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SB-204990, SB 204990, SB204990
SB-204990 is the prodrug of the potent ATP citrate-lyase inhibitor SB-201076. SB-204990, when administered orally to rats, was absorbed into the systemic circulation, pharmacologically relevant concentrations of SB-201076 were recovered in the liver. SB-204990 (25 mg/kg per day) also decreased plasma cholesterol levels (by up to 23%) and triglyceride levels (by up to 38%) in the dog, preferentially decreasing low-density lipoprotein compared with high-density lipoprotein cholesterol levels. SB-204990 is an important enzyme in controlling substrate supply for lipid synthesis de novo and a potential enzyme target for hypolipidaemic intervention.