Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C45H57NO14 |
Molecular Weight | 835.9324 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 11 / 11 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CO[C@H]1C[C@H]2OC[C@@]2(OC(C)=O)[C@H]3[C@H](OC(=O)C4=CC=CC=C4)[C@]5(O)C[C@H](OC(=O)[C@H](O)[C@@H](NC(=O)OC(C)(C)C)C6=CC=CC=C6)C(C)=C([C@@H](OC)C(=O)[C@]13C)C5(C)C
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
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 |
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
Sources: https://www.ncbi.nlm.nih.gov/pubmed/26723976
Curator's Comment: Known to be CNS active in rats. Human data not available.
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 |
---|---|---|---|---|
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: |
|
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: |
|
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 |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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: |
|
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: |
|
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 |
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) Health Status: unhealthy Age Group: 11.0 years (range: 5–17 years) Sex: M+F 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) Health Status: unhealthy Age Group: 49 years (range: 34–67) Sex: M+F 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) Health Status: unhealthy Age Group: 54.0 years (range: 37–70 years) Sex: M+F 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) Health Status: unhealthy Age Group: 54.0 years (range: 48–60 years) Sex: F 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) Health Status: unhealthy Age Group: 56.0 years (range: 52–67 years) Sex: M+F 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) Health Status: unhealthy Age Group: 59.0 years (range: 18–75 years) Sex: M+F 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) Health Status: unhealthy Age Group: 63 years (range: 55–67 years) Sex: M 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 Sources: |
unhealthy, 68 years (range: 46-92 years) Health Status: unhealthy Age Group: 68 years (range: 46-92 years) Sex: M 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 Sources: |
unhealthy, 68 years (range: 46-92 years) Health Status: unhealthy Age Group: 68 years (range: 46-92 years) Sex: M Sources: |
Disc. AE: Cellulitis, Pneumonia... AEs leading to discontinuation/dose reduction: Cellulitis (6 patients) Sources: Pneumonia (6 patients) Salmonellosis (6 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 Sources: |
unhealthy, 68 years (range: 46-92 years) Health Status: unhealthy Age Group: 68 years (range: 46-92 years) Sex: M Sources: |
Disc. AE: Campylobacter infection, Urinary tract infection fungal... AEs leading to discontinuation/dose reduction: Campylobacter infection (6 patients) Sources: 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) |
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) Health Status: unhealthy Age Group: 7.0 years (range: 6–18 years) Sex: M+F 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) Health Status: unhealthy Age Group: 9.5 years (range: 3–16 years) Sex: M+F Sources: |
Disc. AE: Anaphylactic reaction, Transaminases increased... Other AEs: Diarrhea, Dysphagia... AEs leading to discontinuation/dose reduction: Anaphylactic reaction (serious, 3 patients) Other AEs:Transaminases increased (grade 2, 1 patient) Diarrhea (43.8%) Sources: Dysphagia (37.5%) Nausea (31.3%) Vomiting (25%) Headache (25%) |
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 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) Health Status: unhealthy Age Group: 11.0 years (range: 5–17 years) Sex: M+F 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) Health Status: unhealthy Age Group: 49 years (range: 34–67) Sex: M+F 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) Health Status: unhealthy Age Group: 49 years (range: 34–67) Sex: M+F 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) Health Status: unhealthy Age Group: 54.0 years (range: 37–70 years) Sex: M+F 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) Health Status: unhealthy Age Group: 54.0 years (range: 37–70 years) Sex: M+F 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) Health Status: unhealthy Age Group: 54.0 years (range: 37–70 years) Sex: M+F 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) Health Status: unhealthy Age Group: 54.0 years (range: 48–60 years) Sex: F 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) Health Status: unhealthy Age Group: 54.0 years (range: 48–60 years) Sex: F 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) Health Status: unhealthy Age Group: 54.0 years (range: 48–60 years) Sex: F 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) Health Status: unhealthy Age Group: 56.0 years (range: 52–67 years) Sex: M+F 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) Health Status: unhealthy Age Group: 56.0 years (range: 52–67 years) Sex: M+F 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) Health Status: unhealthy Age Group: 56.0 years (range: 52–67 years) Sex: M+F 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) Health Status: unhealthy Age Group: 56.0 years (range: 52–67 years) Sex: M+F 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) Health Status: unhealthy Age Group: 56.0 years (range: 52–67 years) Sex: M+F 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) Health Status: unhealthy Age Group: 56.0 years (range: 52–67 years) Sex: M+F 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) Health Status: unhealthy Age Group: 56.0 years (range: 52–67 