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Details

Stereochemistry ABSOLUTE
Molecular Formula C45H57NO14
Molecular Weight 835.9341
Optical Activity UNSPECIFIED
Defined Stereocenters 11 / 11
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of CABAZITAXEL

SMILES

CC1=C2[C@]([H])(C(=O)[C@]3(C)[C@]([H])(C[C@]4([H])[C@@](CO4)([C@@]3([H])[C@@]([H])([C@](C[C@]1([H])OC(=O)[C@@]([H])([C@]([H])(c5ccccc5)N=C(O)OC(C)(C)C)O)(C2(C)C)O)OC(=O)c6ccccc6)OC(=O)C)OC)OC

InChI

InChIKey=BMQGVNUXMIRLCK-OAGWZNDDSA-N
InChI=1S/C45H57NO14/c1-24-28(57-39(51)33(48)32(26-17-13-11-14-18-26)46-40(52)60-41(3,4)5)22-45(53)37(58-38(50)27-19-15-12-16-20-27)35-43(8,36(49)34(55-10)31(24)42(45,6)7)29(54-9)21-30-44(35,23-56-30)59-25(2)47/h11-20,28-30,32-35,37,48,53H,21-23H2,1-10H3,(H,46,52)/t28-,29-,30+,32-,33+,34+,35-,37-,43+,44-,45+/m0/s1

HIDE SMILES / InChI
Cabazitaxel (JEVTANA®) is an antineoplastic agent belonging to the taxane class and is used to treat people with prostate cancer that has progressed despite treatment with docetaxel. It is prepared by semi-synthesis with a precursor extracted from yew needles (10-deacetylbaccatin III). Cabazitaxel (JEVTANA®) is a microtubule inhibitor. It binds to tubulin and promotes its assembly into microtubules while simultaneously inhibiting disassembly. This leads to the stabilization of microtubules, which results in the inhibition of mitotic and interphase cellular functions. The cell is then unable to progress further into the cell cycle, being stalled at metaphase, thus triggering apoptosis of the cancer cell.

CNS Activity

Curator's Comment:: Known to be CNS active in rats. Human data not available.

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
JEVTANA KIT

Approved Use

JEVTANA is a microtubule inhibitor indicated in combination with prednisone for treatment of patients with hormone-refractory metastatic prostate cancer previously treated with a docetaxel-containing treatment regimen.

