Targeting 12-Lipoxygenase as a Potential Novel Antiplatelet Therapy

Trends Pharmacol Sci. 2017 Nov;38(11):1006-1015. doi: 10.1016/ Epub 2017 Aug 29.


Platelets are key contributors to the formation of occlusive thrombi; the major underlying cause of ischemic heart disease and stroke. Antiplatelet therapy has reduced the morbidity and mortality associated with thrombotic events; however, the utility of current antiplatelet therapies is limited by the concomitant risk of an adverse bleeding event. Novel antiplatelet therapies that are more efficacious at inhibiting thrombosis while minimally affecting hemostasis are required. Platelet-type 12-(S)-lipoxygenase (12-LOX), an oxygenase shown to potentiate platelet activation, represents a novel antiplatelet target. Recently, a selective 12-LOX inhibitor, ML355, was shown to decrease thrombosis without prolonging hemostasis. While published data suggests targeting 12-LOX is a viable approach, further work is required to determine the safety and effectiveness of 12-LOX inhibitors in humans.

Keywords: 12-lipoxygenase; antiplatelet; cardiovascular; eicosanoid; oxygenase.

Publication types

  • Review

MeSH terms

  • Animals
  • Arachidonate 12-Lipoxygenase / blood*
  • Blood Platelets / drug effects
  • Blood Platelets / enzymology
  • Humans
  • Lipoxygenase Inhibitors / pharmacology*
  • Molecular Targeted Therapy
  • Platelet Aggregation Inhibitors / pharmacology*


  • Lipoxygenase Inhibitors
  • Platelet Aggregation Inhibitors
  • Arachidonate 12-Lipoxygenase