Taxanes

Summary

The taxane drug class includes the drugs docetaxel and paclitaxel.

Taxanes work as microtubule inhibitors. They hyperstabilize polymerized microtubules and prevent the normal breakdown of the mitotic spindle. This leads to mitotic arrest and cell death. Notably, their action is specific to the M-phase of the cell cycle.

Clinically, taxanes are used to treat various cancers, including ovarian, breast, and lung cancers.

Key side effects to remember include hypersensitivity reactions and peripheral neuropathy.

Key Points

• Taxanes
  • Drug Names
    • Docetaxel
    • Paclitaxel
  • Mechanism
    • Microtubule inhibitor
      • Hyperstabilize polymerized microtubules
        • Normal microtubules exhibit dynamic instability, with a plus end that lengthens by the addition of tubulin dimers and a minus end that shortens by the removal of tubulin dimers, resulting in a process known as 'treadmilling'
        • Hyperstabilization of microtubules prevents their shortening, leading to the impairment of cellular functions
      • Prevent mitotic spindle breakdown
        • The mitotic spindle is predominantly composed of microtubules. The inability to disassemble the mitotic spindle due to the action of taxanes after anaphase leads to mitotic arrest
      • Acts on M-phase of cell cycle
  • Clinical Use
    • Treat various tumors
      • e.g. ovarian and breast carcinomas
  • Side Effects
    • Myelosuppression
    • Neuropathy
      • Neurons rely on microtubule-based transport along their long axons; impairment of normal microtubule function disproportionately affects neuronal function
    • Hypersensitivity