Lipid-modifying efficacy of extended release niacin/laropiprant in Asian patients with primary hypercholesterolemia or mixed hyperlipidemia

Kush, D.; Kim, Hyo–Soo; Hu, Da Yi; Liu, Ji; Sirah, Waheeda; Sapre, Aditi; Sisk, Christine McCrary; Paolini, John F.; Maccubbin, Darbie

doi:10.1016/j.jacl.2009.04.048

Cited by 3 publications

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“…Antagonism of DP1 suppresses niacininduced vasodilation signifi cantly in mice and humans ( 80 (85)(86)(87)(88)(89)(90). Interestingly, despite tachyphylaxis of niacin-induced PGD 2 within a week ( 75 ), LRPT's anti-fl ushing effect is reportedly sustained for months ( 82,83 ).…”

Section: Effects On Hdlmentioning

confidence: 99%

Niacin, an old drug with a new twist

Song

FitzGerald

2013

Journal of Lipid Research

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This article is available online at http://www.jlr.org the only approved drug with such an effect ( 1 ). It has proven to be an attractive option for those intolerant of statin treatment. It has been demonstrated to reduce risk of atherosclerotic cardiovascular disease ( 4 ). The clinical use of niacin has been markedly limited by cutaneous fl ushing. The molecular target of niacin responsible for lipid metabolic changes and fl ushing was unknown until 2003 ( 5-7 ), when the niacin receptor, namely HM74A in humans and PUMA-G in mice, was discovered. The niacin receptor, also known as GPR109A, was shown to be activated by niacin and to mediate its antilipolytic effect as well as the fl ushing effect ( 8-10 ). Interest in niacin has risen because there is still signifi cant residual risk in patients with intensive statin therapy ( 11 ). However, recent outcome trials ( 11, 12 ) failed to show niacin's benefi t on top of statin therapy in lipid-targeted approaches to reduce major cardiovascular events in high-risk patients. In this review we will summarize the pharmacology of niacin, with a particular emphasis on recent outcome trials, including discussion of their limitations . NIACIN'S LIPID EFFECTSNiacin has long been shown to have effects on lipids ( 13 ). Niacin increases high density lipoprotein cholesterol (HDLc), but reduces low density lipoprotein cholesterol (LDLc), VLDL cholesterol, and triglycerides (TGs) ( 14 ) Niacin is also known as vitamin B3. Chronic dietary defi ciency of niacin can cause pellagra ( 1 ). It is a precursor to NAD+/NADH and NADP+/NADPH, both of which play essential metabolic roles in living cells ( 2 ). Niacin has been used for more than half a century in the treatment of dyslipidemia. When Altschul, Hoffer, and Stephen ( 3 ) discovered that niacin could lower plasma levels of cholesterol, it was

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Section: Effects On Hdlmentioning

confidence: 99%

Niacin, an old drug with a new twist

Song

FitzGerald

2013

Journal of Lipid Research

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Safety and tolerability of extended-release niacin-laropiprant: Pooled analyses for 11,310 patients in 12 controlled clinical trials

McKenney

Bays

Gleim

et al. 2015

Journal of Clinical Lipidology

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Extended-Release Niacin (Nicotinic Acid)/Laropiprant

Perry

2009

Drugs

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Extended-release (ER) niacin (nicotinic acid)/laropiprant is a once-daily fixed-dose combination tablet that has been evaluated (with or without an HMG-CoA reductase inhibitor [statin]) in the treatment of adults with dyslipidaemia or primary hypercholesterolaemia. Niacin (vitamin B3) is a lipid-modifying drug and laropiprant is an anti-flushing agent, which reduces flushing induced by niacin. In a randomized, double-blind, placebo-controlled, multicentre, 24-week trial, a significant (p < 0.001) reduction (18.4%) in plasma low-density lipoprotein cholesterol (LDL-C) levels (primary endpoint) was achieved with ER niacin/laropiprant 2000 mg/40 mg once daily (after an initial 4-week 1000 mg/20 mg once-daily regimen) compared with placebo (weeks 12-24) in adults with primary hypercholesterolaemia or mixed dyslipidaemia. ER niacin/laropiprant 2000 mg/40 mg plus simvastatin 20 mg or 40 mg once daily (after an initial 4-week lower-dose regimen) produced significant (p < 0.05) improvements, from baseline, in LDL-C levels (primary endpoint) compared with once-daily ER niacin/laropiprant 2000 mg/40 mg or simvastatin alone at week 12 in a randomized, double-blind, multicentre, factorial trial in adults with primary hypercholesterolaemia or mixed dyslipidaemia. The incidence and intensity of flushing (an efficacy endpoint) were significantly (p < 0.05) reduced with ER niacin/laropiprant compared with ER niacin in randomized trials. ER niacin/laropiprant, alone or in combination with a statin, was generally well tolerated for up to 24 weeks by adults with dyslipidaemia or primary hyercholesterolaemia.

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Lipid-modifying efficacy of extended release niacin/laropiprant in Asian patients with primary hypercholesterolemia or mixed hyperlipidemia

Cited by 3 publications

References 22 publications

Niacin, an old drug with a new twist

Niacin, an old drug with a new twist

Safety and tolerability of extended-release niacin-laropiprant: Pooled analyses for 11,310 patients in 12 controlled clinical trials

Extended-Release Niacin (Nicotinic Acid)/Laropiprant

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