Peringatan Keamanan

The oral LD50 in rats is 500 mg/kg.L47421

Cabazitaxel

DB06772

small molecule approved

Deskripsi

Cabazitaxel is a taxoid synthesized from 10-deacetylbaccatin III, a compound isolated from the yew tree.A260621 As a second-generation semisynthetic microtubule inhibitor, cabazitaxel stabilizes microtubules and induces tumour cell death.A7056 Due to its low affinity for the P-glycoprotein (P-gp) efflux pump, cabazitaxel can more readily penetrate the blood–brain barrier compared to other taxanes like paclitaxel and docetaxel.A7056, A260421, A260621

Cabazitaxel is used to treat metastatic castration-resistant prostate cancer. It was first approved by the FDA on June 17, 2010.A260421 It was also approved by the EMA on March 17, 2011 L47381 and Health Canada on December 17, 2019.L47376

Struktur Molekul 2D

Berat 835.9324
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) Following a one-hour intravenous infusion, plasma concentrations of cabazitaxel can be described by a three-compartment pharmacokinetic model with ?-, ?-, and ?- half-lives of four minutes, two hours, and 95 hours, respectively.[L47366]
Volume Distribusi Steady-state volume of distribution (V<sub>ss</sub>) was 4,864 L (2,643 L/m<sup>2</sup> for a patient with a median BSA of 1.84 m<sup>2</sup>).[L47366]
Klirens (Clearance) Based on the population pharmacokinetic analysis, cabazitaxel has a plasma clearance of 48.5 L/h (CV 39%; 26.4 L/h/m<sup>2</sup> for a patient with a median BSA of 1.84 m<sup>2</sup>) in patients with metastatic prostate cancer.[L47366]

Absorpsi

Based on the population pharmacokinetic analysis, after an intravenous dose of cabazitaxel 25 mg/m2 every three weeks, 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 metastatic prostate cancer was 991 ng x h/mL (CV 34%). No major deviation from the dose proportionality was observed from 10 to 30 mg/m2 in patients with advanced solid tumours.L47366

Metabolisme

More than 95% of cabazitaxel is extensively metabolized in the liver. CYP3A4 and CYP3A5 are responsible for 80% to 90% of drug metabolism, while CYP2C8 is involved to a lesser extent. While cabazitaxel is the main circulating moiety in human plasma, seven metabolites have been detected in plasma, including three active metabolites arising from O-demethylation L47366 - docetaxel, RPR112698, and RPR123142.A7055 The main metabolite accounts for 5% of total cabazitaxel exposure.L47366

Rute Eliminasi

After a one-hour intravenous infusion 14C-cabazitaxel 25 mg/m2, approximately 80% of the administered dose was eliminated within two 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 the dose (2.3% as unchanged drug in urine). Around 20 metabolites of cabazitaxel are excreted into human urine and feces.L47366

Interaksi Makanan

2 Data
  • 1. Avoid grapefruit products. Grapefruit inhibits the CYP3A4 metabolism of cabazitaxel, which may increase its serum concentration.
  • 2. Avoid St. John's Wort. This herb induces the CYP3A4 metabolism of cabazitaxel and may reduce its serum concentration.

