HDL biology
Gemfibrozil raises HDL3 cholesterol 34.5% and plasma CETP activity 15.8% in hypertriglyceridaemic patients (J Intern Med 1995)
Original title: Effect of gemfibrozil on the regulation of HDL subfractions in hypertriglyceridaemic patients
Twenty patients with hypertriglyceridaemia were randomized to gemfibrozil 1200 mg/day or placebo for 3 months, following a 6-week single-blind placebo period, in a double-blind design; HDL subfractions, apolipoproteins, and lipolytic and transfer enzyme activities were measured in six patients from each group. Gemfibrozil increased HDL cholesterol (+11.1%) due to a rise in HDL3 cholesterol (+34.5%, P < 0.01). LpA-I particle concentration decreased (-12.4%, P < 0.05) while apoA-II increased (+12.3%, P < 0.01), and the LpA-I to LpA-I:A-II ratio decreased (-18.9%, P < 0.01). Gemfibrozil increased lipoprotein lipase and hepatic lipase activities by 18.2% (P < 0.05) and 19.6%, and plasma CETP activity also increased (+15.8%, P < 0.05). The authors conclude the gemfibrozil-induced rise in HDL3 and apoA-II may reflect the combined action of lipoprotein lipase, hepatic lipase, and CETP.
Original abstract
Objectives: To study changes of HDL subfractions and their regulation during gemfibrozil treatment in hypertriglyceridaemia.
Design: Twenty patients with hypertriglyceridaemia were randomized to receive either 1200 mg day-1 gemfibrozil or placebo for 3 months. After a 6-week, single-blind placebo period, the patients were randomized to receive either gemfibrozil or placebo for 3 months in a double-blind study.
Setting: The patients were studied as outpatients in the Third Department of Medicine, Helsinki University Central Hospital, Helsinki, Finland.
Main Outcome Measures: Ultracentrifugally isolated HDL subclasses; concentrations of apoA-I, apoA-II, LpA-I and LpA-I:A-II particles; post-heparin plasma lipoprotein lipase (LPL), hepatic lipase (HL) and plasma cholesteryl ester transfer protein (CETP) activities; phospholipid transfer protein (PLTP) and lecithine cholesteryl acyltransferase (LCAT) activities were measured in plasma from six patients from both groups.
Results: Gemfibrozil increased the concentration of HDL cholesterol (+11.1%) because of the rise of HDL3 cholesterol (34.5%, P < 0.01). The concentration of LpA-I particles was reduced during gemfibrozil treatment (-12.4%, P < 0.05), while that of apoA-II increased (+12.3%, P < 0.01). The LpA-I to LpA-I:A-II ratio decreased significantly in the gemfibrozil group (-18.9%, P < 0.01). Gemfibrozil increased LPL and HL activities by 18.2% (P < 0.05) and by 19.6%, respectively. Plasma CETP activity was also increased during gemfibrozil treatment (+15.8%, P < 0.05).
Conclusion: The gemfibrozil-induced elevation of HDL3 and apoA-II may reflect the combined action of LPL, HL and CETP on plasma HDL metabolism.
Summary written by cetpinhibition.org from the published abstract; figures as published. Page updated 19 August 2026. Methods.