Lomitapide

For research use only. Not for therapeutic Use.

  • CAT Number: A000126
  • CAS Number: 182431-12-5
  • Molecular Formula: C₃₉H₃₇F₆N₃O₂
  • Molecular Weight: 693.72
  • Purity: ≥95%
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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.


Catalog Number A000126
CAS Number 182431-12-5
Synonyms

182431-12-5; Juxtapid; Lojuxta; BMS-201038; AEGR 733

Molecular Formula C₃₉H₃₇F₆N₃O₂
Purity ≥95%
Target MTP inhibitor
Storage -20°C
InChI 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)
InChIKey MBBCVAKAJPKAKM-UHFFFAOYSA-N
SMILES C1CN(CCC1NC(=O)C2=CC=CC=C2C3=CC=C(C=C3)C(F)(F)F)CCCCC4(C5=CC=CC=C5C6=CC=CC=C64)C(=O)NCC(F)(F)F
Reference

1: Bruckert E, Gallo A. Is lomitapide a life-saving drug in homozygous familial
hypercholesterolemia. Eur J Prev Cardiol. 2017 Jan 1:2047487317734387. doi:
10.1177/2047487317734387. [Epub ahead of print] PubMed PMID: 28952803.
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2: Leipold R, Raal F, Ishak J, Hovingh K, Phillips H. The effect of lomitapide on
cardiovascular outcome measures in homozygous familial hypercholesterolemia: A
modelling analysis. Eur J Prev Cardiol. 2017 Jan 1:2047487317730473. doi:
10.1177/2047487317730473. [Epub ahead of print] PubMed PMID: 28925748.

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3: Blom DJ, Averna MR, Meagher EA, du Toit Theron H, Sirtori CR, Hegele RA, Shah
PK, Gaudet D, Stefanutti C, Vigna GB, Larrey D, Bloedon LT, Foulds P, Rader DJ,
Cuchel M. Long-Term Efficacy and Safety of the Microsomal Triglyceride Transfer
Protein Inhibitor Lomitapide in Patients With Homozygous Familial
Hypercholesterolemia. Circulation. 2017 Jul 18;136(3):332-335. doi:
10.1161/CIRCULATIONAHA.117.028208. PubMed PMID: 28716835.
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4: Berberich AJ, Hegele RA. Lomitapide for the treatment of hypercholesterolemia.
Expert Opin Pharmacother. 2017 Aug;18(12):1261-1268. doi:
10.1080/14656566.2017.1340941. Epub 2017 Jul 30. Review. PubMed PMID: 28598687.

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5: Won JI, Zhang J, Tecson KM, McCullough PA. Balancing Low-density Lipoprotein
Cholesterol Reduction and Hepatotoxicity With Lomitapide Mesylate and Mipomersen
in Patients With Homozygous Familial Hypercholesterolemia. Rev Cardiovasc Med.
2017;18(1):21-28. PubMed PMID: 28509890.
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6: D/’Erasmo L, Cefalù AB, Noto D, Giammanco A, Averna M, Pintus P, Medde P, Vigna
GB, Sirtori C, Calabresi L, Pavanello C, Bucci M, Sabbà C, Suppressa P, Natale F,
Calabrò P, Sampietro T, Bigazzi F, Sbrana F, Bonomo K, Sileo F, Arca M. Efficacy
of Lomitapide in the Treatment of Familial Homozygous Hypercholesterolemia:
Results of a Real-World Clinical Experience in Italy. Adv Ther. 2017
May;34(5):1200-1210. doi: 10.1007/s12325-017-0531-x. Epub 2017 Apr 21. PubMed
PMID: 28432645.
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7: Liu X, Men P, Wang Y, Zhai S, Zhao Z, Liu G. Efficacy and Safety of Lomitapide
in Hypercholesterolemia. Am J Cardiovasc Drugs. 2017 Aug;17(4):299-309. doi:
10.1007/s40256-017-0214-7. Review. PubMed PMID: 28255870.

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8: Yoshida H. A First-in-Class Drug, Lomitapide, Tailored to Patients with
Homozygous Familial Hypercholesterolemia is Just about Meeting with Good News to
Them. J Atheroscler Thromb. 2017 Apr 3;24(4):390-392. doi: 10.5551/jat.ED069.
Epub 2017 Feb 24. PubMed PMID: 28239069; PubMed Central PMCID: PMC5392476.
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9: Harada-Shiba M, Ikewaki K, Nohara A, Otsubo Y, Yanagi K, Yoshida M, Chang Q,
Foulds P. Efficacy and Safety of Lomitapide in Japanese Patients with Homozygous
Familial Hypercholesterolemia. J Atheroscler Thromb. 2017 Apr 3;24(4):402-411.
doi: 10.5551/jat.38216. Epub 2017 Feb 2. PubMed PMID: 28154305; PubMed Central
PMCID: PMC5392478.
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10: Brahm AJ, Hegele RA. Lomitapide for the treatment of hypertriglyceridemia.
Expert Opin Investig Drugs. 2016 Dec;25(12):1457-1463. Epub 2016 Nov 9. Review.
PubMed PMID: 27785928.

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