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| Other names | SB-480848 |
| Routes of administration | By mouth |
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| ECHA InfoCard | 100.130.738 |
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| Formula | C36H38F4N4O2S |
| Molar mass | 666.78 g·mol−1 |
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Darapladib is an inhibitor oflipoprotein-associated phospholipase A2 (Lp-PLA2) that is indevelopment as adrug for treatment ofatherosclerosis.[1]
It was discovered byHuman Genome Sciences in collaboration withGlaxoSmithKline (GSK).[2]
In November 2013, GSK announced that the drug had failed to meet Phase III endpoints in a trial of 16,000 patients withacute 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 ofcoronary heart disease death,myocardial infarction, and urgent coronaryrevascularization compared with placebo in acute coronary syndrome patients treated with standard medical care.[4]
In 2022, Darapladib has been found to inhibitintraerythrocytic growth of the malaria parasitePlasmodium falciparum by inhibition of the human host enzymeperoxiredoxin 6.[5] The authors present data that the original target of Darapladib,Lp-PLA2, is absent in the hostred blood cell.
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