Current progress and future perspectives of polypharmacology : From the view of non-small cell lung cancer

Semin Cancer Biol. 2021 Jan;68:84-91. doi: 10.1016/j.semcancer.2019.10.019. Epub 2019 Nov 4.


A pre-eminent subtype of lung carcinoma, Non-small cell lung cancer accounts for paramount causes of cancer-associated mortality worldwide. Undeterred by the endeavour in the treatment strategies, the overall cure and survival rates for NSCLC remain substandard, particularly in metastatic diseases. Moreover, the emergence of resistance to classic anticancer drugs further deteriorates the situation. These demanding circumstances culminate the need of extended and revamped research for the establishment of upcoming generation cancer therapeutics. Drug repositioning introduces an affordable and efficient strategy to discover novel drug action, especially when integrated with recent systems biology driven stratagem. This review illustrates the trendsetting approaches in repurposing along with their numerous success stories with an emphasize on the NSCLC therapeutics. Indeed, these novel hits, in combination with conventional anticancer agents, will ideally make their way the clinics and strengthen the therapeutic arsenal to combat drug resistance in the near future.

Keywords: Drug Discovery; Drug repurposing; Drug resistance; Lung cancer; Repositioned hits.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.
  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents / therapeutic use*
  • Carcinoma, Non-Small-Cell Lung / drug therapy*
  • Drug Discovery*
  • Drug Repositioning / methods*
  • Humans
  • Lung Neoplasms / drug therapy*
  • Polypharmacology / methods*


  • Antineoplastic Agents