Lomitapide (Synonyms: AEGR 773, BMS 201038) |
رقم الكتالوجGC16870 |
Lomitapide (AEGR-733 ؛ BMS-201038) هو مثبط قوي لبروتين نقل الدهون الثلاثية الميكروسومي (MTP) مع IC 50 من 8 نانومتر في المختبر
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 182431-12-5
Sample solution is provided at 25 µL, 10mM.
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.
Average Rating: 5
(Based on Reviews and 24 reference(s) in Google Scholar.)GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *