James McKenney, Harold Bays, Michael Koren, Christie M. Ballantyne, John F. Paolini, Yale Mitchel, Abigaile Betteridge, Olga Kuznetsova, Aditi Sapre, Christine McCrary Sisk and Darbie Maccubbin
Journal of Clinical Lipidology, 2010, 4(2), 105-112. DOI: 10.1016/j.jacl.2010.02.002
To evaluate the safety profile of extended-release niacin/laropiprant (ERN/LRPT), pooling data from studies in the clinical development program.
Data were pooled from three active- or placebo-controlled phase 3 studies and three 1-year extensions of phase 2 studies that ranged from 12 to 52 weeks (N = 4747): ERN/LRPT = 2548; ERN or Niaspan® (ERN-NSP = 1268); or simvastatin or placebo (SIMVA-PBO = 931).
The safety and tolerability profile for ERN/LRPT was similar to that of ERN-NSP, except for fewer flushing-related adverse experiences and discontinuations with ERN/LRPT than ERN-NSP. The incidence of consecutive ≥3x the upper limit of normal increases in alanine aminotransferase and/or aspartate aminotransferase was numerically (but not statistically) greater with ERN/LRPT (1.0%) than ERN-NSP (0.5%) and similar to SIMVA-PBO (0.9%). Elevations were reversible with therapy discontinuation and not associated with clinical hepatotoxicity. There was no evidence that ERN/LRPT administered alone or concurrently with a statin had adverse effects on muscle. ERN/LRPT and ERN-NSP produced small median increases in fasting blood glucose levels (∼4 mg/dL) after 24 weeks of treatment, consistent with known effects of niacin.
The favorable safety and tolerability profile of ERN/LRPT for up to 1 year supports the use of LRPT to achieve improved therapeutic dosing of niacin, an agent with comprehensive lipid-modifying efficacy and shown to reduce cardiovascular risk.
Journal of Clinical Lipidology, 2009, 3(3), 179-186. DOI: 10.1016/j.jacl.2009.04.048Extended-release niacin reduces LDL particle number without changing total LDL cholesterol in patients with stable CAD
Journal of Clinical Lipidology, 2009, 3(1), 45-50. DOI: 10.1016/j.jacl.2008.12.003Flushing and other dermatologic adverse events associated with extended-release niacin therapy
Journal of Clinical Lipidology, 2009, 3(2), 101-108. DOI: 10.1016/j.jacl.2009.02.003Effects of coadministered extended-release niacin/laropiprant and simvastatin on lipoprotein subclasses in patients with dyslipidemia
Journal of Clinical Lipidology, 2012, 6(3), 235-243. DOI: 10.1016/j.jacl.2011.11.004Lipid-modifying efficacy of extended release niacin/laropiprant in Asian patients with primary hypercholesterolemia or mixed hyperlipidemia
Journal of Clinical Lipidology, 2009, 3(3), 179-186. DOI: 10.1016/j.jacl.2009.04.048Efficacy and tolerability of extended-release niacin/laropiprant in dyslipidemic patients with metabolic syndrome
Journal of Clinical Lipidology, 2010, 4(6), 515-521. DOI: 10.1016/j.jacl.2010.08.020Extended-Release Niacin/Laropiprant Significantly Improves Lipid Levels in Type 2 Diabetes Patients Irrespective of Baseline Glycemic Control
Journal of Clinical Lipidology, 2012, 6(3), 270-271. DOI: 10.1016/j.jacl.2012.04.041Effects of coadministered extended-release niacin/laropiprant and simvastatin on lipoprotein subclasses in patients with dyslipidemia
Journal of Clinical Lipidology, 2012, 6(3), 235-243. DOI: 10.1016/j.jacl.2011.11.004A systematic review of bile acid sequestrant therapy in children with familial hypercholesterolemia
Journal of Clinical Lipidology, 2011, 5(2), 76-81. DOI: 10.1016/j.jacl.2011.01.005Antisense therapy and emerging applications for the management of dyslipidemia
Journal of Clinical Lipidology, 2011, 5(6), 441-449. DOI: 10.1016/j.jacl.2011.08.007