Basic information Antitumour Activity Pharmacokinetics Safety Related Supplier
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Cabazitaxel

Basic information Antitumour Activity Pharmacokinetics Safety Related Supplier
Cabazitaxel Basic information
Cabazitaxel Chemical Properties
  • Boiling point:870.7±65.0 °C(Predicted)
  • Density 1.31
  • form White solid.
  • pka11.20±0.46(Predicted)
Safety Information
  • Safety Statements 24/25
  • HS Code 29329990
Cabazitaxel Usage And Synthesis
  • Antitumour Activity

    Cabazitaxel is a semisynthetic taxane derivative that acts as a microtubule inhibitor. It binds to tubulin, promoting the assembly of tubulin into microtubules and inhibiting their disassembly, which results in microtubule stabilization, the inhibition of cell division, cell cycle arrest and the arrest of tumour proliferation. Cabazitaxel demonstrated antitumour activity against advanced human tumours xenografted in mice. As well as being active in docetaxel-sensitive tumours, cabazitaxel showed activity in tumour models insensitive to chemotherapy, including docetaxel. Cabazitaxel also penetrates the blood-brain barrier to a greater extent than docetaxel.

  • Pharmacokinetics

    The pharmacokinetic data for cabazitaxel demonstrated dose proportionality, with a high plasma clearance and a long terminal half-life. The very large volume of distribution at steady state suggests extensive penetration into tissues. Of interest, cabazitaxel is able to cross the blood-brain barrier in preclinical models. Cabazitaxel is mainly metabolized by the cytochrome P450 (CYP) enzyme 3A4/5 and to a lesser extent by CYP2C8, suggesting that it has the potential to inhibit CYP3A enzymes.

  • DescriptionIn June 2010, the U.S. FDA approved cabazitaxel (also referred to as XRP6258 and RPR 116258A) in combination with the steroid prednisone for the treatment of metastatic Castration-Resistant Prostate Cancer (mCRPC) for patients who were previously treated with a docetaxelcontaining regimen for late-stage disease.
    Cabazitaxel is a semisynthetic analog of the natural product taxol, which is isolated from the bark of the yew tree. Cabazitaxel is a microtubule inhibitor that binds to the taxol-binding site of tubulin. Similar to other tubulin inhibitors of the taxol class, cabazitaxel inhibits microtubule disassembly resulting in mitotic blockade and cell death. Docetaxel, also a semisynthetic taxol analog, was approved by the FDA for the treatment of mCRPC in 2004. However, docetaxel is a substrate for P-gp, which is thought to contribute to the constitutive and acquired resistance of cancer cells to taxanes. Cabazitaxel has poor affinity for P-gp and showed antitumor activity in preclinical in vitro studies and in vivo tumor models that overexpress this protein. Cabazitaxel is synthesized on a commercial scale from 10-deacetylbaccatin .
  • Chemical PropertiesWhite solid
  • OriginatorSanofi-Aventis (France)
  • UsesCabazitaxel (Jevtana, XRP6258) is a semi-synthetic derivative of a natural taxoid.
  • UsesA novel semi-synthetic taxane with antitumor activity used for the treatment of castration-resistant prostate cancer. A microtubule inhibitor.
  • DefinitionChEBI: A tetracyclic diterpenoid that is 10-deacetylbaccatin III having O-methyl groups attached at positions 7 and 10 as well as an O-(2R,3S)-3-[(tert-butoxycarbonyl)amino]-2-hy roxy-3-phenylpropanoyl group attached at position 13. Acts as a microtubule inhibitor, binds tubulin and promotes microtubule assembly and simultaneously inhibits disassembly.
  • brand nameJevtana
Cabazitaxel(183133-96-2)Related Product Information
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  • Company Name:Chembest Research Laboratories Limited Gold
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