Efficacy and safety of disodium ascorbyl phytostanol phosphates in men with moderate dyslipidemia

Abstract

Objective This study investigated the efficacy, safety, tolerability, and pharmacokinetics of a novel cholesterol absorption inhibitor, FM-

Lipid-lowering Activity of Natural and Semi-Synthetic Sterols and Stanols

“…Interestingly, the cholesterol-lowering effects of FM-VP4 were associated with a significant reduction in abdominal fat and less body weight gain in diet-induced obese mice (178) and hamsters (174 Results from clinical trials in humans have shown that administration of FM-VP4 at a dose of 400 mg/day reduced LDL-C by 6.5% compared with baseline levels over four weeks' treatment period. Similar reduction in LDL-C levels was reported with plant sterol and stanol esters but at doses 2-3 times higher than that of FM-VP4 (175).…”

“…Mild adverse effects were reported including dizziness, headache and fatigue (175). These adverse effects were resolved spontaneously.…”

“…Evidence from previous studies has suggested that FM-VP4 is more effective in lowering plasma cholesterol levels than plant sterols/ stanols (159,174,175). In an early study, Apo E-deficient mice have been used to evaluate the lipid-lowering effects and anti-atherosclerotic properties of FM-VP4.…”

“…It has been suggested that FM-VP4 could inhibit cholesterol incorporation into mixed micelles and thereby reduce the extent of cholesterol solubilisation and absorption into intestinal epithelial cells (175,181). FM-VP4 actually has a significant advantage over other plant sterols/stanols in that it has greater solubility in GI mixed micelles.…”

“…This advantage is achieved by incorporation of hydrophilic ascorbyl residue to the hydrophobic campestanol and sitostanol tail through a phosphodiester bond. The unique amphiphilic structure of FM-VP4 allows selfassembly into micelle structures in aqueous solutions in the absence of bile salt (175,182).…”