Anacetrapib, a New CETP Inhibitor: The New Tool for the Management of Dyslipidemias?
Department of Internal Medicine, School of Medicine, University of Ioannina, Ioannina 45110, Greece
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Diseases 2017, 5(4), 21; https://doi.org/10.3390/diseases5040021
Received: 14 September 2017 / Revised: 28 September 2017 / Accepted: 29 September 2017 / Published: 29 September 2017
(This article belongs to the Special Issue New Lipid Lowering Therapies for Cardiovascular and Metabolic Diseases: Lessons from the Past and Future Challenges)
Cholesteryl ester transfer protein (CETP) inhibitors significantly increase serum high-density lipoprotein cholesterol (HDL) cholesterol levels and decrease low-density lipoprotein cholesterol (LDL) cholesterol concentration. However, three drugs of this class failed to show a decrease of cardiovascular events in high-risk patients. A new CETP inhibitor, anacetrapib, substantially increases HDL cholesterol and apolipoprotein (Apo) AI levels with a profound increase of large HDL2 particles, but also pre-β HDL particles, decreases LDL cholesterol levels mainly due to increased catabolism of LDL particles through LDL receptors, decreases lipoprotein a (Lp(a)) levels owing to a decreased Apo (a) production and, finally, decreases modestly triglyceride (TRG) levels due to increased lipolysis and increased receptor-mediated catabolism of TRG-rich particles. Interestingly, anacetrapib may be associated with a beneficial effect on carbohydrate homeostasis. Furthermore, the Randomized EValuation of the Effects of Anacetrapib Through Lipid-modification (REVEAL) trial showed that anacetrapib administration on top of statin treatment significantly reduces cardiovascular events in patients with atherosclerotic vascular disease without any significant increase of adverse events despite its long half-life. Thus, anacetrapib could be useful for the effective management of dyslipidemias in high-risk patients that do not attain their LDL cholesterol target or are statin intolerable, while its role in patients with increased Lp(a) levels remains to be established.
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Keywords:
anacetrapib; cholesteryl ester transfer protein; cardiovascular disease; apolipoprotein; diabetes
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MDPI and ACS Style
Filippatos, T.D.; Kei, A.; Elisaf, M.S. Anacetrapib, a New CETP Inhibitor: The New Tool for the Management of Dyslipidemias? Diseases 2017, 5, 21.
AMA Style
Filippatos TD, Kei A, Elisaf MS. Anacetrapib, a New CETP Inhibitor: The New Tool for the Management of Dyslipidemias? Diseases. 2017; 5(4):21.
Chicago/Turabian StyleFilippatos, Theodosios D.; Kei, Anastazia; Elisaf, Moses S. 2017. "Anacetrapib, a New CETP Inhibitor: The New Tool for the Management of Dyslipidemias?" Diseases 5, no. 4: 21.
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