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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.

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).