Lomitapide mesylate
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MedKoo CAT#: 314228

CAS#: 202914-84-9 (mesylate)

Description: Lomitapide is a MTP inhibitor. Lomitapid is a novel agent for the treatment of homozygous familial hypercholesterolemia. Lomitapide is an orally active inhibitor of microsomal triglyceride transfer protein that is indicated as an adjunct to a low-fat diet and other lipid-lowering treatments, including LDL apheresis where available for the reduction of LDL-C, total cholesterol, apolipoprotein B, and non-high-density lipoprotein cholesterol in adult patients with HoFH.


Chemical Structure

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Lomitapide mesylate
CAS# 202914-84-9 (mesylate)

Theoretical Analysis

MedKoo Cat#: 314228
Name: Lomitapide mesylate
CAS#: 202914-84-9 (mesylate)
Chemical Formula: C40H41F6N3O5S
Exact Mass:
Molecular Weight: 789.83
Elemental Analysis: C, 60.83; H, 5.23; F, 14.43; N, 5.32; O, 10.13; S, 4.06

Price and Availability

Size Price Availability Quantity
25.0mg USD 150.0 Same day
50.0mg USD 250.0 Same day
100.0mg USD 450.0 Same day
200.0mg USD 650.0 Same day
500.0mg USD 1450.0 Same day
1.0g USD 2450.0 Same day
2.0g USD 4250.0 Same day
5.0g USD 6850.0 2 Weeks
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Related CAS #: 202914-84-9 (mesylate)   182431-12-5 (free base)    

Synonym: AEGR 733; AEGR733; AEGR-733; BMS 201038; BMS-201038; BMS201038; BMS 201038-01. Lomitapide mesylate. Brand name: Juxtapid; Lojuxta.

IUPAC/Chemical Name: N-(2,2,2-trifluoroethyl)-9-(4-(4-(4'-(trifluoromethyl)-[1,1'-biphenyl]-2-carboxamido)piperidin-1-yl)butyl)-9H-fluorene-9-carboxamide methanesulfonate

InChi Key: QKVKOFVWUHNEBX-UHFFFAOYSA-N

InChi Code: InChI=1S/C39H37F6N3O2.CH4O3S/c40-38(41,42)25-46-36(50)37(33-13-5-3-10-30(33)31-11-4-6-14-34(31)37)21-7-8-22-48-23-19-28(20-24-48)47-35(49)32-12-2-1-9-29(32)26-15-17-27(18-16-26)39(43,44)45;1-5(2,3)4/h1-6,9-18,28H,7-8,19-25H2,(H,46,50)(H,47,49);1H3,(H,2,3,4)

SMILES Code: 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.OS(=O)(C)=O

Appearance: White to off-white Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO.

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

Preparing Stock Solutions

The following data is based on the product molecular weight 789.83 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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1: Marbach JA, Thapa J, Goldenberg E, Duffy D. Pharmacogenetics in the Development of Lipid Lowering Medications: Lomitapide & Mipomersen in Clinical Practice. Del Med J. 2015 Aug;87(8):238-43. PubMed PMID: 26402926.

2: Roeters van Lennep J, Averna M, Alonso R. Treating homozygous familial hypercholesterolemia in a real-world setting: Experiences with lomitapide. J Clin Lipidol. 2015 Jul-Aug;9(4):607-17. doi: 10.1016/j.jacl.2015.05.001. Epub 2015 May 14. PubMed PMID: 26228681.

3: Patel G, King A, Dutta S, Korb S, Wade JR, Foulds P, Sumeray M. Evaluation of the effects of the weak CYP3A inhibitors atorvastatin and ethinyl estradiol/norgestimate on lomitapide pharmacokinetics in healthy subjects. J Clin Pharmacol. 2015 Jun 26. doi: 10.1002/jcph.581. [Epub ahead of print] PubMed PMID: 26120010.

4: Gouni-Berthold I, Berthold HK. Mipomersen and lomitapide: Two new drugs for the treatment of homozygous familial hypercholesterolemia. Atheroscler Suppl. 2015 May;18:28-34. doi: 10.1016/j.atherosclerosissup.2015.02.005. PubMed PMID: 25936301.

5: Stefanutti C, Blom DJ, Averna MR, Meagher EA, Theron Hd, Marais AD, Hegele RA, Sirtori CR, Shah PK, Gaudet D, Vigna GB, Sachais BS, Di Giacomo S, du Plessis AM, Bloedon LT, Balser J, Rader DJ, Cuchel M; Phase 3 HoFH Lomitapide Study Investigators. The lipid-lowering effects of lomitapide are unaffected by adjunctive apheresis in patients with homozygous familial hypercholesterolaemia - a post-hoc analysis of a Phase 3, single-arm, open-label trial. Atherosclerosis. 2015 Jun;240(2):408-14. doi: 10.1016/j.atherosclerosis.2015.03.014. Epub 2015 Mar 14. PubMed PMID: 25897792; PubMed Central PMCID: PMC4573555.

