Metabolic Effects of the PPARdelta Agonist SAR351034 after Two Weeks of QD Dosing in Healthy Elderly Subjects

摘要

Materials and methods: In a placebo-controlled, parallel-group, escalating oral dose study, 47 subjects (mean age 71.5 years) received once daily either 5, 15, 75 or 150 mg SAR351034 (n=9 per group) or placebo (n=11 total) over 15 days. Subjects received a standardized moderate-fat diet throughout the in-house period, which comprised 5 days run-in, 15-days treatment, and 7 days follow-up.The primary PD parameter was the change from baseline to Day 15 in the area under the 24-h serum triglyceride profile (TG-AUC) following a high-fat breakfast challenge at 2 h after dosing. Secondary parameters were the changes from baseline to Day 14 in fasting triglycerides, non-esterified fatty acids (NEFA), HDL and LDL cholesterol, Apolipoproteins -B, -AI and -CIII, high-sensitivity CRP, fasting blood glucose, and fasting insulin.