Description

Simple

An anticancer medication used to treat prostate cancer that developed resistance to other cancer therapies.

Clinical

An antineoplastic agent used for the treatment of hormone-refractory metastatic prostate cancer previously treated with a docetaxel-containing treatment regimen.

Overview

Cabazitaxel is an anti-neoplastic used with the steroid medicine prednisone. Cabazitaxel is used to treat people with prostate cancer that has progressed despite treatment with docetaxel. Cabazitaxel is prepared by semi-synthesis with a precursor extracted from yew needles (10-deacetylbaccatin III). It was approved by the U.S. Food and Drug Administration (FDA) on June 17, 2010.

Pharmacology

Indication

For treatment of patients with hormone-refractory metastatic prostate cancer previously treated with a docetaxel-containing treatment regimen.

Pharmacodynamic

Cabaitaxel has anti-tumour properties and is effective against docetaxel-sensitive and -insensitive tumours.

Mechanism of action

Cabazitaxel is a microtubule inhibitor. Cabazitaxel binds to tubulin and promotes its assembly into microtubules while simultaneously inhibiting disassembly. This leads to the stabilization of microtubules, which results in the interference of mitotic and interphase cellular functions. The cell is t... Read more

Absorption

After an intravenous dose of cabazitaxel 25 mg/m2 every three weeks to a population of 170 patients with solid tumors, the mean Cmax in patients with metastatic prostate cancer was 226 ng/mL (CV 107%) and was reached at the end of the one-hour infusion (Tmax). The mean AUC in patients with metastati... Read more

Protein binding

Cabazitaxel is mainly bound to human serum albumin (82%) and lipoproteins (88% for HDL, 70% for LDL, and 56% for VLDL).

Volume of distribution

The volume of distribution (Vss) was 4,864 L (2,643 L/m2 for a patient with a median BSA of 1.84 m2) at steady state. Compared to other taxanes, penetrates the CNS to a greater extent.

Clearance

Cabazitaxel has a plasma clearance of 48.5 L/h (CV 39%; 26.4 L/h/m2 for a patient with a median BSA of 1.84 m2) in patients with metastatic prostate cancer.

Half life

Following a one-hour intravenous infusion, plasma concentrations of cabazitaxel can be described by a three-compartment pharmacokinetic model with α-, β-, and γ- half-lives of 4 minutes, 2 hours, and 95 hours, respectively.

Route of elimination

After a one-hour intravenous infusion [14C]-cabazitaxel 25 mg/m2, approximately 80% of the administered dose was eliminated within 2 weeks. Cabazitaxel is mainly excreted in the feces as numerous metabolites (76% of the dose); while renal excretion of cabazitaxel and metabolites account for 3.7% of... Read more

Toxicity

Cabazitaxel may cause serious side effects including neutropenia, hypersensitivity reactions, gastrointestinal symptoms, and renal failure. Anticipated complications of overdose include exacerbation of adverse reactions such as bone marrow suppression and gastrointestinal disorders. Cabazitaxel pene... Read more

Adverse Effects

Contraindications

  • Regions: US
  • Patient Conditions:
      • Name: Pregnancy
      • Drugbank Id: DBCOND0018394
  • Hypersensitivity:
    • polysorbate 80
  • Regions: US
  • Lab Values:
    • neutrophil counts of ≤1,500/mm^3
  • Regions: US
  • Lab Values:
    • total bilirubin >3 × ULN
  • Regions: US
  • Patient Conditions:
      • Name: Severe Hepatic Impairment
      • Drugbank Id: DBCOND0070791
      • Modification Of:
        • Base:
          • Name: Heptic Impairment
          • Drugbank Id: DBCOND0072269
        • Severity:
          • Includes:
            • severe

Food Interactions

    Information currently not available.

Interactions

Type in a drug name to check for interaction with Cabazitaxel
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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
(R)-warfarin
The metabolism of (R)-warfarin can be decreased when combined with Cabazitaxel.
(S)-Warfarin
The metabolism of (S)-Warfarin can be decreased when combined with Cabazitaxel.
2-Methoxyethanol
The risk or severity of adverse effects can be increased when 2-Methoxyethanol is combined with Cabazitaxel.
4-hydroxycoumarin
The risk or severity of bleeding can be increased when 4-hydroxycoumarin is combined with Cabazitaxel.
9-(N-methyl-L-isoleucine)-cyclosporin A
The risk or severity of adverse effects can be increased when Cabazitaxel is combined with 9-(N-methyl-L-isoleucine)-cyclosporin A.
Abatacept
The metabolism of Cabazitaxel can be increased when combined with Abatacept.
Abciximab
The risk or severity of bleeding can be increased when Abciximab is combined with Cabazitaxel.
Abemaciclib
Cabazitaxel may decrease the excretion rate of Abemaciclib which could result in a higher serum level.
Abetimus
The risk or severity of adverse effects can be increased when Abetimus is combined with Cabazitaxel.
Abiraterone
The metabolism of Cabazitaxel can be decreased when combined with Abiraterone.
Acalabrutinib
The metabolism of Cabazitaxel can be decreased when combined with Acalabrutinib.
Acenocoumarol
The risk or severity of bleeding can be increased when Acenocoumarol is combined with Cabazitaxel.
Acetyldigitoxin
Acetyldigitoxin may decrease the cardiotoxic activities of Cabazitaxel.
Acteoside
The risk or severity of adverse effects can be increased when Cabazitaxel is combined with Acteoside.
Adalimumab
The metabolism of Cabazitaxel can be increased when combined with Adalimumab.
Adenovirus type 7 vaccine live
The risk or severity of infection can be increased when Adenovirus type 7 vaccine live is combined with Cabazitaxel.
Afatinib
Cabazitaxel may decrease the excretion rate of Afatinib which could result in a higher serum level.
Afelimomab
The metabolism of Cabazitaxel can be increased when combined with Afelimomab.
Aldesleukin
The risk or severity of adverse effects can be increased when Aldesleukin is combined with Cabazitaxel.
Aldosterone
The risk or severity of adverse effects can be increased when Aldosterone is combined with Cabazitaxel.
3 References
  1. 1 . Galsky MD, Dritselis A, Kirkpatrick P, Oh WK: Cabazitaxel. Nat Rev Drug Discov. 2010 Sep;9(9):677-8. doi: 10.1038/nrd3254.PubMed: 20811375
  2. 2 . Kort A, Hillebrand MJ, Cirkel GA, Voest EE, Schinkel AH, Rosing H, Schellens JH, Beijnen JH: 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. J Chromatogr B Analyt Technol Biomed Life Sci. 2013 Apr 15;925:117-23. doi: 10.1016/j.jchromb.2013.02.034. Epub 2013 Mar 5.PubMed: 23542607
  3. 3 . Nightingale G, Ryu J: Cabazitaxel (jevtana): a novel agent for metastatic castration-resistant prostate cancer. P T. 2012 Aug;37(8):440-8.PubMed: 23091336