Launch Date

1.27673277E12
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
226 ng/mL
25 mg/m² 1 times / 3 weeks multiple, intravenous
dose: 25 mg/m²
route of administration: Intravenous
experiment type: MULTIPLE
co-administered:
CABAZITAXEL plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
233.29 ng/mL
35 mg/m^2 single, intravenous
dose: 35 mg/m^2
route of administration: intravenous
experiment type: single
co-administered:
CABAZITAXEL plasma
Homo sapiens
population: unhealthy
age: Children
sex:
food status:
204.864 ng/mL
20 mg/m^2 single, intravenous
dose: 20 mg/m^2
route of administration: intravenous
experiment type: single
co-administered:
CABAZITAXEL plasma
Homo sapiens
population: unhealthy
age: Children
sex:
food status:
283.657 ng/mL
25 mg/m^2 single, intravenous
dose: 25 mg/m^2
route of administration: intravenous
experiment type: single
co-administered:
CABAZITAXEL plasma
Homo sapiens
population: unhealthy
age: Children
sex:
food status:
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
991 ng × h/mL
25 mg/m² 1 times / 3 weeks multiple, intravenous
dose: 25 mg/m²
route of administration: Intravenous
experiment type: MULTIPLE
co-administered:
CABAZITAXEL plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
1002.5 ng*h/mL
35 mg/m^2 single, intravenous
dose: 35 mg/m^2
route of administration: intravenous
experiment type: single
co-administered:
CABAZITAXEL plasma
Homo sapiens
population: unhealthy
age: Children
sex:
food status:
669.5 ng*h/mL
20 mg/m^2 single, intravenous
dose: 20 mg/m^2
route of administration: intravenous
experiment type: single
co-administered:
CABAZITAXEL plasma
Homo sapiens
population: unhealthy
age: Children
sex:
food status:
879 ng*h/mL
25 mg/m^2 single, intravenous
dose: 25 mg/m^2
route of administration: intravenous
experiment type: single
co-administered:
CABAZITAXEL plasma
Homo sapiens
population: unhealthy
age: Children
sex:
food status:
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
96 h
25 mg/m² 1 times / 3 weeks multiple, intravenous
dose: 25 mg/m²
route of administration: Intravenous
experiment type: MULTIPLE
co-administered:
CABAZITAXEL plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
9.5%
CABAZITAXEL serum
Homo sapiens
population: UNKNOWN
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
20 mg/m2 1 times / 3 weeks multiple, intravenous
Dose: 20 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 20 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, 11.0 years (range: 5–17 years)
n = 6
Health Status: unhealthy
Condition: refractory solid tumors
Age Group: 11.0 years (range: 5–17 years)
Sex: M+F
Population Size: 6
Sources:
DLT: Febrile neutropenia...
Dose limiting toxicities:
Febrile neutropenia (grade 3, 1 patient)
Sources:
20 mg/m2 1 times / 3 weeks multiple, intravenous
Dose: 20 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 20 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, 49 years (range: 34–67)
n = 7
Health Status: unhealthy
Condition: advanced solid tumours
Age Group: 49 years (range: 34–67)
Sex: M+F
Population Size: 7
Sources:
DLT: Diarrhoea, Neutropenia...
Dose limiting toxicities:
Diarrhoea (grade 3, 2 patients)
Neutropenia (grade 4, 1 patient)
Sources:
25 mg/m2 1 times / 3 weeks multiple, intravenous
Dose: 25 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 25 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, 54.0 years (range: 37–70 years)
n = 6
Health Status: unhealthy
Condition: advanced, non-hematologic cancer, mild hepatic impairment
Age Group: 54.0 years (range: 37–70 years)
Sex: M+F
Population Size: 6
Sources:
DLT: Febrile neutropenia, Hypophosphatemia...
Dose limiting toxicities:
Febrile neutropenia (grade 4, 5 patients)
Hypophosphatemia (grade 3, 5 patients)
Neutropenia (grade 4, 5 patients)
Sources:
20 mg/m2 1 times / 3 weeks multiple, intravenous
Dose: 20 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 20 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, 54.0 years (range: 48–60 years)
n = 2
Health Status: unhealthy
Condition: advanced, non-hematologic cancer, moderate hepatic impairment
Age Group: 54.0 years (range: 48–60 years)
Sex: F
Population Size: 2
Sources:
DLT: Neutropenic sepsis, Febrile neutropenia...
Dose limiting toxicities:
Neutropenic sepsis (grade 4, 2 patients)
Febrile neutropenia (grade 3, 2 patients)
Stoma site infection (grade 3, 2 patients)
Sources:
15 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 15 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 15 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, 56.0 years (range: 52–67 years)
n = 7
Health Status: unhealthy
Condition: advanced, non-hematologic cancer, moderate hepatic impairment
Age Group: 56.0 years (range: 52–67 years)
Sex: M+F
Population Size: 7
Sources:
Other AEs: Neutropenia, Febrile neutropenia...
Other AEs:
Neutropenia (57.1%)
Febrile neutropenia (14.3%)
Hepatic failure (14.3%)
Leukopenia (28.6%)
Jaundice (14.3%)
Cholangitis (14.3%)
Hyperbilirubinemia (14.3%)
Sources:
