[CAS NO. 182431-12-5] Lomitapide

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PRODUCTS SPECIFICATIONS [182431-12-5]

Catalog

HY-14667

Brand

MCE

CAS

182431-12-5

DESCRIPTION [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

For research use only. We do not sell to patients.

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

In Vitro:

DMSO : ≥ 100 mg/mL ( 144.15 mM )

* "≥" means soluble, but saturation unknown.

Preparing
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

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.5 mg/mL (3.60 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: 2.5 mg/mL (3.60 mM); Suspended solution; Need ultrasonic
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.5 mg/mL (3.60 mM); Clear solution

* All of the co-solvents are available by MCE.

References

Synonyms

9H-Fluorene-9-carboxamide, N-(2,2,2-trifluoroethyl)-9-[4-[4-[[[4′-(trifluoromethyl)[1,1′-biphenyl]-2-yl]carbonyl]amino]-1-piperidinyl]butyl]-

N-(2,2,2-Trifluoroethyl)-9-[4-[4-[[[4′-(trifluoromethyl)[1,1′-biphenyl]-2-yl]carbonyl]amino]-1-piperidinyl]butyl]-9H-fluorene-9-carboxamide

BMS 201238

BMS 201038

AEGR 733

BMS 201038-01

Lomitapide

Lojuxta