洛美他派
洛美他派 性质
| 熔点 | 142°C(lit.) |
|---|---|
| 沸点 | 778.2±60.0 °C(Predicted) |
| 密度 | 1.34±0.1 g/cm3(Predicted) |
| 储存条件 | 2-8°C |
| 溶解度 | 可溶于DMSO（少许）、甲醇（少许） |
| 酸度系数(pKa) | 12.66±0.20(Predicted) |
| 形态 | 粉末 |
| 颜色 | 白色至米色 |
洛美他派 用途与合成方法
| 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%).
