The microsomal triglyceride transfer protein (MTTP) is necessary for the assembly of very low-density lipoprotein (VLDL), a precursor of LDL, and its secretion from the liver. Preventing the activity of MTTP has been examined as a therapeutic strategy for reducing LDL production and plasma LDL cholesterol levels in patients with homozygous familial hypercholesterolemia (FH), an autosomal dominant disease caused by mutations in the LDL receptor gene.{28401} Lomitapide is a potent inhibitor of MTTP with an IC50 value of 8 nM in vitro.{28400} It has been shown to reduce the production of apolipoprotein B, thereby lowering LDL cholesterol levels, in both preclinical and clinical FH studies.{28401,14582}
产品描述
An inhibitor of MTTP (IC50 = 8 nM in vitro) that has been shown to reduce the production of apolipoprotein B, thereby lowering LDL cholesterol levels, in both preclinical and clinical homozygous familial hypercholesterolemia studies
