The class
CETP inhibition boosts postprandial insulin secretion via enhanced cholesterol efflux from beta cells (Circ Res 2013)
Original title: Effects of high-density lipoprotein elevation with cholesteryl ester transfer protein inhibition on insulin secretion
Since raising HDL cholesterol through CETP inhibition may have relevance for type 2 diabetes as well as atherosclerosis, researchers tested its effects on insulin secretion in a randomised, double-blind study in which healthy participants received a daily CETP inhibitor (n=10) or placebo (n=15) for 14 days. CETP inhibition raised plasma HDL cholesterol, apolipoprotein AI, and postprandial insulin. When cultured MIN6N8 pancreatic beta cells were incubated with plasma from CETP-inhibitor-treated participants, they showed increased glucose-stimulated insulin secretion and increased cholesterol efflux compared with plasma from placebo-treated participants, over the 14-day treatment period. The authors conclude CETP inhibition increases postprandial insulin secretion, potentially mediated by enhanced cholesterol efflux from pancreatic beta cells.
Original abstract
Rationale: High-density lipoprotein cholesterol elevation via cholesteryl ester transfer protein (CETP) inhibition represents a novel therapy for atherosclerosis, which also may have relevance for type 2 diabetes mellitus.
Objective: The current study assessed the effects of a CETP inhibitor on postprandial insulin, ex vivo insulin secretion, and cholesterol efflux from pancreatic β-cells.
Methods And Results: Healthy participants received a daily dose of CETP inhibitor (n=10) or placebo (n=15) for 14 days in a randomized double-blind study. Insulin secretion and cholesterol efflux from MIN6N8 β-cells were determined after incubation with treated plasma. CETP inhibition increased plasma high-density lipoprotein cholesterol, apolipoprotein AI, and postprandial insulin. MIN6N8 β-cells incubated with plasma from CETP inhibitor-treated individuals (compared with placebo) exhibited an increase in both glucose-stimulated insulin secretion and cholesterol efflux over the 14-day treatment period.
Conclusions: CETP inhibition increased postprandial insulin and promoted ex vivo β-cell glucose-stimulated insulin secretion, potentially via enhanced β-cell cholesterol efflux.
Summary written by cetpinhibition.org from the published abstract; figures as published. Page updated 19 August 2026. Methods.