora kinase inhibitor VX-680.
2006 Jan 15
Looking beyond imatinib: next line of targeted drugs for CML shows promise.
2006 Jan 25
Dasatinib (BMS-354825) inhibits KITD816V, an imatinib-resistant activating mutation that triggers neoplastic growth in most patients with systemic mastocytosis.
2006 Jul 1
Gateways to clinical trials.
2006 Jun
Dasatinib-related alveolar pneumonia responsive to corticosteroids.
2006 Jun
Impact of genetic diagnostics on drug development strategy.
2006 Jun
The structure of Dasatinib (BMS-354825) bound to activated ABL kinase domain elucidates its inhibitory activity against imatinib-resistant ABL mutants.
2006 Jun 1
Complete regression of cutaneous lesions of refractory Ph+ ALL after 4 weeks of treatment with BMS-354825.
2006 Jun 1
Dasatinib (BMS-354825) targets an earlier progenitor population than imatinib in primary CML but does not eliminate the quiescent fraction.
2006 Jun 1
Panniculitis during dasatinib therapy for imatinib-resistant chronic myelogenous leukemia.
2006 Jun 15
Circumventing resistance to kinase-inhibitor therapy.
2006 Jun 15
The second generation of BCR-ABL tyrosine kinase inhibitors.
2006 May
Emerging drugs in chronic myelogenous leukaemia.
2006 Nov
Novel tyrosine kinase inhibitors in chronic myelogenous leukemia.
2006 Nov
2-aminothiazole as a novel kinase inhibitor template. Structure-activity relationship studies toward the discovery of N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1- piperazinyl)]-2-methyl-4-pyrimidinyl]amino)]-1,3-thiazole-5-carboxamide (dasatinib, BMS-354825) as a potent pan-Src kinase inhibitor.
2006 Nov 16
Gateways to clinical trials.
2006 Oct
Novel approaches in the treatment of systemic mastocytosis.
2006 Oct 1
Comparison of imatinib mesylate, dasatinib (BMS-354825), and nilotinib (AMN107) in an N-ethyl-N-nitrosourea (ENU)-based mutagenesis screen: high efficacy of drug combinations.
2006 Oct 1
ReSETting PP2A tumour suppressor activity in blast crisis and imatinib-resistant chronic myelogenous leukaemia.
2006 Oct 9
Dasatinib.
2006 Sep
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
[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
With targeted drugs, chronic myelogenous leukemia therapy may follow HIV's model.
2007 Feb 7
MK-0457, a novel kinase inhibitor, is active in patients with chronic myeloid leukemia or acute lymphocytic leukemia with the T315I BCR-ABL mutation.
2007 Jan 15
Dasatinib (BMS-354825) is active in Philadelphia chromosome-positive chronic myelogenous leukemia after imatinib and nilotinib (AMN107) therapy failure.
2007 Jan 15
L576P KIT mutation in anal melanomas correlates with KIT protein expression and is sensitive to specific kinase inhibition.
2007 Jul 15
Emerging therapeutic options for Philadelphia-positive acute lymphocytic leukemia.
2007 Mar
In silico profiling of tyrosine kinases binding specificity and drug resistance using Monte Carlo simulations with the ensembles of protein kinase crystal structures.
2007 Mar
Dasatinib inhibits migration and invasion in diverse human sarcoma cell lines and induces apoptosis in bone sarcoma cells dependent on SRC kinase for survival.
2007 Mar 15
Dasatinib induces notable hematologic and cytogenetic responses in chronic-phase chronic myeloid leukemia after failure of imatinib therapy.
2007 Mar 15
Dasatinib induces significant hematologic and cytogenetic responses in patients with imatinib-resistant or -intolerant chronic myeloid leukemia in accelerated phase.
