Drug Details
| General Information of the Drug (ID: DR1078) | ||||
|---|---|---|---|---|
| Name |
Cabazitaxel
|
|||
| Synonyms |
Jevtana; Taxoid XRP6258; Jevtana (TN)
Click to Show/Hide
|
|||
| Molecular Type |
Small molecule
|
|||
| Disease | Breast cancer [ICD-11: 2C60] | Approved | [1] | |
| Structure |
|
Click to Download Mol2D MOL |
||
| ADMET Property |
Clearance
The drug present in the plasma can be removed from the body at the rate of 11 mL/min/kg
Half-life
The concentration or amount of drug in body reduced by one-half in 4 minutes (alpha), 2 hours (beta), and 95 hours (gamma)
Metabolism
The drug is metabolized via the liver
Unbound Fraction
The unbound fraction of drug in plasma is 0.24%
Vd
The volume of distribution (Vd) of drug is 4,864 L
Click to Show/Hide
|
|||
| Click to Show/Hide the Molecular Information and External Link(s) of This Natural Product | ||||
| Formula |
C45H57NO14
|
|||
| PubChem CID | ||||
| Canonical SMILES |
CC1=C2C(C(=O)C3(C(CC4C(C3C(C(C2(C)C)(CC1OC(=O)C(C(C5=CC=CC=C5)NC(=O)OC(C)(C)C)O)O)OC(=O)C6=CC=CC=C6)(CO4)OC(=O)C)OC)C)OC
|
|||
| 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
|
|||
| InChIKey |
BMQGVNUXMIRLCK-OAGWZNDDSA-N
|
|||
| CAS Number |
CAS 183133-96-2
|
|||
| TTD Drug ID | ||||
| DrugBank ID | ||||
| Combinatorial Therapeutic Effect(s) Validated Clinically or Experimentally | ||||||
|---|---|---|---|---|---|---|
| α. A List of Natural Product(s) Able to Enhance the Efficacy of This Drug | ||||||
| Fisetin | Toxicodendron succedaneum | Click to Show/Hide the Molecular Data of This NP | ||||
| Achieving Therapeutic Synergy | Click to Show/Hide | |||||
| Representative Experiment Reporting the Effect of This Combination | [2] | |||||
| Detail(s) |
Combination Info
click to show the detail info of this combination
|
|||||
| Molecule(s)
Regulation |
Down-regulation | Expression | ABCB1 | Molecule Info |
Pathway MAP
|
|
| Up-regulation | Expression | BAX | Molecule Info |
Pathway MAP
|
||
| Up-regulation | Expression | MCL1 | Molecule Info |
Pathway MAP
|
||
| Down-regulation | Expression | MKI67 | Molecule Info | |||
| Down-regulation | Expression | MMP-2 | Molecule Info |
Pathway MAP
|
||
| Down-regulation | Expression | MMP-9 | Molecule Info |
Pathway MAP
|
||
| Up-regulation | Expression | PARP1 | Molecule Info |
Pathway MAP
|
||
| Down-regulation | Expression | PCNA | Molecule Info |
Pathway MAP
|
||
| Down-regulation | Expression | PECAM1 | Molecule Info |
Pathway MAP
|
||
| Down-regulation | Expression | PRAP1 | Molecule Info |
Pathway MAP
|
||
| In-vitro Model | LNCaP C4-2 | CVCL_4782 | Prostate carcinoma | Homo sapiens | ||
| A-549 | CVCL_0023 | Lung adenocarcinoma | Homo sapiens | |||
| PrEC | Prostate cancer | Homo sapiens | ||||
| 22Rv1 | Prostate cancer | Homo sapiens | ||||
| In-vivo Model | A total of 24 athymic nude male mice 6-8 weeks old were injected subcutaneously with 1*106 22Rv1 cells. | |||||
| Experimental
Result(s) |
Fisetin Enhances Chemotherapeutic Effect of Cabazitaxel against Human Prostate Cancer Cells. | |||||
| Genistein | Glycine max | Click to Show/Hide the Molecular Data of This NP | ||||
| Augmenting Drug Sensitivity | Click to Show/Hide | |||||
| Representative Experiment Reporting the Effect of This Combination | [3] | |||||
| Detail(s) |
Combination Info
click to show the detail info of this combination
|
|||||
| Molecule(s)
Regulation |
Up-regulation | Expression | BAX | Molecule Info |
Pathway MAP
|
|
| Up-regulation | Cleavage | CASP3 | Molecule Info |
Pathway MAP
|
||
| Up-regulation | Cleavage | PARP1 | Molecule Info |
Pathway MAP
|
||
| In-vitro Model | LNCaP C4-2 | CVCL_4782 | Prostate carcinoma | Homo sapiens | ||
| PC-3 | CVCL_0035 | Prostate carcinoma | Homo sapiens | |||
| ARCaPM | Prostate cancer | Homo sapiens | ||||
| In-vivo Model | PC3-luc cells (2*106) per 100L per site were injected subcutaneously in athymic nude mice (BALB/c, 6-week-old). | |||||
| Experimental
Result(s) |
Genistein increases the expression of pro-apoptotic protein Bax, activates apoptotic signals, and enhances the response to cabazitaxel treatment in mCRPC cells. | |||||
| Target and Pathway | ||||
|---|---|---|---|---|
| Target(s) | Tubulin (TUB) | Molecule Info | [4] | |