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[CAS NO. 182431-12-5] Lomitapide
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-14667 |
| Brand: | MCE |
| CAS: | 182431-12-5 |
Overview
| MDL | - |
|---|---|
| Molecular Weight | 693.72 |
| Molecular Formula | C39H37F6N3O2 |
| SMILES | O=C(C1(CCCCN2CCC(NC(C3=CC=CC=C3C4=CC=C(C(F)(F)F)C=C4)=O)CC2)C5=C(C6=C1C=CC=C6)C=CC=C5)NCC(F)(F)F |
2 Publications Citing Use of MCE
Summary
Lomitapide (AEGR-733; BMS-201038) is a potent inhibitor of microsomal triglyceride-transfer protein ( MTP ) with an IC 50 of 8 nM in vitro .
IC50 & Target
IC50: 8 nM (MTP) [1]
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 via cytochrome P-450 (CYP) isoenzyme 3A4 and interacts with CYP3A4 substrates including atorvastatin and simvastatin [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
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 [2] . 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%) [3] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT02173158 | Aegerion Pharmaceuticals, Inc. |
Familial Hypercholesterolemia - Homozygous
|
April 2, 2014 | Phase 3 |
| NCT02135705 | Amryt Pharma |
Homozygous Familial Hypercholesterolemia
|
March 18, 2014 | |
| NCT00690443 | Aegerion Pharmaceuticals, Inc. |
Hypercholesterolemia
|
May 2008 | Phase 2 |
| NCT02044419 | Aegerion Pharmaceuticals, Inc. |
Healthy
|
October 30, 2013 | Phase 1 |
| NCT00559962 | Aegerion Pharmaceuticals, Inc. |
Hyperlipidemia
|
October 2007 | Phase 2 |
| NCT02765841 | Aegerion Pharmaceuticals, Inc. |
Homozygous Familial Hypercholesterolemia
|
May 2016 | Phase 3 |
| NCT02399839 | Amryt Pharma |
Pregnancy
|
October 2014 | |
| NCT00474240 | Aegerion Pharmaceuticals, Inc. |
Hypercholesterolemia
|
April 2007 | Phase 2 |
| NCT04681170 | Amryt Pharma |
Homozygous Familial Hypercholesterolaemia (HoFH)
|
December 14, 2020 | Phase 3 |
| NCT01915771 | Aegerion Pharmaceuticals, Inc. |
Intra-subject Variability of Pharmacokinetics
|
July 29, 2013 | Phase 1 |
| NCT02080468 | Aegerion Pharmaceuticals, Inc. |
Healthy
|
February 19, 2014 | Phase 1 |
| NCT00730236 | Aegerion Pharmaceuticals, Inc.|FDA Office of Orphan Products Development |
Homozygous Familial Hypercholesterolemia
|
December 2007 | Phase 3 |
| NCT00943306 | Aegerion Pharmaceuticals, Inc. |
Familial Hypercholesterolemia
|
October 29, 2009 | Phase 3 |
| NCT01556906 | Aegerion Pharmaceuticals, Inc.|University of Pennsylvania|Doris Duke Charitable Foundation |
Homozygous Familial Hypercholesterolemia
|
June 2003 | Phase 2 |
| NCT02399852 | Aegerion Pharmaceuticals, Inc. |
Homozygous Familial Hypercholesterolemia
|
June 2015 | |
| NCT00405067 | Aegerion Pharmaceuticals, Inc. |
Hypercholesterolemia
|
May 2006 | Phase 2 |
| NCT01760187 | Aegerion Pharmaceuticals, Inc.|Richmond Pharmacology Limited |
Healthy Volunteer
|
November 7, 2012 | Phase 1 |
| NCT02080455 | Aegerion Pharmaceuticals, Inc. |
Effect of Atorvastatin on the Pharmacokinetics of Lomitapide
|
January 27, 2014 | Phase 1 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : ≥ 100 mg/mL ( 144.15 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.4415 mL | 7.2075 mL | 14.4150 mL |
| 5 mM | 0.2883 mL | 1.4415 mL | 2.8830 mL |
| 10 mM | 0.1442 mL | 0.7208 mL | 1.4415 mL |
References
- [1] Sulsky R, et al. 5-Carboxamido-1,3,2-dioxaphosphorinanes, potent inhibitors of MTP. Bioorg Med Chem Lett. 2004 Oct 18;14(20):5067-70.
- [2] Davis KA. et al. Lomitapide: A novel agent for the treatment of homozygous familial hypercholesterolemia. Am J Health Syst Pharm. 2014 Jun 15;71(12):1001-8.
- [3] Dhote V, et al. Inhibition of microsomal triglyceride transfer protein improves insulin sensitivity and reduces atherogenic risk in Zucker fatty rats. Clin Exp Pharmacol Physiol. 2011 May;38(5):338-44.
Synonyms
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