Unravelling exemestane: From biology to clinical prospects

J Steroid Biochem Mol Biol. 2016 Oct:163:1-11. doi: 10.1016/j.jsbmb.2016.03.019. Epub 2016 Mar 15.

Abstract

Aromatase inhibitors (AIs) are anti-tumor agents used in clinic to treat hormone-dependent breast cancer. AIs block estrogens biosynthesis by inhibiting the enzyme aromatase, preventing tumor progression. Exemestane, a third-generation steroidal AI, belongs to this class of drugs and is currently used in clinic to treat postmenopausal women, due to its high efficacy and good tolerability. Here, its pharmacological and biological aspects as well as its clinical applications and comparison to other endocrine therapeutic agents, are reviewed. It is also focused the benefits and risks of exemestane, drawbacks to be overcome and aspects to be explored.

Keywords: Aromatase inhibitors; Clinical trials; Endocrine resistance; Endocrine therapy; Exemestane; Hormone-dependent breast cancer.

Publication types

  • Review

MeSH terms

  • Anastrozole
  • Androstadienes / metabolism
  • Androstadienes / therapeutic use*
  • Antineoplastic Agents / therapeutic use*
  • Apoptosis / drug effects
  • Aromatase Inhibitors / therapeutic use*
  • Autophagy / drug effects
  • Biotransformation
  • Breast Neoplasms / drug therapy*
  • Breast Neoplasms / metabolism
  • Breast Neoplasms / pathology
  • Cell Cycle Checkpoints / drug effects
  • Cell Line, Tumor
  • Clinical Trials as Topic
  • Drug Resistance, Neoplasm
  • Female
  • Humans
  • Nitriles / therapeutic use
  • Tamoxifen / therapeutic use
  • Triazoles / therapeutic use

Substances

  • Androstadienes
  • Antineoplastic Agents
  • Aromatase Inhibitors
  • Nitriles
  • Triazoles
  • Tamoxifen
  • Anastrozole
  • exemestane
  • 17-dihydroexemestane