Interaksi Obat

1067 Data
Denosumab The risk or severity of adverse effects can be increased when Denosumab is combined with Cabazitaxel.
Peginterferon alfa-2a The risk or severity of adverse effects can be increased when Peginterferon alfa-2a is combined with Cabazitaxel.
Interferon alfa-n1 The risk or severity of adverse effects can be increased when Interferon alfa-n1 is combined with Cabazitaxel.
Interferon alfa-n3 The risk or severity of adverse effects can be increased when Interferon alfa-n3 is combined with Cabazitaxel.
Peginterferon alfa-2b The risk or severity of adverse effects can be increased when Peginterferon alfa-2b is combined with Cabazitaxel.
Interferon gamma-1b The risk or severity of adverse effects can be increased when Interferon gamma-1b is combined with Cabazitaxel.
Interferon alfa-2a The risk or severity of adverse effects can be increased when Interferon alfa-2a is combined with Cabazitaxel.
Gemtuzumab ozogamicin The risk or severity of adverse effects can be increased when Gemtuzumab ozogamicin is combined with Cabazitaxel.
Pegaspargase The risk or severity of adverse effects can be increased when Pegaspargase is combined with Cabazitaxel.
Interferon beta-1b The risk or severity of adverse effects can be increased when Interferon beta-1b is combined with Cabazitaxel.
Interferon alfacon-1 The risk or severity of adverse effects can be increased when Interferon alfacon-1 is combined with Cabazitaxel.
Rituximab The risk or severity of adverse effects can be increased when Rituximab is combined with Cabazitaxel.
Basiliximab The risk or severity of adverse effects can be increased when Basiliximab is combined with Cabazitaxel.
Muromonab The risk or severity of adverse effects can be increased when Muromonab is combined with Cabazitaxel.
Ibritumomab tiuxetan The risk or severity of adverse effects can be increased when Ibritumomab tiuxetan is combined with Cabazitaxel.
Tositumomab The risk or severity of adverse effects can be increased when Tositumomab is combined with Cabazitaxel.
Alemtuzumab The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Cabazitaxel.
Alefacept The risk or severity of adverse effects can be increased when Alefacept is combined with Cabazitaxel.
Efalizumab The risk or severity of adverse effects can be increased when Efalizumab is combined with Cabazitaxel.
Antithymocyte immunoglobulin (rabbit) The risk or severity of adverse effects can be increased when Antithymocyte immunoglobulin (rabbit) is combined with Cabazitaxel.
Interferon alfa-2b The risk or severity of adverse effects can be increased when Interferon alfa-2b is combined with Cabazitaxel.
Daclizumab The risk or severity of adverse effects can be increased when Daclizumab is combined with Cabazitaxel.
Phenylalanine The risk or severity of adverse effects can be increased when Phenylalanine is combined with Cabazitaxel.
Bortezomib The risk or severity of adverse effects can be increased when Bortezomib is combined with Cabazitaxel.
Cladribine Cabazitaxel may increase the immunosuppressive activities of Cladribine.
Carmustine The risk or severity of adverse effects can be increased when Carmustine is combined with Cabazitaxel.
Amsacrine The risk or severity of adverse effects can be increased when Amsacrine is combined with Cabazitaxel.
Bleomycin The risk or severity of adverse effects can be increased when Bleomycin is combined with Cabazitaxel.
Chlorambucil The risk or severity of adverse effects can be increased when Chlorambucil is combined with Cabazitaxel.
Raltitrexed The risk or severity of adverse effects can be increased when Raltitrexed is combined with Cabazitaxel.
Mitomycin The risk or severity of adverse effects can be increased when Mitomycin is combined with Cabazitaxel.
Vindesine The risk or severity of adverse effects can be increased when Vindesine is combined with Cabazitaxel.
Floxuridine The risk or severity of adverse effects can be increased when Floxuridine is combined with Cabazitaxel.
Indomethacin The risk or severity of adverse effects can be increased when Indomethacin is combined with Cabazitaxel.
Tioguanine The risk or severity of adverse effects can be increased when Tioguanine is combined with Cabazitaxel.
Vinorelbine The risk or severity of adverse effects can be increased when Vinorelbine is combined with Cabazitaxel.
Dexrazoxane The risk or severity of adverse effects can be increased when Dexrazoxane is combined with Cabazitaxel.
Streptozocin The risk or severity of adverse effects can be increased when Streptozocin is combined with Cabazitaxel.
Trifluridine The risk or severity of adverse effects can be increased when Trifluridine is combined with Cabazitaxel.
Gemcitabine The risk or severity of adverse effects can be increased when Gemcitabine is combined with Cabazitaxel.
Epirubicin The risk or severity of adverse effects can be increased when Epirubicin is combined with Cabazitaxel.
Lenalidomide The risk or severity of adverse effects can be increased when Lenalidomide is combined with Cabazitaxel.
Altretamine The risk or severity of adverse effects can be increased when Altretamine is combined with Cabazitaxel.
Cisplatin The risk or severity of adverse effects can be increased when Cisplatin is combined with Cabazitaxel.
Oxaliplatin The risk or severity of adverse effects can be increased when Oxaliplatin is combined with Cabazitaxel.
Propylthiouracil The risk or severity of adverse effects can be increased when Propylthiouracil is combined with Cabazitaxel.
Pentostatin The risk or severity of adverse effects can be increased when Pentostatin is combined with Cabazitaxel.
Methotrexate The risk or severity of adverse effects can be increased when Methotrexate is combined with Cabazitaxel.
Linezolid The risk or severity of adverse effects can be increased when Linezolid is combined with Cabazitaxel.
