Lomitapide (Synonyms: AEGR 773, BMS 201038) |
| カタログ番号GC16870 |
ロミタピド (AEGR-733; BMS-201038) は、インビトロで 8 nM の IC50 を持つミクロソーム トリグリセリド転送タンパク質 (MTP) の強力な阻害剤です。
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Cas No.: 182431-12-5
Sample solution is provided at 25 µL, 10mM.
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Lomitapide (AEGR-733, BMS-201038) is an oral inhibitor of microsomal triglyceride transfer protein [1].
Microsomal triglyceride transfer protein (MTP) plays an important role in lipoprotein assembly. The mutation of MTP can cause abetalipoproteinemia.
Lomitapide is a MTP inhibitor and used for the treatment of homozygous familial hypercholesterolemia. In patients with familial hypercholesterolemia, lomitapide reduced low-density lipoprotein cholesterol (LDL-C) by more than 50% both as monotherapy and in combination with prescribed lipid-lowering therapies [1]. Lomitapide bound to and inhibited MTP within the lumen of the endoplasmic reticulum and inhibited the synthesis of VLDL and chylomicrons, resulting in the reduction of circulating LDL-C concentrations. In human, lomitapide (50 mg) reduced apo B, LDL-C and total cholesterol concentrations in a dose dependent way. However, lomitapide caused significant gastrointestinal (GI) disturbances at the concentration of 100 mg [2].
References:
[1]. Rizzo M. Lomitapide, a microsomal triglyceride transfer protein inhibitor for the treatment of hypercholesterolemia. IDrugs, 2010, 13(2): 103-111.
[2]. Davis KA, Miyares MA. Lomitapide: A novel agent for the treatment of homozygous familial hypercholesterolemia. Am J Health Syst Pharm, 2014, 71(12): 1001-1008.
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