Lomitapide free base
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MedKoo CAT#: 319516

CAS#: 182431-12-5 (free base)

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.


Price and Availability

Size Price Shipping out time Quantity
5mg USD 45 2 Weeks
10mg USD 60 2 Weeks
25mg USD 90 2 Weeks
50mg USD 150 2 Weeks
100mg USD 250 2 Weeks
200mg USD 450 2 Weeks
500mg USD 650 2 Weeks
1g USD 950 2 Weeks
2g USD 1650 2 Weeks
5g USD 2950 2 Weeks
10g USD 4650 2 Weeks
20g USD 6950 2 Weeks
Inquire bulk and customized quantity

Pricing updated 2020-10-26. Prices are subject to change without notice.

Lomitapide free base, purity > 98%, is in stock. The same day shipping out after order is received.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 319516
Name: Lomitapide free base
CAS#: 182431-12-5 (free base)
Chemical Formula: C39H37F6N3O2
Exact Mass: 693.279
Molecular Weight: 693.73442
Elemental Analysis: C, 67.52; H, 5.38; F, 16.43; N, 6.06; O, 4.61


Related CAS #: 202914-84-9 (mesylate)   182431-12-5 (free base)    

Synonym: Lomitapide free base, 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

InChi Key: MBBCVAKAJPKAKM-UHFFFAOYSA-N

InChi Code: InChI=1S/C39H37F6N3O2/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/h1-6,9-18,28H,7-8,19-25H2,(H,46,50)(H,47,49)

SMILES Code: O=C(NCC(F)(F)F)C1(C2=C(C=CC=C2)C3=C1C=CC=C3)CCCCN4CCC(CC4)NC(C5=CC=CC=C5C6=CC=C(C=C6)C(F)(F)F)=O


Technical Data

Appearance:
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, not in water

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


References

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.