The class
Phase 1 single ascending dose study of the CETP inhibitor CKD-519 shows potent target inhibition (Drug Des Devel Ther 2016)
Original title: Pharmacokinetics, pharmacodynamics and safety of CKD-519, a CETP inhibitor, in healthy subjects
In a randomised, double-blinded, placebo-controlled single ascending dose study, healthy adults received CKD-519, a selective CETP inhibitor being developed to raise HDL cholesterol, at doses of 25, 50, 100, 200 or 400 mg (6 active, 2 placebo per group). CKD-519 reached maximum plasma concentration at 5 to 6 hours post-dose with a long terminal half-life of 40 to 70 hours, and CETP activity fell with dose, with the maximum decrease of 63% to 83% observed at 6 to 8 hours post-dose; a sigmoid Emax model described the concentration-effect relationship with an EC50 of 17.3 ng/mL. Eleven adverse events occurred, all mild or moderate and resolved without complication, with no clinically significant effects on blood pressure, indicating doses up to 400 mg were well tolerated with potent CETP inhibition.
Original abstract
CKD-519 is a selective and potent cholesteryl ester transfer protein (CETP) inhibitor being developed for the treatment of dyslipidemia to raise high-density lipoprotein cholesterol. We investigated the safety, tolerability, pharmacokinetics, and pharmacodynamics of single doses of CKD-519 in healthy adult subjects. A randomized, double-blinded, placebo-controlled, single ascending dose study was performed. Eight healthy subjects were enrolled in each CKD-519 dose group (25, 50, 100, 200, or 400 mg) and randomized to CKD-519 (n=6) or matching placebo (n=2). CKD-519 reached the maximum plasma concentration (Cmax) at 5-6 h post-dose, and had a long terminal half-life ranging between 40-70 h. The area under the plasma concentration-time curve (AUC) and Cmax increased with the dose, however, Cmax and AUC normalized by dose decreased with each incremental dose. CETP activity decreased with dose, and the maximum decrease (63%-83%) was observed at 6-8 h post-dose. A sigmoid Emax model best described the relationship between CKD-519 plasma concentrations and CETP activity with an EC50 of 17.3 ng/mL. Overall, 11 adverse events (AEs) were observed. All AEs were mild or moderate in intensity, and resolved without any complications. There were no clinically significant effects on blood pressure. In conclusion, single doses of CKD-519 up to 400 mg were well tolerated and showed potent inhibition of CETP activity.
the classpharmacologyphase 1safety
Summary written by cetpinhibition.org from the published abstract; figures as published. Page updated 19 August 2026. Methods.