Evacetrapib
Evacetrapib cuts small LDL particles by up to 95% and lipoprotein(a) by up to 40%, alone or added to statins (J Clin Lipidol 2016)
Original title: Evacetrapib alone or in combination with statins lowers lipoprotein(a) and total and small LDL particle concentrations in mildly hypercholesterolemic patients
In a placebo-controlled trial of 393 mildly hypercholesterolemic patients (NCT01105975), VLDL and LDL particle concentrations and sizes were measured by NMR spectroscopy and lipoprotein(a) by nephelometry at baseline and week 12, in patients treated with evacetrapib monotherapy (30, 100, or 500 mg/d) or evacetrapib 100 mg combined with simvastatin 40 mg/d, atorvastatin 20 mg/d, or rosuvastatin 10 mg/d. Evacetrapib monotherapy produced significant, dose-dependent, placebo-adjusted reductions from baseline in lipoprotein(a) (up to -40% at 500 mg), total LDL particle concentration (up to -54%), and small LDL particle concentration (up to -95%). Combined with statins, evacetrapib further reduced lipoprotein(a) by 31%, total LDL particles by 22%, and small LDL particles by 60% versus statin alone, and the proportion of patients above optimal LDL particle and small LDL particle thresholds fell from 88% and 55% at baseline to 20% and 12% at week 12 with combination treatment; evacetrapib also significantly increased LDL particle size, alone or with statins.
Original abstract
Background: Potent CETP inhibitors reduce plasma concentrations of atherogenic lipoprotein biomarkers of cardiovascular risk.
Objectives: To evaluate the effects of the cholesteryl ester transfer protein (CETP) inhibitor evacetrapib, as monotherapy or with statins, on atherogenic apolipoprotein B (apoB)-containing lipoproteins in mildly hypercholesterolemic patients.
Methods: VLDL and LDL particle concentrations and sizes (using nuclear magnetic resonance spectroscopy) and lipoprotein(a) concentration (using nephelometry) were measured at baseline and week 12 in a placebo-controlled trial of 393 patients treated with evacetrapib as monotherapy (30 mg/d, 100 mg/d, or 500 mg/d) or in combination with statins (100 mg plus simvastatin 40 mg/d, atorvastatin 20 mg/d, or rosuvastatin 10 mg/d; Clinicaltrials.gov Identifier: NCT01105975).
Results: Evacetrapib monotherapy resulted in significant placebo-adjusted dose-dependent decreases from baseline in Lp(a) (up to -40% with evacetrapib 500 mg), total LDL particle (LDL-P) (up to -54%), and small LDL particle (sLDL) (up to -95%) concentrations. Compared to statin alone, coadministration of evacetrapib and statins also resulted in significant reduction from baseline in Lp(a) (-31%), LDL-P (-22%), and sLDL (-60%) concentrations. The percentage of patients with concentrations above optimal concentrations for LDL-P (>1000 nmol/L) and sLDL (>600 nmol/L) decreased from 88% and 55% at baseline, respectively, to 20% and 12% at week 12, for patients treated with evacetrapib plus statins. Evacetrapib, alone or with statins, significantly increased LDL-P size.
Conclusions: Evacetrapib, as monotherapy or with statins, significantly reduces the concentrations of atherogenic apoB-containing lipoproteins, including Lp(a), LDL-P, and sLDL.
evacetrapibLDL and apoBlipoprotein a
Summary written by cetpinhibition.org from the published abstract; figures as published. Page updated 18 August 2026. Methods.