2007 May 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
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 Dec 15 16:26:50 GMT 2023
Edited
by admin
on Fri Dec 15 16:26:50 GMT 2023
Record UNII
X78UG0A0RN
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
DASATINIB ANHYDROUS
Common Name English
BMS-354825
Code English
5-THIAZOLECARBOXAMIDE, N-(2-CHLORO-6-METHYLPHENYL)-2-((6-(4-(2-HYDROXYETHYL)-1-PIPERAZINYL)-2-METHYL-4-PYRIMIDINYL)AMINO)-
Systematic Name English
dasatinib [INN]
Common Name English
Dasatinib [WHO-DD]
Common Name English
DASATINIB [MI]
Common Name English
Classification Tree Code System Code
NCI_THESAURUS C155700
Created by admin on Fri Dec 15 16:26:51 GMT 2023 , Edited by admin on Fri Dec 15 16:26:51 GMT 2023
NCI_THESAURUS C1967
Created by admin on Fri Dec 15 16:26:51 GMT 2023 , Edited by admin on Fri Dec 15 16:26:51 GMT 2023
NDF-RT N0000175605
Created by admin on Fri Dec 15 16:26:51 GMT 2023 , Edited by admin on Fri Dec 15 16:26:51 GMT 2023
WHO-ATC L01XE06
Created by admin on Fri Dec 15 16:26:51 GMT 2023 , Edited by admin on Fri Dec 15 16:26:51 GMT 2023
NDF-RT N0000175076
Created by admin on Fri Dec 15 16:26:51 GMT 2023 , Edited by admin on Fri Dec 15 16:26:51 GMT 2023
Code System Code Type Description
RXCUI
1546019
Created by admin on Fri Dec 15 16:26:51 GMT 2023 , Edited by admin on Fri Dec 15 16:26:51 GMT 2023
PRIMARY RxNorm
NDF-RT
N0000182141
Created by admin on Fri Dec 15 16:26:51 GMT 2023 , Edited by admin on Fri Dec 15 16:26:51 GMT 2023
PRIMARY Cytochrome P450 3A4 Inhibitors [MoA]
MERCK INDEX
m4101
Created by admin on Fri Dec 15 16:26:51 GMT 2023 , Edited by admin on Fri Dec 15 16:26:51 GMT 2023
PRIMARY Merck Index
NCI_THESAURUS
C74556
Created by admin on Fri Dec 15 16:26:51 GMT 2023 , Edited by admin on Fri Dec 15 16:26:51 GMT 2023
PRIMARY
EPA CompTox
DTXSID4040979
Created by admin on Fri Dec 15 16:26:51 GMT 2023 , Edited by admin on Fri Dec 15 16:26:51 GMT 2023
PRIMARY
EVMPD
SUB23322
Created by admin on Fri Dec 15 16:26:51 GMT 2023 , Edited by admin on Fri Dec 15 16:26:51 GMT 2023
PRIMARY
CHEBI
49375
Created by admin on Fri Dec 15 16:26:51 GMT 2023 , Edited by admin on Fri Dec 15 16:26:51 GMT 2023
PRIMARY
PUBCHEM
3062316
Created by admin on Fri Dec 15 16:26:51 GMT 2023 , Edited by admin on Fri Dec 15 16:26:51 GMT 2023
PRIMARY
INN
8712
Created by admin on Fri Dec 15 16:26:51 GMT 2023 , Edited by admin on Fri Dec 15 16:26:51 GMT 2023
PRIMARY
DRUG BANK
DB01254
Created by admin on Fri Dec 15 16:26:51 GMT 2023 , Edited by admin on Fri Dec 15 16:26:51 GMT 2023
PRIMARY
CAS
302962-49-8
Created by admin on Fri Dec 15 16:26:51 GMT 2023 , Edited by admin on Fri Dec 15 16:26:51 GMT 2023
PRIMARY
DAILYMED
X78UG0A0RN
Created by admin on Fri Dec 15 16:26:51 GMT 2023 , Edited by admin on Fri Dec 15 16:26:51 GMT 2023
PRIMARY
FDA UNII
X78UG0A0RN
Created by admin on Fri Dec 15 16:26:51 GMT 2023 , Edited by admin on Fri Dec 15 16:26:51 GMT 2023
PRIMARY
SMS_ID
100000088015
Created by admin on Fri Dec 15 16:26:51 GMT 2023 , Edited by admin on Fri Dec 15 16:26:51 GMT 2023
PRIMARY
Related Record Type Details
TARGET -> INHIBITOR
IC50
SOLVATE->ANHYDROUS
EXCRETED UNCHANGED
URINE
TARGET -> INHIBITOR
IC50
SOLVATE->ANHYDROUS
METABOLIC ENZYME -> SUBSTRATE
TARGET -> INHIBITOR
IC50
RESISTANT TARGET->INHIBITOR
EXCRETED UNCHANGED
FECAL
BINDER->LIGAND
with no concentration dependence over the range of 100–500 ng/mL
BINDING
SOLVATE->ANHYDROUS
SALT/SOLVATE -> PARENT
TARGET -> INHIBITOR
IC50
TARGET -> INHIBITOR
IC50
TARGET -> INHIBITOR
IC50
SALT/SOLVATE -> PARENT
METABOLIC ENZYME -> SUBSTRATE
MAJOR
TARGET -> INHIBITOR
IC50
METABOLIC ENZYME -> INHIBITOR
In human liver microsomes, dasatinib was a weak time-dependent inhibitor of CYP3A4.
TIME-DEPENDENT INHIBITION
TARGET -> INHIBITOR
IC50
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Tmax PHARMACOKINETIC ORAL ADMINISTRATION

Volume of Distribution PHARMACOKINETIC
Biological Half-life PHARMACOKINETIC