Darapladib Explained

Darapladib is an inhibitor of lipoprotein-associated phospholipase A2 (Lp-PLA2) that is in development as a drug for treatment of atherosclerosis.[1]

It was discovered by Human Genome Sciences in collaboration with GlaxoSmithKline (GSK).[2]

In November 2013, GSK announced that the drug had failed to meet Phase III endpoints in a trial of 16,000 patients with acute coronary syndrome (ACS).[3] An additional trial of 13,000 patients (SOLID-TIMI 52) finished in May 2014. The study failed to reduce the risk of coronary heart disease death, myocardial infarction, and urgent coronary revascularization compared with placebo in acute coronary syndrome patients treated with standard medical care.[4]

In 2022, Darapladib has been found to inhibit intraerythrocytic development of the malaria parasite Plasmodium falciparum by inhibition of the human host enzyme peroxiredoxin 6.[5] The authors present data that the original target of Darapladib, Lp-PLA2, is absent in the host red blood cell.

Notes and References

  1. Thompson PL, Nidorf SM, Eikelboom J . Targeting the unstable plaque in acute coronary syndromes . Clinical Therapeutics . 35 . 8 . 1099–107 . August 2013 . 23973042 . 10.1016/j.clinthera.2013.07.332 .
  2. Web site: Reuters . 12 April 2007 . Spotlight on Glaxo Heart Drug as Others Fail . .
  3. Web site: John . Carroll . Fierce Biotech . 12 November 2013 . GlaxoSmithKline loses its first big PhIII bet on heart drug darapladib .
  4. Web site: GSK announces phase III study with darapladib did not meet primary endpoint in patients following an acute coronary syndrome . 13 May 2014 . GlaxoSmithKline plc . 2014-07-02 . https://web.archive.org/web/20140714200904/http://www.gsk.com/media/press-releases/2014/gsk-announces-phase-iii-study-with-darapladib-did-not-meet-prima.html . 2014-07-14 . dead .
  5. Wagner MP, Formaglio P, Gorgette O, Dziekan JM, Huon C, Berneburg I, Rahlfs S, Barale JC, Feinstein SI, Fisher AB, Ménard D, Bozdech Z, Amino R, Touqui L, Chitnis CE . Human peroxiredoxin 6 is essential for malaria parasites and provides a host-based drug target . Cell Rep . 39 . 11 . 110923 . June 2022 . 35705035 . 10.1016/j.celrep.2022.110923 . 10356/164886 . free .

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