years) Sex: M+F 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) Health Status: unhealthy Age Group: 59.0 years (range: 18–75 years) Sex: M+F 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) Health Status: unhealthy Age Group: 59.0 years (range: 18–75 years) Sex: M+F 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) Health Status: unhealthy Age Group: 59.0 years (range: 18–75 years) Sex: M+F 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) Health Status: unhealthy Age Group: 59.0 years (range: 18–75 years) Sex: M+F 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) Health Status: unhealthy Age Group: 59.0 years (range: 18–75 years) Sex: M+F 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) Health Status: unhealthy Age Group: 59.0 years (range: 18–75 years) Sex: M+F 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) Health Status: unhealthy Age Group: 59.0 years (range: 18–75 years) Sex: M+F 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) Health Status: unhealthy Age Group: 59.0 years (range: 18–75 years) Sex: M+F 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) Health Status: unhealthy Age Group: 59.0 years (range: 18–75 years) Sex: M+F 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) Health Status: unhealthy Age Group: 63 years (range: 55–67 years) Sex: M 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) Health Status: unhealthy Age Group: 63 years (range: 55–67 years) Sex: M 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) Health Status: unhealthy Age Group: 63 years (range: 55–67 years) Sex: M 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) Health Status: unhealthy Age Group: 63 years (range: 55–67 years) Sex: M 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) Health Status: unhealthy Age Group: 63 years (range: 55–67 years) Sex: M 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) Health Status: unhealthy Age Group: 63 years (range: 55–67 years) Sex: M 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 Sources: |
unhealthy, 68 years (range: 46-92 years) Health Status: unhealthy Age Group: 68 years (range: 46-92 years) Sex: M 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 Sources: |
unhealthy, 68 years (range: 46-92 years) Health Status: unhealthy Age Group: 68 years (range: 46-92 years) Sex: M Sources: |
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 Sources: |
unhealthy, 68 years (range: 46-92 years) Health Status: unhealthy Age Group: 68 years (range: 46-92 years) Sex: M Sources: |
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 Sources: |
unhealthy, 68 years (range: 46-92 years) Health Status: unhealthy Age Group: 68 years (range: 46-92 years) Sex: M Sources: |
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 Sources: |
unhealthy, 68 years (range: 46-92 years) Health Status: unhealthy Age Group: 68 years (range: 46-92 years) Sex: M 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 Sources: |
unhealthy, 68 years (range: 46-92 years) Health Status: unhealthy Age Group: 68 years (range: 46-92 years) Sex: M Sources: |
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 Sources: |
unhealthy, 68 years (range: 46-92 years) Health Status: unhealthy Age Group: 68 years (range: 46-92 years) Sex: M Sources: |
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 Sources: |
unhealthy, 68 years (range: 46-92 years) Health Status: unhealthy Age Group: 68 years (range: 46-92 years) Sex: M Sources: |
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 Sources: |
unhealthy, 68 years (range: 46-92 years) Health Status: unhealthy Age Group: 68 years (range: 46-92 years) Sex: M Sources: |
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 Sources: |
unhealthy, 68 years (range: 46-92 years) Health Status: unhealthy Age Group: 68 years (range: 46-92 years) Sex: M Sources: |
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 Sources: |
unhealthy, 68 years (range: 46-92 years) Health Status: unhealthy Age Group: 68 years (range: 46-92 years) Sex: M Sources: |
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 Sources: |
unhealthy, 68 years (range: 46-92 years) Health Status: unhealthy Age Group: 68 years (range: 46-92 years) Sex: M Sources: |
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 Sources: |
unhealthy, 68 years (range: 46-92 years) Health Status: unhealthy Age Group: 68 years (range: 46-92 years) Sex: M Sources: |
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 Sources: |
unhealthy, 68 years (range: 46-92 years) Health Status: unhealthy Age Group: 68 years (range: 46-92 years) Sex: M Sources: |
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 Sources: |
unhealthy, 68 years (range: 46-92 years) Health Status: unhealthy Age Group: 68 years (range: 46-92 years) Sex: M Sources: |
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 Sources: |
unhealthy, 68 years (range: 46-92 years) Health Status: unhealthy Age Group: 68 years (range: 46-92 years) Sex: M Sources: |
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 Sources: |
unhealthy, 68 years (range: 46-92 years) Health Status: unhealthy Age Group: 68 years (range: 46-92 years) Sex: M Sources: |
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 Sources: |
unhealthy, 68 years (range: 46-92 years) Health Status: unhealthy Age Group: 68 years (range: 46-92 years) Sex: M Sources: |
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 Sources: |
unhealthy, 68 years (range: 46-92 years) Health Status: unhealthy Age Group: 68 years (range: 46-92 years) Sex: M Sources: |
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 Sources: |
unhealthy, 68 years (range: 46-92 years) Health Status: unhealthy Age Group: 68 years (range: 46-92 years) Sex: M Sources: |
