Merck, SML3097-10MG, Darapladib

Biochem/physiol Actions
Darapladib (SB-480848) is an orally active and highly potent lipoprotein associated phospholipase A2 inhibitor (rhLp-PLA2 IC50 = 0.25 nM) with little interaction with cytochrome P450 enzymes (3A4 & 2D6 IC50 >26 μM). Darapladib effectively inhibits plasma Lp-PLA2 activtiy ex vivo (by 60% at 10 nM in human plasma & by 79% at 100 nM in Watanabe hereditable hyperlipidaemic (WHHL) rabbit plasma) and in vivo (by 95% & 91%, respectively, 3 & 5 hrs post 10 mg/kg WHHL rabbits via p.o.).
Orally active and highly potent lipoprotein associated phospholipase A2 inhibitor (Lp-PLA2 ) with little interaction with cytochrome P450 enzymes.