20 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 20 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 20 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, 59.0 years (range: 18–75 years)
n = 12
Health Status: unhealthy
Condition: advanced, non-hematologic cancer, mild hepatic impairment
Age Group: 59.0 years (range: 18–75 years)
Sex: M+F
Population Size: 12
Sources:
Other AEs: Neutropenia, Febrile neutropenia...
Other AEs:
Neutropenia (25%)
Febrile neutropenia (25%)
Anemia (16.7%)
Leukopenia (16.7%)
Lymphopenia (8.3%)
Diarrhoea (8.3%)
Dehydration (8.3%)
Platelet count decreased (16.7%)
White blood cell count decreased (8.3%)
Sources:
30 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 30 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 30 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, 63 years (range: 55–67 years)
n = 5
Health Status: unhealthy
Condition: advanced solid tumours
Age Group: 63 years (range: 55–67 years)
Sex: M
Population Size: 5
Sources:
DLT: Neutropenia, Febrile neutropenia...
Disc. AE: Thrombocytopenia...
Dose limiting toxicities:
Neutropenia (grade 4, 2 patients)
Febrile neutropenia (grade 4, 1 patient)
Bilirubin elevated (grade 3, 1 patient)
Diarrhoea (grade 3, 1 patient)
Neutropenic infection (grade 3, 1 patient)
AEs leading to
discontinuation/dose reduction:
Thrombocytopenia (2 patients)
Sources:
25 mg/m2 1 times / 3 weeks multiple, intravenous
Recommended
Dose: 25 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 25 mg/m2, 1 times / 3 weeks
Co-administed with::
prednisone(oral 10 mg daily)
Sources:
unhealthy, 68 years (range: 46-92 years)
n = 371
Health Status: unhealthy
Condition: hormone-refractory metastatic prostate cancer
Age Group: 68 years (range: 46-92 years)
Sex: M
Population Size: 371
Sources:
Disc. AE: Neutropenia, Renal failure...
AEs leading to
discontinuation/dose reduction:
Neutropenia (9 patients)
Renal failure (7 patients)
Sources:
25 mg/m2 1 times / 3 weeks multiple, intravenous
Recommended
Dose: 25 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 25 mg/m2, 1 times / 3 weeks
Co-administed with::
prednisone
Sources: Page: p. 59
unhealthy, 68 years (range: 46-92 years)
n = 371
Health Status: unhealthy
Condition: hormone-refractory metastatic prostate cancer
Age Group: 68 years (range: 46-92 years)
Sex: M
Population Size: 371
Sources: Page: p. 59
Disc. AE: Campylobacter infection, Urinary tract infection fungal...
AEs leading to
discontinuation/dose reduction:
Campylobacter infection (6 patients)
Urinary tract infection fungal (6 patients)
Hematuria (5 patients)
Neutropenic sepsis (5 patients)
Pneumococcal sepsis (5 patients)
Septic shock (5 patients)
Fatigue (4 patients)
Diarrhea (4 patients)
Abdominal pain (3 patients)
Febrile neutropenia (3 patients)
Anemia (2 patients)
Cardiac arrest (2 patients)
Deep vein thrombosis (2 patients)
Transaminases increased (2 patients)
Leukopenia (2 patients)
Sources: Page: p. 59
25 mg/m2 1 times / 3 weeks multiple, intravenous
Recommended
Dose: 25 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 25 mg/m2, 1 times / 3 weeks
Co-administed with::
prednisone(oral 10 mg daily)
Sources: Page: p. 59
unhealthy, 68 years (range: 46-92 years)
n = 371
Health Status: unhealthy
Condition: hormone-refractory metastatic prostate cancer
Age Group: 68 years (range: 46-92 years)
Sex: M
Population Size: 371
Sources: Page: p. 59
Disc. AE: Cellulitis, Pneumonia...
AEs leading to
discontinuation/dose reduction:
Cellulitis (6 patients)
Pneumonia (6 patients)
Salmonellosis (6 patients)
Sources: Page: p. 59
35 mg/m2 1 times / 3 weeks multiple, intravenous
Highest studied dose
Dose: 35 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 35 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, 7.0 years (range: 6–18 years)
n = 7
Health Status: unhealthy
Condition: refractory solid tumors
Age Group: 7.0 years (range: 6–18 years)
Sex: M+F
Population Size: 7
Sources:
DLT: Febrile neutropenia...
Dose limiting toxicities:
Febrile neutropenia (grade 3, 2 patients)
Sources:
30 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 30 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 30 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, 9.5 years (range: 3–16 years)
n = 16
Health Status: unhealthy
Condition: refractory solid tumors
Age Group: 9.5 years (range: 3–16 years)
Sex: M+F
Population Size: 16
Sources:
Disc. AE: Anaphylactic reaction, Transaminases increased...
Other AEs: Vomiting, Headache...
AEs leading to
discontinuation/dose reduction:
Anaphylactic reaction (serious, 3 patients)
Transaminases increased (grade 2, 1 patient)
Other AEs:
Vomiting (25%)
Headache (25%)
Nausea (31.3%)
Diarrhea (43.8%)
Dysphagia (37.5%)
Sources:
25 mg/m2 1 times / 3 weeks multiple, intravenous
Recommended
Dose: 25 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 25 mg/m2, 1 times / 3 weeks
Co-administed with::
prednisone(oral 10 mg daily)
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sources:
Other AEs: Neutropenia, Hypersensitivity reaction...
Other AEs:
Neutropenia (grade 5)
Hypersensitivity reaction (severe)
Sources:
AEs

AEs

AESignificanceDosePopulation
Febrile neutropenia grade 3, 1 patient
DLT
20 mg/m2 1 times / 3 weeks multiple, intravenous
Dose: 20 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 20 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, 11.0 years (range: 5–17 years)
n = 6
Health Status: unhealthy
Condition: refractory solid tumors
Age Group: 11.0 years (range: 5–17 years)
Sex: M+F
Population Size: 6
Sources:
Diarrhoea grade 3, 2 patients
DLT
20 mg/m2 1 times / 3 weeks multiple, intravenous
Dose: 20 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 20 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, 49 years (range: 34–67)
n = 7
Health Status: unhealthy
Condition: advanced solid tumours
Age Group: 49 years (range: 34–67)
Sex: M+F
Population Size: 7
Sources:
Neutropenia grade 4, 1 patient
DLT
20 mg/m2 1 times / 3 weeks multiple, intravenous
Dose: 20 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 20 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, 49 years (range: 34–67)
n = 7
Health Status: unhealthy
Condition: advanced solid tumours
Age Group: 49 years (range: 34–67)
Sex: M+F
Population Size: 7
Sources:
Hypophosphatemia grade 3, 5 patients
DLT
25 mg/m2 1 times / 3 weeks multiple, intravenous
Dose: 25 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 25 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, 54.0 years (range: 37–70 years)
n = 6
Health Status: unhealthy
Condition: advanced, non-hematologic cancer, mild hepatic impairment
Age Group: 54.0 years (range: 37–70 years)
Sex: M+F
Population Size: 6
Sources:
Febrile neutropenia grade 4, 5 patients
DLT
25 mg/m2 1 times / 3 weeks multiple, intravenous
Dose: 25 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 25 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, 54.0 years (range: 37–70 years)
n = 6
Health Status: unhealthy
Condition: advanced, non-hematologic cancer, mild hepatic impairment
Age Group: 54.0 years (range: 37–70 years)
Sex: M+F
Population Size: 6
Sources:
Neutropenia grade 4, 5 patients
DLT
25 mg/m2 1 times / 3 weeks multiple, intravenous
Dose: 25 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 25 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, 54.0 years (range: 37–70 years)
n = 6
Health Status: unhealthy
Condition: advanced, non-hematologic cancer, mild hepatic impairment
Age Group: 54.0 years (range: 37–70 years)
Sex: M+F
Population Size: 6
Sources:
Febrile neutropenia grade 3, 2 patients
DLT
20 mg/m2 1 times / 3 weeks multiple, intravenous
Dose: 20 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 20 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, 54.0 years (range: 48–60 years)
n = 2
Health Status: unhealthy
Condition: advanced, non-hematologic cancer, moderate hepatic impairment
Age Group: 54.0 years (range: 48–60 years)
Sex: F
Population Size: 2
Sources:
Stoma site infection grade 3, 2 patients
DLT
20 mg/m2 1 times / 3 weeks multiple, intravenous
Dose: 20 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 20 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, 54.0 years (range: 48–60 years)
n = 2
Health Status: unhealthy
Condition: advanced, non-hematologic cancer, moderate hepatic impairment
Age Group: 54.0 years (range: 48–60 years)
Sex: F
Population Size: 2
Sources:
Neutropenic sepsis grade 4, 2 patients
DLT
20 mg/m2 1 times / 3 weeks multiple, intravenous
Dose: 20 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 20 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, 54.0 years (range: 48–60 years)
n = 2
Health Status: unhealthy
Condition: advanced, non-hematologic cancer, moderate hepatic impairment
Age Group: 54.0 years (range: 48–60 years)
Sex: F
Population Size: 2
Sources:
Cholangitis 14.3%
15 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 15 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 15 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, 56.0 years (range: 52–67 years)
n = 7
Health Status: unhealthy
Condition: advanced, non-hematologic cancer, moderate hepatic impairment
Age Group: 56.0 years (range: 52–67 years)
Sex: M+F
Population Size: 7
Sources:
Febrile neutropenia 14.3%
15 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 15 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 15 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, 56.0 years (range: 52–67 years)
n = 7
Health Status: unhealthy
Condition: advanced, non-hematologic cancer, moderate hepatic impairment
Age Group: 56.0 years (range: 52–67 years)
Sex: M+F
Population Size: 7
Sources:
Hepatic failure 14.3%
15 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 15 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 15 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, 56.0 years (range: 52–67 years)
n = 7
Health Status: unhealthy
Condition: advanced, non-hematologic cancer, moderate hepatic impairment
Age Group: 56.0 years (range: 52–67 years)
Sex: M+F
Population Size: 7
Sources:
Hyperbilirubinemia 14.3%
15 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 15 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 15 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, 56.0 years (range: 52–67 years)
n = 7
Health Status: unhealthy
Condition: advanced, non-hematologic cancer, moderate hepatic impairment
Age Group: 56.0 years (range: 52–67 years)
Sex: M+F
Population Size: 7
Sources:
Jaundice 14.3%
15 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 15 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 15 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, 56.0 years (range: 52–67 years)
n = 7
Health Status: unhealthy
Condition: advanced, non-hematologic cancer, moderate hepatic impairment
Age Group: 56.0 years (range: 52–67 years)
Sex: M+F
Population Size: 7
Sources:
Leukopenia 28.6%
15 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 15 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 15 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, 56.0 years (range: 52–67 years)
n = 7
Health Status: unhealthy
Condition: advanced, non-hematologic cancer, moderate hepatic impairment
Age Group: 56.0 years (range: 52–67 years)
Sex: M+F
Population Size: 7
Sources:
Neutropenia 57.1%
15 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 15 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 15 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, 56.0 years (range: 52–67 years)
n = 7
Health Status: unhealthy
Condition: advanced, non-hematologic cancer, moderate hepatic impairment
Age Group: 56.0 years (range: 52–67 years)
Sex: M+F
Population Size: 7
Sources:
Anemia 16.7%
20 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 20 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 20 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, 59.0 years (range: 18–75 years)
n = 12
Health Status: unhealthy
Condition: advanced, non-hematologic cancer, mild hepatic impairment
Age Group: 59.0 years (range: 18–75 years)
Sex: M+F
Population Size: 12
Sources:
Leukopenia 16.7%
20 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 20 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 20 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, 59.0 years (range: 18–75 years)
n = 12
Health Status: unhealthy
Condition: advanced, non-hematologic cancer, mild hepatic impairment
Age Group: 59.0 years (range: 18–75 years)
Sex: M+F
Population Size: 12
Sources:
Platelet count decreased 16.7%
20 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 20 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 20 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, 59.0 years (range: 18–75 years)
n = 12
Health Status: unhealthy
Condition: advanced, non-hematologic cancer, mild hepatic impairment
Age Group: 59.0 years (range: 18–75 years)
Sex: M+F
Population Size: 12
Sources:
Febrile neutropenia 25%
20 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 20 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 20 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, 59.0 years (range: 18–75 years)
n = 12
Health Status: unhealthy
Condition: advanced, non-hematologic cancer, mild hepatic impairment
Age Group: 59.0 years (range: 18–75 years)
Sex: M+F
Population Size: 12
Sources:
Neutropenia 25%
20 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 20 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 20 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, 59.0 years (range: 18–75 years)
n = 12
Health Status: unhealthy
Condition: advanced, non-hematologic cancer, mild hepatic impairment
Age Group: 59.0 years (range: 18–75 years)
Sex: M+F
Population Size: 12
Sources:
Dehydration 8.3%
20 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 20 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 20 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, 59.0 years (range: 18–75 years)
n = 12
Health Status: unhealthy
Condition: advanced, non-hematologic cancer, mild hepatic impairment
Age Group: 59.0 years (range: 18–75 years)
Sex: M+F
Population Size: 12
Sources:
Diarrhoea 8.3%
20 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 20 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 20 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, 59.0 years (range: 18–75 years)
n = 12
Health Status: unhealthy
Condition: advanced, non-hematologic cancer, mild hepatic impairment
Age Group: 59.0 years (range: 18–75 years)
Sex: M+F
Population Size: 12
Sources:
Lymphopenia 8.3%
20 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 20 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 20 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, 59.0 years (range: 18–75 years)
n = 12
Health Status: unhealthy
Condition: advanced, non-hematologic cancer, mild hepatic impairment
Age Group: 59.0 years (range: 18–75 years)
Sex: M+F
Population Size: 12
Sources:
White blood cell count decreased 8.3%
20 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 20 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 20 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, 59.0 years (range: 18–75 years)
n = 12
Health Status: unhealthy
Condition: advanced, non-hematologic cancer, mild hepatic impairment
Age Group: 59.0 years (range: 18–75 years)
Sex: M+F
Population Size: 12
Sources:
Thrombocytopenia 2 patients
Disc. AE
30 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 30 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 30 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, 63 years (range: 55–67 years)
n = 5
Health Status: unhealthy
Condition: advanced solid tumours
Age Group: 63 years (range: 55–67 years)
Sex: M
Population Size: 5
Sources:
Bilirubin elevated grade 3, 1 patient
DLT
30 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 30 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 30 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, 63 years (range: 55–67 years)
n = 5
Health Status: unhealthy
Condition: advanced solid tumours
Age Group: 63 years (range: 55–67 years)
Sex: M
Population Size: 5
Sources:
Diarrhoea grade 3, 1 patient
DLT
30 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 30 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 30 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, 63 years (range: 55–67 years)
n = 5
Health Status: unhealthy
Condition: advanced solid tumours
Age Group: 63 years (range: 55–67 years)
Sex: M
Population Size: 5
Sources:
Neutropenic infection grade 3, 1 patient
DLT
30 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 30 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 30 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, 63 years (range: 55–67 years)
n = 5
Health Status: unhealthy
Condition: advanced solid tumours
Age Group: 63 years (range: 55–67 years)
Sex: M
Population Size: 5
Sources:
Febrile neutropenia grade 4, 1 patient
DLT
30 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 30 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 30 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, 63 years (range: 55–67 years)
n = 5
Health Status: unhealthy
Condition: advanced solid tumours
Age Group: 63 years (range: 55–67 years)
Sex: M
Population Size: 5
Sources:
Neutropenia grade 4, 2 patients
DLT
30 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 30 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 30 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, 63 years (range: 55–67 years)
n = 5
Health Status: unhealthy
Condition: advanced solid tumours
Age Group: 63 years (range: 55–67 years)
Sex: M
Population Size: 5
Sources:
Renal failure 7 patients
Disc. AE
25 mg/m2 1 times / 3 weeks multiple, intravenous
Recommended
Dose: 25 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 25 mg/m2, 1 times / 3 weeks
Co-administed with::
prednisone(oral 10 mg daily)
Sources:
unhealthy, 68 years (range: 46-92 years)
n = 371
Health Status: unhealthy
Condition: hormone-refractory metastatic prostate cancer
Age Group: 68 years (range: 46-92 years)
Sex: M
Population Size: 371
Sources:
Neutropenia 9 patients
Disc. AE
25 mg/m2 1 times / 3 weeks multiple, intravenous
Recommended
