title: Micronized fenofibrate in dyslipidemia: a focus on plasma high-density lipoprotein cholesterol (HDL-C) levels.
abstract: The prodrug fenofibrate, a synthetic phenoxy-isobutyric acid derivative, is rapidly hydrolyzed in vivo to form fenofibric acid, which alters plasma lipid levels by activating the peroxisome proliferator-activated receptor alpha. The micronized fenofibrate 200 mg capsule formulation, and the recently developed micronized fenofibrate 160 mg tablet formulation, are bioequivalent. Micronized fenofibrate 200 mg/day (capsules) increased high density lipoprotein cholesterol (HDL-C) levels significantly from baseline in up to 7098 patients with various dyslipidemias in noncomparative studies. Micronized fenofibrate 200 mg/day (capsules) produced significantly greater elevations in HDL-C levels than a variety of HMG-CoA reductase inhibitors in small, randomized, double-blind and nonblind studies in patients with dyslipidemia (n = 91 to 227). This formulation of fenofibrate and gemfibrozil produced similar increases in HDL-C levels in a randomized, double-blind study (n = 234). Micronized fenofibrate 160 mg once daily (tablet) increased HDL-C levels significantly from baseline by 10.6 to 14.5% in patients with type IIa or IIb dyslipidemia (n = 353) in two noncomparative studies. Additionally, total cholesterol (TC), low-density lipoprotein cholesterol (LDL-C) and triglyceride levels, and LDL-C to HDL-C and TC to HDL-C ratios were lowered significantly from baseline. The tablet and capsule formulations of fenofibrate were both generally well tolerated in two noncomparative studies in 375 or 9884 patients. In double-blind, placebo-controlled trials in a total of 804 patients, the pooled incidences of individual adverse events were generally similar with fenofibrate and placebo.
authors.affiliation: Adis International Limited, Langhorne, Pennsylvania 19047, USA. demail@adis.com
authors.forename: Miriam
authors.initials: M
authors.lastname: Sharpe
authors.forename: Douglas
authors.initials: D
authors.lastname: Ormrod
authors.forename: Blair
authors.initials: B
authors.lastname: Jarvis
mesh_terms: D001682:Biological Availability; D008076:Cholesterol, HDL / Q000097:blood*; D004359:Drug Therapy, Combination; D011345:Fenofibrate / Q000008:administration & dosage / Q000493:pharmacokinetics* / Q000627:therapeutic use; D006801:Humans; D006949:Hyperlipidemias / Q000188:drug therapy*; D000960:Hypolipidemic Agents / Q000008:administration & dosage / Q000493:pharmacokinetics* / Q000627:therapeutic use; D016032:Randomized Controlled Trials as Topic; D013810:Therapeutic Equivalency
chemical_list: D008076:Cholesterol, HDL; D000960:Hypolipidemic Agents; D011345:Fenofibrate