Clofarabine The risk or severity of adverse effects can be increased when Clofarabine is combined with Cabazitaxel.
Prednisone The risk or severity of adverse effects can be increased when Prednisone is combined with Cabazitaxel.
Pemetrexed The risk or severity of adverse effects can be increased when Pemetrexed is combined with Cabazitaxel.
Fludrocortisone The risk or severity of adverse effects can be increased when Fludrocortisone is combined with Cabazitaxel.
Sulfasalazine The risk or severity of adverse effects can be increased when Sulfasalazine is combined with Cabazitaxel.
Dacarbazine The risk or severity of adverse effects can be increased when Dacarbazine is combined with Cabazitaxel.
Temozolomide The risk or severity of adverse effects can be increased when Temozolomide is combined with Cabazitaxel.
Penicillamine The risk or severity of adverse effects can be increased when Penicillamine is combined with Cabazitaxel.
Mechlorethamine The risk or severity of adverse effects can be increased when Mechlorethamine is combined with Cabazitaxel.
Azacitidine The risk or severity of adverse effects can be increased when Azacitidine is combined with Cabazitaxel.
Carboplatin The risk or severity of adverse effects can be increased when Carboplatin is combined with Cabazitaxel.
Dactinomycin The risk or severity of adverse effects can be increased when Dactinomycin is combined with Cabazitaxel.
Cytarabine The risk or severity of adverse effects can be increased when Cytarabine is combined with Cabazitaxel.
Azathioprine The risk or severity of adverse effects can be increased when Azathioprine is combined with Cabazitaxel.
Hydroxyurea The risk or severity of adverse effects can be increased when Hydroxyurea is combined with Cabazitaxel.
Mycophenolic acid The risk or severity of adverse effects can be increased when Mycophenolic acid is combined with Cabazitaxel.
Mercaptopurine The risk or severity of adverse effects can be increased when Mercaptopurine is combined with Cabazitaxel.
Thalidomide The metabolism of Cabazitaxel can be increased when combined with Thalidomide.
Melphalan The risk or severity of adverse effects can be increased when Melphalan is combined with Cabazitaxel.
Fludarabine The risk or severity of adverse effects can be increased when Fludarabine is combined with Cabazitaxel.
Flucytosine The risk or severity of adverse effects can be increased when Flucytosine is combined with Cabazitaxel.
Capecitabine The risk or severity of adverse effects can be increased when Capecitabine is combined with Cabazitaxel.
Trilostane The risk or severity of adverse effects can be increased when Trilostane is combined with Cabazitaxel.
Procarbazine The risk or severity of adverse effects can be increased when Procarbazine is combined with Cabazitaxel.
Idarubicin The risk or severity of adverse effects can be increased when Idarubicin is combined with Cabazitaxel.
Estramustine The risk or severity of adverse effects can be increased when Estramustine is combined with Cabazitaxel.
Lomustine The risk or severity of adverse effects can be increased when Lomustine is combined with Cabazitaxel.
Eculizumab The risk or severity of adverse effects can be increased when Eculizumab is combined with Cabazitaxel.
Decitabine The risk or severity of adverse effects can be increased when Decitabine is combined with Cabazitaxel.
Nelarabine The risk or severity of adverse effects can be increased when Nelarabine is combined with Cabazitaxel.
Ciclesonide The risk or severity of adverse effects can be increased when Ciclesonide is combined with Cabazitaxel.
Stepronin The risk or severity of adverse effects can be increased when Stepronin is combined with Cabazitaxel.
Castanospermine The risk or severity of adverse effects can be increased when Castanospermine is combined with Cabazitaxel.
Vorinostat The risk or severity of adverse effects can be increased when Vorinostat is combined with Cabazitaxel.
2-Methoxyethanol The risk or severity of adverse effects can be increased when 2-Methoxyethanol is combined with Cabazitaxel.
Brequinar The risk or severity of adverse effects can be increased when Brequinar is combined with Cabazitaxel.
Thiotepa The risk or severity of adverse effects can be increased when Thiotepa is combined with Cabazitaxel.
Aldosterone The risk or severity of adverse effects can be increased when Aldosterone is combined with Cabazitaxel.
Pirfenidone The risk or severity of adverse effects can be increased when Pirfenidone is combined with Cabazitaxel.
Belinostat The risk or severity of adverse effects can be increased when Belinostat is combined with Cabazitaxel.
Trabectedin The risk or severity of adverse effects can be increased when Trabectedin is combined with Cabazitaxel.
Interferon alfa The risk or severity of adverse effects can be increased when Interferon alfa is combined with Cabazitaxel.
Glatiramer The risk or severity of adverse effects can be increased when Glatiramer is combined with Cabazitaxel.
Briakinumab The risk or severity of adverse effects can be increased when Briakinumab is combined with Cabazitaxel.
Human interferon omega-1 The risk or severity of adverse effects can be increased when Human interferon omega-1 is combined with Cabazitaxel.
Panobinostat The risk or severity of adverse effects can be increased when Panobinostat is combined with Cabazitaxel.
Mepolizumab The risk or severity of adverse effects can be increased when Mepolizumab is combined with Cabazitaxel.
Abetimus The risk or severity of adverse effects can be increased when Abetimus is combined with Cabazitaxel.
Belatacept The risk or severity of adverse effects can be increased when Belatacept is combined with Cabazitaxel.
Bendamustine The risk or severity of adverse effects can be increased when Bendamustine is combined with Cabazitaxel.
Pralatrexate The risk or severity of adverse effects can be increased when Cabazitaxel is combined with Pralatrexate.