6: Goulooze SC, Cohen AF, Rissmann R. Lomitapide. Br J Clin Pharmacol. 2015 Aug;80(2):179-81. doi: 10.1111/bcp.12612. Epub 2015 Jul 2. PubMed PMID: 25702706; PubMed Central PMCID: PMC4541964.

7: Alonso R, Mata P, Alonso Y Gregorio M, de Andrés R. [Homozygous familial hypercholesterolemia. First case in Spain treated with lomitapide, an inhibitor of the synthesis of lipoproteins with apolipoprotein B]. Med Clin (Barc). 2015 Sep 7;145(5):229-30. doi: 10.1016/j.medcli.2014.11.002. Epub 2014 Dec 24. Spanish. PubMed PMID: 25543225.

8: deGoma EM. Correction to "lomitapide for the management of homozygous familial hypercholesterolemia". Rev Cardiovasc Med. 2014;15(3):281-2. PubMed PMID: 25290735.

9: Catapano AL. Management of homozygous familial hypercholesterolaemia--unmet needs, updated recommendations, and clinical experience with the MTP inhibitor, lomitapide. Concluding comments. Atheroscler Suppl. 2014 Sep;15(2):52. doi: 10.1016/j.atherosclerosissup.2014.07.001. Review. PubMed PMID: 25257077.

10: Cuchel M, Blom DJ, Averna MR. Clinical experience of lomitapide therapy in patients with homozygous familial hypercholesterolaemia. Atheroscler Suppl. 2014 Sep;15(2):33-45. doi: 10.1016/j.atherosclerosissup.2014.07.005. Review. PubMed PMID: 25257075.

11: Sacks FM, Stanesa M, Hegele RA. Progression to hepatitis and fibrosis secondary to lomitapide use--reply. JAMA Intern Med. 2014 Sep;174(9):1522-3. doi: 10.1001/jamainternmed.2014.1528. PubMed PMID: 25178869.

12: Miyares MA. Progression to hepatitis and fibrosis secondary to lomitapide use: selecting the next course of action. JAMA Intern Med. 2014 Sep;174(9):1522. doi: 10.1001/jamainternmed.2014.1538. PubMed PMID: 25178868.

13: deGoma EM. Lomitapide for the management of homozygous familial hypercholesterolemia. Rev Cardiovasc Med. 2014;15(2):109-18. Review. PubMed PMID: 25051128.

14: Davis KA, Miyares MA. Lomitapide: A novel agent for the treatment of homozygous familial hypercholesterolemia. Am J Health Syst Pharm. 2014 Jun 15;71(12):1001-8. doi: 10.2146/ajhp130592. Review. PubMed PMID: 24865757.

15: Tuteja S, Duffy D, Dunbar RL, Movva R, Gadi R, Bloedon LT, Cuchel M. Pharmacokinetic interactions of the microsomal triglyceride transfer protein inhibitor, lomitapide, with drugs commonly used in the management of hypercholesterolemia. Pharmacotherapy. 2014 Mar;34(3):227-39. PubMed PMID: 24734312.

16: Rader DJ, Kastelein JJ. Lomitapide and mipomersen: two first-in-class drugs for reducing low-density lipoprotein cholesterol in patients with homozygous familial hypercholesterolemia. Circulation. 2014 Mar 4;129(9):1022-32. doi: 10.1161/CIRCULATIONAHA.113.001292. Review. PubMed PMID: 24589695.

17: Sacks FM, Stanesa M, Hegele RA. Severe hypertriglyceridemia with pancreatitis: thirteen years' treatment with lomitapide. JAMA Intern Med. 2014 Mar;174(3):443-7. doi: 10.1001/jamainternmed.2013.13309. PubMed PMID: 24366202.

18: Dixon DL, Sisson EM, Butler M, Higbea A, Muoio B, Turner B. Lomitapide and mipomersen: novel lipid-lowering agents for the management of familial hypercholesterolemia. J Cardiovasc Nurs. 2014 Sep-Oct;29(5):E7-E12. doi: 10.1097/JCN.0000000000000104. Review. PubMed PMID: 24231894.

19: Hussar DA, Ahmad A. Vilanterol trifenatate/fluticasone furoate, lomitapide mesylate, and mipomersen sodium. J Am Pharm Assoc (2003). 2013 Nov-Dec;53(6):662-70. doi: 10.1331/JAPhA.2013.13538. PubMed PMID: 24185435.

20: Darpo B, Ferber G, Zhou M, Sumeray M, Sager P. Lomitapide at supratherapeutic plasma levels does not prolong the Qtc interval--results from a TQT study with moxifloxacin and ketoconazole. Ann Noninvasive Electrocardiol. 2013 Nov;18(6):577-89. doi: 10.1111/anec.12103. Epub 2013 Sep 30. PubMed PMID: 24118671.