Anacetrapib-driven triglyceride lowering explained: the fortuitous role of CETP in the intravascular catabolism of triglyceride-rich lipoproteins

Brown, Amanda

doi:10.1194/jlr.c077131

Cited by 2 publications

(3 citation statements)

References 24 publications

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“…(1) Increased lipolysis of the large TRG-rich VLDL particles through lipoprotein lipase (even without increased lipolytic activity) [ 23 ].…”

Section: Main Results Of the Reveal Trialmentioning

confidence: 99%

“…(2) Other compositional changes in VLDL particles, such as increased Apo E and reduced Apo CIII content, which can increase lipoprotein lipase activity and the hepatic receptor-mediated clearance of remnant particles [ 12 , 23 ].…”

Section: Main Results Of the Reveal Trialmentioning

confidence: 99%

“…(3) Increased hepatic uptake of the large triglyceride-rich (depleted of cholesterol) VLDL particles [ 16 , 23 ].…”

Section: Main Results Of the Reveal Trialmentioning

confidence: 99%

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Anacetrapib, a New CETP Inhibitor: The New Tool for the Management of Dyslipidemias?

2017

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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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“…(1) Increased lipolysis of the large TRG-rich VLDL particles through lipoprotein lipase (even without increased lipolytic activity) [ 23 ].…”

Section: Main Results Of the Reveal Trialmentioning

confidence: 99%

Section: Main Results Of the Reveal Trialmentioning

confidence: 99%

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Anacetrapib, a New CETP Inhibitor: The New Tool for the Management of Dyslipidemias?

2017

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The effect and safety of anacetrapib in the treatment of dyslipidemia: a systematic review and meta-analysis

Zhou

Zhang

Wang

et al. 2017

Postgraduate Medicine

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Anacetrapib-driven triglyceride lowering explained: the fortuitous role of CETP in the intravascular catabolism of triglyceride-rich lipoproteins

Abstract: Abbreviations: CETP, cholesteryl ester transfer protein; FCR, fractional catabolic rate; HDL, high density lipoprotein; PR, production rate; LDL, low density lipoprotein; VLDL, very low density lipoprotein.

Cited by 2 publications

References 24 publications

Anacetrapib, a New CETP Inhibitor: The New Tool for the Management of Dyslipidemias?

Anacetrapib, a New CETP Inhibitor: The New Tool for the Management of Dyslipidemias?

The effect and safety of anacetrapib in the treatment of dyslipidemia: a systematic review and meta-analysis

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