Target Protein

Tubulin beta-1 chain TUBB1

Referensi & Sumber

Synthesis reference: Nagesh Palepu, "CABAZITAXEL FORMULATIONS AND METHODS OF PREPARING THEREOF." U.S. Patent US20120065255, issued March 15, 2012.
Artikel (PubMed)
  • PMID: 23542607
    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.
  • PMID: 23091336
    Nightingale G, Ryu J: Cabazitaxel (jevtana): a novel agent for metastatic castration-resistant prostate cancer. P T. 2012 Aug;37(8):440-8.
  • PMID: 21448449
    Paller CJ, Antonarakis ES: Cabazitaxel: a novel second-line treatment for metastatic castration-resistant prostate cancer. Drug Des Devel Ther. 2011 Mar 10;5:117-24. doi: 10.2147/DDDT.S13029.
  • PMID: 21770474
    Villanueva C, Bazan F, Kim S, Demarchi M, Chaigneau L, Thiery-Vuillemin A, Nguyen T, Cals L, Dobi E, Pivot X: Cabazitaxel: a novel microtubule inhibitor. Drugs. 2011 Jul 9;71(10):1251-8. doi: 10.2165/11591390-000000000-00000.

Contoh Produk & Brand

Produk: 9 • International brands: 0
Produk
  • Cabazitaxel
    Injection, solution, concentrate; Kit • 60 mg/1.5mL • Intravenous • US • Generic • Approved
  • Cabazitaxel Accord
    Injection, solution, concentrate • 20 mg/ml • Intravenous • EU • Approved
  • Cabazitaxel for Injection
    Solution • 45 mg / 4.5 mL • Intravenous • Canada • Approved
  • Cabazitaxel for Injection
    Solution • 60 mg / 6 mL • Intravenous • Canada • Approved
  • Cabazitaxel for Injection
    Solution • 40 mg / mL • Intravenous • Canada • Approved
  • Cabazitaxel for Injection
    Kit; Solution • 40 mg / mL • Intravenous • Canada • Approved
  • Jevtana
    Injection, solution, concentrate; Kit • 60 mg/1.5mL • Intravenous • US • Approved
  • Jevtana
    Solution • 40 mg / mL • Intravenous • Canada • Approved
Menampilkan 8 dari 9 produk.

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