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von Eckardstein A, Binder CJ, editors. Prevention and Treatment of Atherosclerosis: Improving State-of-the-Art Management and Search for Novel Targets [Internet]. Cham (CH): Springer; 2022. doi: 10.1007/164_2020_361

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Prevention and Treatment of Atherosclerosis: Improving State-of-the-Art Management and Search for Novel Targets [Internet].

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Fig. 4. Mechanism of action of bempedoic acid.

Fig. 4

Mechanism of action of bempedoic acid. Bempedoic acid inhibits cellular cholesterol biosynthesis by blocking the activity of ATP citrate lyase (ACLY), an enzyme upstream of hydroxymethylglutaryl-CoA reductase (the target of statins). Therefore cells upregulate the expression of the LDLR to compensate for reduced cholesterol biosynthesis. A specific enzyme, ACSVL1 (very-long-chain acyl-CoA sinthetase-1), expressed in the liver but not in other peripheral tissues, converts bempedoic acid into the active form thus conferring hepatoselectivity to the drug

From: LDL-Cholesterol-Lowering Therapy

Copyright 2020, The Author(s)

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