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) Health Status: unhealthy Age Group: 7.0 years (range: 6–18 years) Sex: M+F 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) Health Status: unhealthy Age Group: 9.5 years (range: 3–16 years) Sex: M+F 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) Health Status: unhealthy Age Group: 9.5 years (range: 3–16 years) Sex: M+F 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) Health Status: unhealthy Age Group: 9.5 years (range: 3–16 years) Sex: M+F 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) Health Status: unhealthy Age Group: 9.5 years (range: 3–16 years) Sex: M+F 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) Health Status: unhealthy Age Group: 9.5 years (range: 3–16 years) Sex: M+F 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) Health Status: unhealthy Age Group: 9.5 years (range: 3–16 years) Sex: M+F 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) Health Status: unhealthy Age Group: 9.5 years (range: 3–16 years) Sex: M+F 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 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 Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Drug as perpetrator
Drug as victim
Tox targets
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Page: 49.0 |
PubMed
Title | Date | PubMed |
---|---|---|
Cabazitaxel. | 2010 Sep |
|
Cabazitaxel (jevtana): a novel agent for metastatic castration-resistant prostate cancer. | 2012 Aug |
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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
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/26154614
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
Mon Mar 31 18:36:14 GMT 2025
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Mon Mar 31 18:36:14 GMT 2025
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Record UNII |
51F690397J
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Validated (UNII)
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NDF-RT |
N0000175085
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NDF-RT |
N0000175592
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NCI_THESAURUS |
C67437
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WHO-ATC |
L01CD04
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EMA ASSESSMENT REPORTS |
JETVANA (AUTHORIZED: PROSTATIC, NEOPLASMS)
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NCI_THESAURUS |
C1490
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LIVERTOX |
NBK548533
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WHO-VATC |
QL01CD04
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100000115694
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996051
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CABAZITAXEL
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m2874
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CHEMBL1201748
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SUB31282
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63584
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51F690397J
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8967
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Related Record | Type | Details | ||
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EXCRETED UNCHANGED |
URINE
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TRANSPORTER -> SUBSTRATE |
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METABOLIC ENZYME -> SUBSTRATE |
As cabazitaxel is mainly metabolized by CYP3A in vitro, strong CYP3A inducers or inhibitors are expected to affect the pharmacokinetics of cabazitaxel.
MAJOR
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SOLVATE->ANHYDROUS |
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SALT/SOLVATE -> PARENT |
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METABOLIC ENZYME -> SUBSTRATE |
MINOR
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SALT/SOLVATE -> PARENT |
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METABOLIC ENZYME -> SUBSTRATE |
As cabazitaxel is mainly metabolized by CYP3A in vitro, strong CYP3A inducers or inhibitors are expected to affect the pharmacokinetics of cabazitaxel.
MAJOR
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BINDER->LIGAND |
BINDING
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SOLVATE->ANHYDROUS |
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EXCRETED UNCHANGED |
FECAL
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Related Record | Type | Details | ||
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METABOLITE ACTIVE -> PARENT |
by the CYP3A4/5 isoenzyme
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METABOLITE ACTIVE -> PARENT |
by the CYP3A4/5 isoenzyme
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METABOLITE -> PARENT |
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METABOLITE ACTIVE -> PARENT |
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Related Record | Type | Details | ||
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ACTIVE MOIETY |
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Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
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Volume of Distribution | PHARMACOKINETIC |
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Biological Half-life | PHARMACOKINETIC |
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Tmax | PHARMACOKINETIC |
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intravenous infusion |
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blood-to-plasma ratio | PHARMACOKINETIC |
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