182431-12-5
基本信息
MTP抑制剂(LOMITAPIDE)
N-(2,2,2-三氟乙基)-9-(4-[4-[4'-(三氟甲基)[1,1'-联苯]-2-甲酰氨基]哌啶-1-基]丁基)-9H-芴-9-甲酰胺
BMS 201038
LoMitapide
BMS 201238
BMS 201038-01
AEGR733, BMS201038
AEGR-733(Lomitapide)
CB62485047,loMitapide
Lomitapide (10mM in DMSO)
AEGR-733(Lomitapide)free base
物理化学性质
常见问题列表
Target | Value |
MTP |
Lomitapide is an oral microsomal triglyceride transfer protein (MTP) inhibitor indicated for the treatment of patients with HoFH, a rare form of hypercholesterolemia that can lead to premature atherosclerotic disease. Lomitapide undergoes hepatic metabolism via cytochrome P-450 (CYP) isoenzyme 3A4 and interacts with CYP3A4 substrates including atorvastatin and simvastatin.
The use of lomitapide alone or in combination with other lipid-lowering modalities reduces plasma concentrations of low density lipoprotein cholesterol (LDL-C) by a mean of more than 50%. Lomitapide is associated with significant gastrointestinal adverse effects and increases in hepatic fat levels. The bioavailability of the 50-mg lomitapide capsule is 7.1%. The mean half-life of lomitapide is 39.7 hours. Single-dose administration of lomitapide is shown to reduce serum triglycerides by 35% and 47% at 0.3- and 1-mg/kg doses, respectively. Multiple-dose treatment with lomitapide also results in dose dependent decrease in triglycerides (71%–87%), nonesterified fattyacids(33%–40%), and LDL-C(26-29%).