Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C45H57NO14.H2O |
| Molecular Weight | 853.9477 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 11 / 11 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
O.[H][C@@]12C[C@H](OC)[C@@]3(C)C(=O)[C@H](OC)C4=C(C)[C@H](C[C@@](O)([C@@H](OC(=O)C5=CC=CC=C5)[C@]3([H])[C@@]1(CO2)OC(C)=O)C4(C)C)OC(=O)[C@H](O)[C@@H](NC(=O)OC(C)(C)C)C6=CC=CC=C6
InChI
InChIKey=CHVARVMIVJJZTG-JVXKREHESA-N
InChI=1S/C45H57NO14.H2O/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);1H2/t28-,29-,30+,32-,33+,34+,35-,37-,43+,44-,45+;/m0./s1
| Molecular Formula | C45H57NO14 |
| Molecular Weight | 835.9324 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 11 / 11 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
| Molecular Formula | H2O |
| Molecular Weight | 18.0153 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
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.
Originator
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: GO:0007019 |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | JEVTANA KIT Approved UseJEVTANA 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 Date2010 |
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
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 Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01751308 |
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 Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01751308 |
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 Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01751308 |
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
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
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 Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01751308 |
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 Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01751308 |
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 Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01751308 |
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
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
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
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
9.5% |
CABAZITAXEL serum | Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
Doses
| Dose | Population | Adverse 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) Sources: Neutropenia (grade 4, 1 patient) |
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) Sources: Hypophosphatemia (grade 3, 5 patients) Neutropenia (grade 4, 5 patients) |
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) Sources: Febrile neutropenia (grade 3, 2 patients) Stoma site infection (grade 3, 2 patients) |
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%) Sources: Febrile neutropenia (14.3%) Hepatic failure (14.3%) Leukopenia (28.6%) Jaundice (14.3%) Cholangitis (14.3%) Hyperbilirubinemia (14.3%) |
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: |
Other AEs: Neutropenia, Febrile neutropenia... Other AEs: Neutropenia (25%) Sources: 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%) |
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) AEs leading toFebrile neutropenia (grade 4, 1 patient) Bilirubin elevated (grade 3, 1 patient) Diarrhoea (grade 3, 1 patient) Neutropenic infection (grade 3, 1 patient) 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) Sources: Renal failure (7 patients) |
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) Sources: Page: p. 59Urinary 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) |
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) Sources: Page: p. 59Pneumonia (6 patients) Salmonellosis (6 patients) |
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) Other AEs:Transaminases increased (grade 2, 1 patient) Vomiting (25%) Sources: Headache (25%) Nausea (31.3%) Diarrhea (43.8%) Dysphagia (37.5%) |
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: |
Other AEs: Neutropenia, Hypersensitivity reaction... Other AEs: Neutropenia (grade 5) Sources: Hypersensitivity reaction (severe) |
AEs
| AE | Significance | Dose | Population |
|---|---|---|---|
| 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: |
Overview
| CYP3A4 | CYP2C9 | CYP2D6 | hERG |
|---|---|---|---|
OverviewOther
Drug as perpetrator
| Target | Modality | Activity | Metabolite | Clinical evidence |
|---|---|---|---|---|
Page: (ClinPharm) 6, 37-38 |
no | |||
Page: (ClinPharm) 6, 37-38 |
no | |||
Page: (ClinPharm) 6, 37-38 |
no | |||
Page: (ClinPharm) 6, 36, 37 |
no | |||
| no | ||||
| no | ||||
| unlikely [IC50 10.8 uM] | ||||
| unlikely [IC50 41.8 uM] | ||||
Page: (ClinPharm) 6, 36, 37 |
unlikely [Ki 1.99 uM] | |||
Page: (ClinPharm) 6, 36, 37 |
unlikely [Ki 130 uM] | |||
Page: (ClinPharm) 6, 36, 37 |
unlikely [Ki 19.7 uM] | |||
Page: (ClinPharm) 6, 36, 37 |
unlikely [Ki 3.26 uM] | |||
Page: (ClinPharm) 6, 36, 37 |
unlikely [Ki 79.1 uM] | |||
Page: (ClinPharm) 6, 36, 37 |
unlikely | |||
Page: (ClinPharm) 6, 36, 37 |
unlikely | |||
Page: (ClinPharm) 6, 36, 37 |
unlikely |
Drug as victim
| Target | Modality | Activity | Metabolite | Clinical 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 |
|||
Page: (ClinPharm) 6, 24, 25, 36 |
minor | |||
| no | ||||
Page: (ClinPharm) 25 |
no | |||
Page: (ClinPharm) 25 |
no | |||
Page: (ClinPharm) 25 |
no | |||
Page: (ClinPharm) 25 |
no | |||
Page: (ClinPharm) 25 |
no | |||
Page: (ClinPharm) 25 |
no | |||
Page: (ClinPharm) 25 |
no | |||
Page: (ClinPharm) 25 |
no | |||
Page: (ClinPharm) 25 |
no | |||
Page: (ClinPharm) 25 |
no | |||
Page: (ClinPharm) 25 |
no | |||
| no | ||||
| no | ||||
| yes |
Tox targets
| Target | Modality | Activity | Metabolite | Clinical evidence |
|---|---|---|---|---|
PubMed
| Title | Date | PubMed |
|---|---|---|
| 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 |
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.
| Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 15:29:49 GMT 2023
by
admin
on
Sat Dec 16 15:29:49 GMT 2023
|
| Record UNII |
P8B6SWJ0O9
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| Record Status |
Validated (UNII)
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| Record Version |
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-
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100000182795
Created by
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P8B6SWJ0O9
Created by
admin on Sat Dec 16 15:29:49 GMT 2023 , Edited by admin on Sat Dec 16 15:29:49 GMT 2023
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140674048
Created by
admin on Sat Dec 16 15:29:49 GMT 2023 , Edited by admin on Sat Dec 16 15:29:49 GMT 2023
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1613316-39-4
Created by
admin on Sat Dec 16 15:29:49 GMT 2023 , Edited by admin on Sat Dec 16 15:29:49 GMT 2023
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PARENT -> SALT/SOLVATE |
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ANHYDROUS->SOLVATE |
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ACTIVE MOIETY |
| Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
|---|---|---|---|---|---|---|
| Tmax | PHARMACOKINETIC |
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intravenous infusion |
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| Volume of Distribution | PHARMACOKINETIC |
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| Biological Half-life | PHARMACOKINETIC |
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| blood-to-plasma ratio | PHARMACOKINETIC |
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