Safety, pharmacokinetics, and pharmacodynamics of oral apoA-I mimetic peptide D-4F in high-risk cardiovascular patients

摘要: Patients with coronary heart disease or equivalent risk received a single dose of 30, 100, 300, 500 mg unformulated D-4F (n = 8, each dose) placebo 8) under fasting conditions. An additional 10 patients 2) low-fat meal. There were no significant trends in any safety parameter. was detectable plasma at all doses T(max) 30 min, 1 h, and 2 h for > 300 mg, respectively. The area the curve((0-t)) 27.81 ng/hr/ml 54.71 groups, respectively, 17.96 given food. HDL from time point subject tested its ability to inhibit LDL-induced monocyte chemotactic activity cultures human aortic endothelial cells. values obtained normalized 1.0 LDL alone obtain inflammatory index. This index significantly improved 4 compared (P < 0.05). changes lipid lipoprotein levels. We conclude that has low bioavailability is conditions, safe well tolerated may improve anti-inflammatory