Polypharmacology of Approved Anticancer Drugs

Ivano Amelio1, Andrey Lisitsa2, Richard A Knight1

  • 1Medical Research Council Toxicology Unit, Leicester LE1 9HN, United Kingdom.

Current Drug Targets
|March 2, 2016
PubMed

Insights

Most cancer drugs target multiple proteins, not just one. This polypharmacology, or targeting multiple mechanisms, is key to achieving clinical efficacy in oncology treatments.

Area of Science:

  • Oncology
  • Pharmacology
  • Drug Discovery

Background:

  • Current oncology drug discovery focuses on highly selective molecules targeting single or few related drug targets.
  • However, data suggests approved anticancer agents interact with numerous proteins, indicating broader mechanisms of action.

Purpose of the Study:

  • To review and systematize information on the targets of anticancer drugs.
  • To revise the potential mechanisms of action for these agents.
  • To explore the role of polypharmacology in cancer treatment.

Main Methods:

  • Literature review of existing bioassay data.
  • Systematization of information on anticancer drug targets.
  • Analysis of drug mechanisms of action.

Main Results:

  • Approved anticancer agents exhibit polypharmacology, targeting multiple proteins with diverse functions.
  • The efficacy of current antineoplastic agents is linked to the modulation of multiple cellular mechanisms.

Conclusions:

  • Anticancer drug efficacy is achieved through the modulation of multiple cellular pathways, not just single targets.
  • Understanding polypharmacology is crucial for future oncology drug development.

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