2459377-96-7

Lomitapide-d₈ is intended for use as an internal standard for the quantification of lomitapide by GC- or LC-MS. Lomitapide is an inhibitor of microsomal triglyceride transfer protein (MTTP; IC₅₀ = 0.5 nM in a triglyceride transfer assay).¹ It inhibits apolipoprotein B (ApoB) secretion in HepG2 cells (EC₅₀ = 0.8 nM). Lomitapide inhibits triglyceride secretion in fasted rats (ED₅₀ = 0.19 mg/kg, p.o.) and reduces total plasma cholesterol levels in hamsters (ED₅₀ = 2.4 mg/kg). It also decreases plasma cholesterol and triglyceride levels in the Watanabe-heritable hyperlipidemic (WHHL) rabbit model of homozygous familial hypercholesterolemia when administered at a dose of 10 mg/kg. Formulations containing lomitapide have been used as an adjunct to a low-fat diet and other lipid-lowering treatments in the treatment of homozygous familial hypercholesterolemia.

Lomitapide-d8 is deuterium labeled Lomitapide. Lomitapide (AEGR-733; BMS-201038) is a potent inhibitor of microsomal triglyceride-transfer protein (MTP) with an IC50 of 8 nM in vitro.

1. Wetterau, J.R., Gregg, R.E., Harrity, T.W., et al. An MTP inhibitor that normalizes atherogenic lipoprotein levels in WHHL rabbits Science 282(5389),751-754(1998).