Lomitapide

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Lomitapide
Clinical data
Trade namesJuxtapid (US), Lojuxta (EU)
Other namesAEGR-773, BMS-201038
License data
Routes of
administration		By mouth
ATC code
Legal status
Legal status
Identifiers
  • N-(2,2,2-Trifluoroethyl)-9-[4-[4-[[[4'-(trifluoromethyl)[1,1'-biphenyl]2-yl]carbonyl]amino]-1-piperidinyl]butyl]-9H-fluoren-9-carboxamide
JSmol)
  • FC(F)(F)c5ccc(cc5)-c1ccccc1C(=O)NC4CCN(CC4)CCCCC2(C(=O)NCC(F)(F)F)c3ccccc3-c6ccccc26
  • 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) ☒N
  • Key:MBBCVAKAJPKAKM-UHFFFAOYSA-N ☒N
 ☒NcheckY (what is this?)  (verify)

Lomitapide , sold under the brand name Juxtapid in the US and Lojuxta in the EU, is a medication used as a

clinical trials as single treatment and in combinations with atorvastatin, ezetimibe and fenofibrate.[4][5]

The US Food and Drug Administration (FDA) approved lomitapide in December 2012, as an

non-high-density lipoprotein (non-HDL) cholesterol in people with homozygous familial hypercholesterolemia (HoFH).[6]

In July 2013, the European Commission approved lomitapide as an adjunct to a low-fat diet and other lipid-lowering medicinal products with or without low density lipoprotein (LDL) apheresis in adults with HoFH.[2]

Mechanism of action

Lomitapide inhibits the microsomal triglyceride transfer protein (MTP or MTTP) which is necessary for very low-density lipoprotein (VLDL) assembly and secretion in the liver.[3][7]

In December 2012, drug manufacturer Aegerion announced they had been approved by the FDA to as "an adjunct to a low-fat diet and other lipid-lowering treatments...in patients with homozygous familial hypercholesterolemia (HoFH)."[8][9]

Side effects

In a

aminotransferase levels and fat accumulation in the liver.[7]

References

  1. ^ "Juxtapid- lomitapide mesylate capsule". DailyMed. Retrieved 27 January 2021.
  2. ^ a b "Lojuxta EPAR". European Medicines Agency (EMA). Retrieved 27 January 2021.
  3. ^ a b H. Spreitzer (12 March 2007). "Neue Wirkstoffe – BMS-201038". Österreichische Apothekerzeitung (in German) (6/2007): 268.
  4. PMID 18663098
    .
  5. ^ "Aegerion Pharmaceuticals, Inc. Announces AEGR-733 Phase II Data Demonstrates Significant Lowering of LDL Cholesterol with Promising Hepatic Safety Profile". Business Wire. 9 November 2008. Archived from the original on 2012-02-29.
  6. ^ "FDA approves new orphan drug for rare cholesterol disorder". U.S. Food and Drug Administration. Archived from the original on 28 January 2013.
  7. ^
    PMID 17215532
    .
  8. ^ "FDA Approves Juxtapid for Homozygous Familial Hypercholesteolemia". 26 December 2012. Archived from the original on 29 December 2012. Retrieved 1 January 2013.
  9. ^ "FDA Approves Aegerion Pharmaceuticals' Juxtapid (lomitapide) Capsules for Homozygous Familial Hypercholesterolemia (HoFH)" (Press release). Aegerion Pharmaceuticals. 24 December 2012. Archived from the original on 22 September 2016. Retrieved 1 January 2013.

External links

  • "Lomitapide". Drug Information Portal. U.S. National Library of Medicine.
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