LY-2484595 (Evacetrapib) is a benzazepine-based, selective inhibitor of cholesteryl ester transfer protein (CETP) at an IC50 value of 5.5 nM for human recombinant CETP. Inhibition in human plasma was 3.6 nM IC50. [1] In H295R cells at concentrations up to 10 uM, LY-2484595 has been shown to elevate HDL cholesterol without inducing aldosterone, cortisol synthesis, or increasing blood pressure.

In a randomized controlled trial of 398 patients with elevated LDL and low HDL, LY-2484595 was shown to be effective in lowering LDL and raising HDL. In combination with statins, LY-2484595 showed greater efficacy in lowering LDL with no adverse effects. [2]