Anacetrapib (MK-0859) (MK0859) is an effective, specific, reversible rhCETP and mutant CETP(C13S) inhibitor (IC50: 7.9 nM and 11.8 nM). Anacetrapib reduces the transfer of cholesteryl ester from HDL to LDL and/or VLDL thereby, producing an increase in serum HDL-cholesterol levels and a decrease in serum LDL-cholesterol levels.

BMS-212122 (UNII-0Z473OO6GB) is a potent inhibitor of microsomal triglyceride transfer protein (MTP) and has shown hypolipidemic effects in animal studies.BMS-212122 significantly reduced lipid content and monocyte-derived (CD68+) cells in atherosclerotic plaques.

Granotapide is a microsomal triglyceride transfer protein (MTP) inhibitor that treats and rather prevents atherosclerosis, coronary artery disease, metabolic syndrome, obesity, diabetes mellitus, prediabetes mellitus, and hypertension.

Dalcetrapib (RO4607381), a rhCETP inhibitor (IC50=0.2 μM), increases the plasma HDL cholesterol.

Obicetrapib (AMG-899) is an inhibitor of cholesteryl ester transfer protein.

Lomitapide Mesylate (BMS-201038 mesylate) is a methanesulfonic acid form of lomitapide, a small molecule inhibitor of microsomal triglyceride transfer protein.

Lomitapide (AEGR-733) is a small molecule inhibitor of microsomal triglyceride transfer protein (MTP), an enzyme located in the lumen of the endoplasmic reticulum responsible for absorbing dietary lipids and transferring triglycerides onto apolipoprotein B (apo-B) in the assembly of very-low-density lipoprotein.

Torcetrapib (CP-529414) is a cholesteryl ester transfer protein (CETP) inhibitor designed to reduce the heterotypic transfer of cholesteryl ester from HDL to LDL and/or VLDL. It failed in phase III trials due to an excess of deaths.