The class
Baseline plasma CETP activity is elevated in dyslipidaemic patients and correlates with triglycerides (Int J Clin Pharmacol Ther 2012)
Original title: Phase 0 study of the inhibition of cholesteryl ester transfer protein activity by JNJ-28545595 in plasma from normolipidemic and dyslipidemic humans
Researchers validated a non-radioactive assay for CETP activity in clinical samples by measuring how the CETP inhibitor JNJ-28545595 suppressed activity in plasma from normolipidaemic subjects and three subgroups of dyslipidaemic subjects with differing lipid profiles. CETP activity was elevated in plasma from dyslipidaemic subjects compared with normolipidaemic subjects, and higher triglyceride levels correlated with reduced CETP inhibition by the drug. The assay showed good analytical precision and high throughput suitable for clinical trial sample analysis. The authors conclude that pharmacological CETP inhibition is affected by the dyslipidaemic nature of the plasma sample, and that this assay could help define optimal CETP inhibitor dosing since the ideal degree of inhibition for cardiovascular benefit remains unknown.
Original abstract
Objective: To assess and validate the application of a non-radioactive assay for cholesteryl ester transfer protein (CETP) activity in clinical samples.
Design And Methods: In this Phase 0 study, CETP activity was measured following addition of the CETP inhibitor JNJ-28545595 to plasma samples from normolipidemic and three subgroups of dyslipidemic subjects with differing lipid profiles.
Results: CETP activity was elevated in plasma samples from dyslipidemic subjects compared to normolipidemic subjects. Increased triglyceride levels correlated with decreased CETP inhibition. The assay was found to have good analytical precision and high throughput potential as required for clinical trial sample analysis.
Conclusions: The results demonstrate that pharmacological inhibition of CETP is affected by the dyslipidemic nature of plasma samples. In addition, since the optimal degree of CETP inhibition for maximal cardiovascular benefit in patients is not known, this assay may be used to help define optimal dosing of CETP inhibitors.
Summary written by cetpinhibition.org from the published abstract; figures as published. Page updated 19 August 2026. Methods.