| Name | Lomitapide |
| Description | Lomitapide (AEGR-733) is a small molecule inhibitor of microsomal triglyceride transfer protein (MTP), an enzyme located in the lumen of the endoplasmic reticulum responsible for absorbing dietary lipids and transferring triglycerides onto apolipoprotein B (apo-B) in the assembly of very-low-density lipoprotein. |
| In vitro | 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 through cytochrome P-450 (CYP) isoenzyme 3A4 and interacts with CYP3A4 substrates including atorvastatin and simvastatin[2]. |
| In vivo | Lomitapide, either as monotherapy or in combination with other lipid-lowering agents, notably reduces low-density lipoprotein cholesterol (LDL-C) levels by over 50%. However, its use is accompanied by significant gastrointestinal side effects and increased hepatic fat. The 50-mg capsule of lomitapide has a bioavailability of 7.1%, and its mean half-life is approximately 39.7 hours[2]. Administration of a single dose of lomitapide can decrease serum triglycerides by 35% and 47% at dosages of 0.3 and 1 mg/kg, respectively. Moreover, multiple-dose regimens have shown a dose-dependent reduction in triglycerides (71%-87%), nonesterified fatty acids (33%-40%), and LDL-C (26-29%)[3]. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 242 mg/mL (348.84 mM), Sonication is recommended.
H2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : 93 mg/mL (134.06 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 5 mg/mL (7.21 mM), Sonication is recommended.
|
| Keywords | MTP | Lomitapide | Inhibitor | inhibit | BMS201038 | BMS 201038 | AEGR733 | AEGR 733 |
| Inhibitors Related | Granotapide | BMS-212122 | KD-026 | CP-346086 dihydrate | Implitapide | CP-346086 | CP-319340(free base) | LAB687 | Dirlotapide | Lomitapide Mesylate | Implitapide Racemate | PF-02575799 |
| Related Compound Libraries | Bioactive Compound Library | Approved Drug Library | ReFRAME Related Library | EMA Approved Drug Library | Anti-Obesity Compound Library | Drug Repurposing Compound Library | Inhibitor Library | NO PAINS Compound Library | FDA-Approved Drug Library | Lipid Metabolism Compound Library | Bioactive Compounds Library Max | Anti-Metabolism Disease Compound Library |
United States