Dose: 25 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 25 mg/m2, 1 times / 3 weeks
Co-administed with::
prednisone(oral 10 mg daily)
Sources:
unhealthy, 68 years (range: 46-92 years)
n = 371
Health Status: unhealthy
Condition: hormone-refractory metastatic prostate cancer
Age Group: 68 years (range: 46-92 years)
Sex: M
Population Size: 371
Sources:
Anemia 2 patients
Disc. AE
25 mg/m2 1 times / 3 weeks multiple, intravenous
Recommended
Dose: 25 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 25 mg/m2, 1 times / 3 weeks
Co-administed with::
prednisone
Sources: Page: p. 59
unhealthy, 68 years (range: 46-92 years)
n = 371
Health Status: unhealthy
Condition: hormone-refractory metastatic prostate cancer
Age Group: 68 years (range: 46-92 years)
Sex: M
Population Size: 371
Sources: Page: p. 59
Cardiac arrest 2 patients
Disc. AE
25 mg/m2 1 times / 3 weeks multiple, intravenous
Recommended
Dose: 25 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 25 mg/m2, 1 times / 3 weeks
Co-administed with::
prednisone
Sources: Page: p. 59
unhealthy, 68 years (range: 46-92 years)
n = 371
Health Status: unhealthy
Condition: hormone-refractory metastatic prostate cancer
Age Group: 68 years (range: 46-92 years)
Sex: M
Population Size: 371
Sources: Page: p. 59
Deep vein thrombosis 2 patients
Disc. AE
25 mg/m2 1 times / 3 weeks multiple, intravenous
Recommended
Dose: 25 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 25 mg/m2, 1 times / 3 weeks
Co-administed with::
prednisone
Sources: Page: p. 59
unhealthy, 68 years (range: 46-92 years)
n = 371
Health Status: unhealthy
Condition: hormone-refractory metastatic prostate cancer
Age Group: 68 years (range: 46-92 years)
Sex: M
Population Size: 371
Sources: Page: p. 59
Leukopenia 2 patients
Disc. AE
25 mg/m2 1 times / 3 weeks multiple, intravenous
Recommended
Dose: 25 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 25 mg/m2, 1 times / 3 weeks
Co-administed with::
prednisone
Sources: Page: p. 59
unhealthy, 68 years (range: 46-92 years)
n = 371
Health Status: unhealthy
Condition: hormone-refractory metastatic prostate cancer
Age Group: 68 years (range: 46-92 years)
Sex: M
Population Size: 371
Sources: Page: p. 59
Transaminases increased 2 patients
Disc. AE
25 mg/m2 1 times / 3 weeks multiple, intravenous
Recommended
Dose: 25 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 25 mg/m2, 1 times / 3 weeks
Co-administed with::
prednisone
Sources: Page: p. 59
unhealthy, 68 years (range: 46-92 years)
n = 371
Health Status: unhealthy
Condition: hormone-refractory metastatic prostate cancer
Age Group: 68 years (range: 46-92 years)
Sex: M
Population Size: 371
Sources: Page: p. 59
Abdominal pain 3 patients
Disc. AE
25 mg/m2 1 times / 3 weeks multiple, intravenous
Recommended
Dose: 25 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 25 mg/m2, 1 times / 3 weeks
Co-administed with::
prednisone
Sources: Page: p. 59
unhealthy, 68 years (range: 46-92 years)
n = 371
Health Status: unhealthy
Condition: hormone-refractory metastatic prostate cancer
Age Group: 68 years (range: 46-92 years)
Sex: M
Population Size: 371
Sources: Page: p. 59
Febrile neutropenia 3 patients
Disc. AE
25 mg/m2 1 times / 3 weeks multiple, intravenous
Recommended
Dose: 25 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 25 mg/m2, 1 times / 3 weeks
Co-administed with::
prednisone
Sources: Page: p. 59
unhealthy, 68 years (range: 46-92 years)
n = 371
Health Status: unhealthy
Condition: hormone-refractory metastatic prostate cancer
Age Group: 68 years (range: 46-92 years)
Sex: M
Population Size: 371
Sources: Page: p. 59
Diarrhea 4 patients
Disc. AE
25 mg/m2 1 times / 3 weeks multiple, intravenous
Recommended
Dose: 25 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 25 mg/m2, 1 times / 3 weeks
Co-administed with::
prednisone
Sources: Page: p. 59
unhealthy, 68 years (range: 46-92 years)
n = 371
Health Status: unhealthy
Condition: hormone-refractory metastatic prostate cancer
Age Group: 68 years (range: 46-92 years)
Sex: M
Population Size: 371
Sources: Page: p. 59
Fatigue 4 patients
Disc. AE
25 mg/m2 1 times / 3 weeks multiple, intravenous
Recommended
Dose: 25 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 25 mg/m2, 1 times / 3 weeks
Co-administed with::
prednisone
Sources: Page: p. 59
unhealthy, 68 years (range: 46-92 years)
n = 371
Health Status: unhealthy
Condition: hormone-refractory metastatic prostate cancer
Age Group: 68 years (range: 46-92 years)
Sex: M
Population Size: 371
Sources: Page: p. 59
Hematuria 5 patients
Disc. AE
25 mg/m2 1 times / 3 weeks multiple, intravenous
Recommended
Dose: 25 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 25 mg/m2, 1 times / 3 weeks
Co-administed with::
prednisone
Sources: Page: p. 59
unhealthy, 68 years (range: 46-92 years)
n = 371
Health Status: unhealthy
Condition: hormone-refractory metastatic prostate cancer
Age Group: 68 years (range: 46-92 years)
Sex: M
Population Size: 371
Sources: Page: p. 59
Neutropenic sepsis 5 patients
Disc. AE
25 mg/m2 1 times / 3 weeks multiple, intravenous
Recommended
Dose: 25 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 25 mg/m2, 1 times / 3 weeks
Co-administed with::
prednisone
Sources: Page: p. 59
unhealthy, 68 years (range: 46-92 years)
n = 371
Health Status: unhealthy
Condition: hormone-refractory metastatic prostate cancer
Age Group: 68 years (range: 46-92 years)
Sex: M
Population Size: 371
Sources: Page: p. 59
Pneumococcal sepsis 5 patients
Disc. AE
25 mg/m2 1 times / 3 weeks multiple, intravenous
Recommended
Dose: 25 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 25 mg/m2, 1 times / 3 weeks
Co-administed with::
prednisone
Sources: Page: p. 59
unhealthy, 68 years (range: 46-92 years)
n = 371
Health Status: unhealthy
Condition: hormone-refractory metastatic prostate cancer
Age Group: 68 years (range: 46-92 years)
Sex: M
Population Size: 371
Sources: Page: p. 59
Septic shock 5 patients
Disc. AE
25 mg/m2 1 times / 3 weeks multiple, intravenous
Recommended
Dose: 25 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 25 mg/m2, 1 times / 3 weeks
Co-administed with::
prednisone
Sources: Page: p. 59
unhealthy, 68 years (range: 46-92 years)
n = 371
Health Status: unhealthy
Condition: hormone-refractory metastatic prostate cancer
Age Group: 68 years (range: 46-92 years)
Sex: M
Population Size: 371
Sources: Page: p. 59
Campylobacter infection 6 patients
Disc. AE
25 mg/m2 1 times / 3 weeks multiple, intravenous
Recommended
Dose: 25 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 25 mg/m2, 1 times / 3 weeks
Co-administed with::
prednisone
Sources: Page: p. 59
unhealthy, 68 years (range: 46-92 years)
n = 371
Health Status: unhealthy
Condition: hormone-refractory metastatic prostate cancer
Age Group: 68 years (range: 46-92 years)
Sex: M
Population Size: 371
Sources: Page: p. 59
Urinary tract infection fungal 6 patients
Disc. AE
25 mg/m2 1 times / 3 weeks multiple, intravenous
Recommended
Dose: 25 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 25 mg/m2, 1 times / 3 weeks
Co-administed with::
prednisone
Sources: Page: p. 59
unhealthy, 68 years (range: 46-92 years)
n = 371
Health Status: unhealthy
Condition: hormone-refractory metastatic prostate cancer
Age Group: 68 years (range: 46-92 years)
Sex: M
Population Size: 371
Sources: Page: p. 59
Cellulitis 6 patients
Disc. AE
25 mg/m2 1 times / 3 weeks multiple, intravenous
Recommended
Dose: 25 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 25 mg/m2, 1 times / 3 weeks
Co-administed with::
prednisone(oral 10 mg daily)
Sources: Page: p. 59
unhealthy, 68 years (range: 46-92 years)
n = 371
Health Status: unhealthy
Condition: hormone-refractory metastatic prostate cancer
Age Group: 68 years (range: 46-92 years)
Sex: M
Population Size: 371
Sources: Page: p. 59
Pneumonia 6 patients
Disc. AE
25 mg/m2 1 times / 3 weeks multiple, intravenous
Recommended
Dose: 25 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 25 mg/m2, 1 times / 3 weeks
Co-administed with::
prednisone(oral 10 mg daily)
Sources: Page: p. 59
unhealthy, 68 years (range: 46-92 years)
n = 371
Health Status: unhealthy
Condition: hormone-refractory metastatic prostate cancer
Age Group: 68 years (range: 46-92 years)
Sex: M
Population Size: 371
Sources: Page: p. 59
Salmonellosis 6 patients
Disc. AE
25 mg/m2 1 times / 3 weeks multiple, intravenous
Recommended
Dose: 25 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 25 mg/m2, 1 times / 3 weeks
Co-administed with::
prednisone(oral 10 mg daily)
Sources: Page: p. 59
unhealthy, 68 years (range: 46-92 years)
n = 371
Health Status: unhealthy
Condition: hormone-refractory metastatic prostate cancer
Age Group: 68 years (range: 46-92 years)
Sex: M
Population Size: 371
Sources: Page: p. 59
Febrile neutropenia grade 3, 2 patients
DLT
35 mg/m2 1 times / 3 weeks multiple, intravenous
Highest studied dose
Dose: 35 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 35 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, 7.0 years (range: 6–18 years)
n = 7
Health Status: unhealthy
Condition: refractory solid tumors
Age Group: 7.0 years (range: 6–18 years)
Sex: M+F
Population Size: 7
Sources:
Headache 25%
30 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 30 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 30 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, 9.5 years (range: 3–16 years)
n = 16
Health Status: unhealthy
Condition: refractory solid tumors
Age Group: 9.5 years (range: 3–16 years)
Sex: M+F
Population Size: 16
Sources:
Vomiting 25%
30 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 30 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 30 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, 9.5 years (range: 3–16 years)
n = 16
Health Status: unhealthy
Condition: refractory solid tumors
Age Group: 9.5 years (range: 3–16 years)
Sex: M+F
Population Size: 16
Sources:
Nausea 31.3%
30 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 30 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 30 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, 9.5 years (range: 3–16 years)
n = 16
Health Status: unhealthy
Condition: refractory solid tumors
Age Group: 9.5 years (range: 3–16 years)
Sex: M+F
Population Size: 16
Sources:
Dysphagia 37.5%
30 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 30 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 30 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, 9.5 years (range: 3–16 years)
n = 16
Health Status: unhealthy
Condition: refractory solid tumors
Age Group: 9.5 years (range: 3–16 years)
Sex: M+F
Population Size: 16
Sources:
Diarrhea 43.8%
30 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 30 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 30 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, 9.5 years (range: 3–16 years)
n = 16
Health Status: unhealthy
Condition: refractory solid tumors
Age Group: 9.5 years (range: 3–16 years)
Sex: M+F
Population Size: 16
Sources:
Transaminases increased grade 2, 1 patient
Disc. AE
30 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 30 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 30 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, 9.5 years (range: 3–16 years)
n = 16
Health Status: unhealthy
Condition: refractory solid tumors
Age Group: 9.5 years (range: 3–16 years)
Sex: M+F
Population Size: 16
Sources:
Anaphylactic reaction serious, 3 patients
Disc. AE
30 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 30 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 30 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, 9.5 years (range: 3–16 years)
n = 16
Health Status: unhealthy
Condition: refractory solid tumors
Age Group: 9.5 years (range: 3–16 years)
Sex: M+F
Population Size: 16
Sources:
Neutropenia grade 5
25 mg/m2 1 times / 3 weeks multiple, intravenous
Recommended
Dose: 25 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 25 mg/m2, 1 times / 3 weeks
Co-administed with::
prednisone(oral 10 mg daily)
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sources:
Hypersensitivity reaction severe
25 mg/m2 1 times / 3 weeks multiple, intravenous
Recommended
Dose: 25 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 25 mg/m2, 1 times / 3 weeks
Co-administed with::
prednisone(oral 10 mg daily)
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sources:
OverviewDrug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
no
no
no
no
no
no
unlikely [IC50 10.8 uM]
unlikely [IC50 41.8 uM]
unlikely [Ki 1.99 uM]
unlikely [Ki 130 uM]
unlikely [Ki 19.7 uM]
unlikely [Ki 3.26 uM]
unlikely [Ki 79.1 uM]
unlikely
unlikely
unlikely
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
major
unlikely (co-administration study)
Comment: Metabolised 80% to 90%, Recombinant isoform; Human liver microsomes; Weak CYP3A inducers prednisone or its metabolite, prednisolone, did not decrease cabazitaxel exposure (AUC) when given in combination with prednisone/prednisolone administered orally at 10-mg daily for three weeks.
Page: (ClinPharm) 6, 24, 25, 36, 38
minor
no
no
no
no
no
no
no
no
no
no
no
no
no
no
yes
Tox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
PubMed

