Polypharmacology: drug discovery for the future

Expert Rev Clin Pharmacol. 2013 Jan;6(1):41-7. doi: 10.1586/ecp.12.74.


In recent years, even with remarkable scientific advancements and a significant increase of global research and development spending, drugs are frequently withdrawn from markets. This is primarily due to their side effects or toxicities. Drug molecules often interact with multiple targets, coined as polypharmacology, and the unintended drug-target interactions could cause side effects. Polypharmacology remains one of the major challenges in drug development, and it opens novel avenues to rationally design the next generation of more effective, but less toxic, therapeutic agents. This review outlines the latest progress and challenges in polypharmacology studies.

Publication types

  • Research Support, N.I.H., Extramural
  • Review

MeSH terms

  • Computational Biology
  • Databases, Pharmaceutical*
  • Drug Discovery / methods*
  • Drug Discovery / standards
  • Drug Interactions*
  • Drug-Related Side Effects and Adverse Reactions*
  • Humans
  • Models, Biological
  • Polypharmacy*