PubMed

TitleDatePubMed
Cabazitaxel.
2010 Sep
Cabazitaxel (jevtana): a novel agent for metastatic castration-resistant prostate cancer.
2012 Aug
Quantification of cabazitaxel, its metabolite docetaxel and the determination of the demethylated metabolites RPR112698 and RPR123142 as docetaxel equivalents in human plasma by liquid chromatography-tandem mass spectrometry.
2013 Apr 15
Molecular alterations and emerging targets in castration resistant prostate cancer.
2014 Mar
Patents

Sample Use Guides

JEVTANA® 25 mg/m2 administered every three weeks as a one-hour intravenous infusion in combination with oral prednisone 10 mg administered daily throughout JEVTANA® treatment.
Route of Administration: Intravenous
Cabazitaxel and docetaxel were tested in vitro against the cancer cell line panel at concentrations from 0.01 to 0.1 uM and in vivo against a subset of the solid tumor xenograft models at a dose of 10 or 7.5 mg/kg on an every 4 days × 3 I.V. schedule. In vitro, both cabazitaxel and docetaxel had similar potency (median relative IC50 0.47 nM and 0.88 nM, respectively) and a similar activity profile, with Ewing sarcoma cells being significantly more sensitive to both agents. In vitro sensitivity to docetaxel inversely correlated with mRNA expression for ABCB1, but the correlation with ABCB1 expression was weaker for cabazitaxel. In vivo cabazitaxel demonstrated significantly greater activity than docetaxel in five of 12 tumor models, inducing regressions in six models compared with three models for docetaxel.
Name Type Language
CABAZITAXEL
EMA EPAR   INN   MART.   MI   ORANGE BOOK   USAN   VANDF   WHO-DD  
INN   USAN  
Official Name English
TXD 258
Code English
CABAZITAXEL [MI]
Common Name English
NSC-761432
Code English
CABAZITAXEL ACETONATE [JAN]
Common Name English
XRP 6258
Code English
CABAZITAXEL [EMA EPAR]
Common Name English
CABAZITAXEL [USAN]
Common Name English
CABAZITAXEL [VANDF]
Common Name English
CABAZITAXEL [MART.]
Common Name English
CABAZITAXEL [ORANGE BOOK]
Common Name English
1-HYDROXY-7.BETA.,10.BETA.-DIMETHOXY-9-OXO-5.BETA.,20-EPOXYTAX-11-ENE-2.ALPHA.,4,13.ALPHA.-TRIYL 4-ACETATE 2-BENZOATE 13-((2R,3S)-3-(((TERT-BUTOXY)CARBONYL)AMINO)-2-HYDROXY-3-PHENYLPROPANOATE)
Common Name English
XRP-6258
Code English
CABAZITAXEL [WHO-DD]
Common Name English
TXD-258
Code English
CABAZITAXEL [INN]
Common Name English
JEVTANA
Brand Name English
Classification Tree Code System Code
NDF-RT N0000175085
Created by admin on Fri Jun 25 22:09:28 UTC 2021 , Edited by admin on Fri Jun 25 22:09:28 UTC 2021
NDF-RT N0000175592
Created by admin on Fri Jun 25 22:09:28 UTC 2021 , Edited by admin on Fri Jun 25 22:09:28 UTC 2021
NCI_THESAURUS C67437
Created by admin on Fri Jun 25 22:09:28 UTC 2021 , Edited by admin on Fri Jun 25 22:09:28 UTC 2021
WHO-ATC L01CD04
Created by admin on Fri Jun 25 22:09:28 UTC 2021 , Edited by admin on Fri Jun 25 22:09:28 UTC 2021
EMA ASSESSMENT REPORTS JETVANA (AUTHORIZED: PROSTATIC, NEOPLASMS)
Created by admin on Fri Jun 25 22:09:28 UTC 2021 , Edited by admin on Fri Jun 25 22:09:28 UTC 2021
NCI_THESAURUS C1490
Created by admin on Fri Jun 25 22:09:28 UTC 2021 , Edited by admin on Fri Jun 25 22:09:28 UTC 2021
LIVERTOX 134
Created by admin on Fri Jun 25 22:09:28 UTC 2021 , Edited by admin on Fri Jun 25 22:09:28 UTC 2021
WHO-VATC QL01CD04
Created by admin on Fri Jun 25 22:09:28 UTC 2021 , Edited by admin on Fri Jun 25 22:09:28 UTC 2021
Code System Code Type Description
MESH
C552428
Created by admin on Fri Jun 25 22:09:28 UTC 2021 , Edited by admin on Fri Jun 25 22:09:28 UTC 2021
PRIMARY
DRUG BANK
DB06772
Created by admin on Fri Jun 25 22:09:28 UTC 2021 , Edited by admin on Fri Jun 25 22:09:28 UTC 2021
PRIMARY
CAS
183133-96-2
Created by admin on Fri Jun 25 22:09:28 UTC 2021 , Edited by admin on Fri Jun 25 22:09:28 UTC 2021
PRIMARY
DRUG CENTRAL
4153
Created by admin on Fri Jun 25 22:09:28 UTC 2021 , Edited by admin on Fri Jun 25 22:09:28 UTC 2021
PRIMARY
PUBCHEM
9854073
Created by admin on Fri Jun 25 22:09:28 UTC 2021 , Edited by admin on Fri Jun 25 22:09:28 UTC 2021
PRIMARY
EPA CompTox
183133-96-2
Created by admin on Fri Jun 25 22:09:28 UTC 2021 , Edited by admin on Fri Jun 25 22:09:28 UTC 2021
PRIMARY
RXCUI
996051
Created by admin on Fri Jun 25 22:09:28 UTC 2021 , Edited by admin on Fri Jun 25 22:09:28 UTC 2021
PRIMARY RxNorm
WIKIPEDIA
CABAZITAXEL
Created by admin on Fri Jun 25 22:09:28 UTC 2021 , Edited by admin on Fri Jun 25 22:09:28 UTC 2021
PRIMARY
MERCK INDEX
M2874
Created by admin on Fri Jun 25 22:09:28 UTC 2021 , Edited by admin on Fri Jun 25 22:09:28 UTC 2021
PRIMARY Merck Index
ChEMBL
CHEMBL1201748
Created by admin on Fri Jun 25 22:09:28 UTC 2021 , Edited by admin on Fri Jun 25 22:09:28 UTC 2021
PRIMARY
NCI_THESAURUS
C66937
Created by admin on Fri Jun 25 22:09:28 UTC 2021 , Edited by admin on Fri Jun 25 22:09:28 UTC 2021
PRIMARY
IUPHAR
6798
Created by admin on Fri Jun 25 22:09:28 UTC 2021 , Edited by admin on Fri Jun 25 22:09:28 UTC 2021
PRIMARY
EVMPD
SUB31282
Created by admin on Fri Jun 25 22:09:28 UTC 2021 , Edited by admin on Fri Jun 25 22:09:28 UTC 2021
PRIMARY
FDA UNII
51F690397J
Created by admin on Fri Jun 25 22:09:28 UTC 2021 , Edited by admin on Fri Jun 25 22:09:28 UTC 2021
PRIMARY
INN
8967
Created by admin on Fri Jun 25 22:09:28 UTC 2021 , Edited by admin on Fri Jun 25 22:09:28 UTC 2021
PRIMARY