Lomitapide

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Chemical compound

title: "Lomitapide" type: doc version: 1 created: 2026-02-28 author: "Wikipedia contributors" status: active scope: public tags: ["benzamides", "biphenyls", "cyp3a4-inhibitors", "fluorenes", "lipid-lowering-agents", "organofluorides", "orphan-drugs", "ortho-phenylene-compounds", "piperidines", "trifluoroethyl-compounds", "4-(trifluoromethyl)phenyl-compounds"] description: "Chemical compound" topic_path: "general/benzamides" source: "https://en.wikipedia.org/wiki/Lomitapide" license: "CC BY-SA 4.0" wikipedia_page_id: 0 wikipedia_revision_id: 0

::summary Chemical compound ::

| Verifiedfields = changed | Watchedfields = changed | verifiedrevid = 444364270 | image = Lomitapide_skeletal.svg | image_class = skin-invert-image

| pronounce = | tradename = Juxtapid (US), Lojuxta (EU) | Drugs.com = | MedlinePlus = | licence_EU = yes | DailyMedID = Lomitapide | licence_US = Lomitapide | pregnancy_AU = | pregnancy_category = | routes_of_administration = By mouth | ATC_prefix = C10 | ATC_suffix = AX12 | ATC_supplemental =

| legal_AU = | legal_CA = | legal_UK = | legal_US = Rx-only | legal_US_comment = | legal_EU = Rx-only | legal_EU_comment = | legal_status =

| bioavailability = | protein_bound = | metabolism = | elimination_half-life = | excretion =

| index2_label = mesylate | IUPHAR_ligand = 7439 | CAS_number_Ref = | CAS_number = 182431-12-5 | CAS_number2 = 202914-84-9 | PubChem = 9853053 | PubChem2 = 11274333 | DrugBank_Ref = | DrugBank = DB08827 | DrugBank2 = DBSALT000110 | ChemSpiderID_Ref = | ChemSpiderID = 8028764 | ChemSpiderID2 = 9449335 | UNII_Ref = | UNII = 82KUB0583F | UNII2 = X4S83CP54E | KEGG_Ref = | KEGG = D09637 | KEGG2 = D09638 | ChEBI_Ref = | ChEBI = 72297 | ChEBI2 = 72299 | ChEMBL = 354541 | ChEMBL2 = 2105662 | synonyms = AEGR-773, BMS-201038

| IUPAC_name = N-(2,2,2-Trifluoroethyl)-9-[4-[4-[[[4'-(trifluoromethyl)[1,1'-biphenyl]2-yl]carbonyl]amino]-1-piperidinyl]butyl]-9H-fluoren-9-carboxamide | C=39 | H=37 | F=6 | N=3 | O=2 | smiles = FC(F)(F)c5ccc(cc5)-c1ccccc1C(=O)NC4CCN(CC4)CCCCC2(C(=O)NCC(F)(F)F)c3ccccc3-c6ccccc26 | StdInChI_Ref = | StdInChI = 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) | StdInChIKey_Ref = | StdInChIKey = MBBCVAKAJPKAKM-UHFFFAOYSA-N

Lomitapide , sold under the brand name Juxtapid in the US and **Lojuxta ** in the EU, is a medication used as a lipid-lowering agent for the treatment of familial hypercholesterolemia, developed by Aegerion Pharmaceuticals.{{cite journal | author = H. Spreitzer | date = 12 March 2007 | title = Neue Wirkstoffe – BMS-201038 | journal = Österreichische Apothekerzeitung | issue = 6/2007 | pages = 268 | language = German

The US Food and Drug Administration (FDA) approved lomitapide in December 2012, as an orphan drug to reduce LDL cholesterol, total cholesterol, apolipoprotein B, and non-high-density lipoprotein (non-HDL) cholesterol in people with homozygous familial hypercholesterolemia (HoFH).

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.

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.

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)."

Side effects

In a Phase III study, lomitapide led to elevated aminotransferase levels and fat accumulation in the liver.

References

References

  1. "Juxtapid- lomitapide mesylate capsule".
  2. (July 2008). "Measures of obesity and outcomes after myocardial infarction". Circulation.
  3. (9 November 2008). "Aegerion Pharmaceuticals, Inc. Announces AEGR-733 Phase II Data Demonstrates Significant Lowering of LDL Cholesterol with Promising Hepatic Safety Profile". Business Wire.
  4. "FDA approves new orphan drug for rare cholesterol disorder". U.S. Food and Drug Administration.
  5. (3 September 2013). "Lojuxta EPAR".
  6. (January 2007). "Inhibition of microsomal triglyceride transfer protein in familial hypercholesterolemia". The New England Journal of Medicine.
  7. (26 December 2012). "FDA Approves Juxtapid for Homozygous Familial Hypercholesteolemia".
  8. (24 December 2012). "FDA Approves Aegerion Pharmaceuticals' Juxtapid (lomitapide) Capsules for Homozygous Familial Hypercholesterolemia (HoFH)". Aegerion Pharmaceuticals.

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benzamidesbiphenylscyp3a4-inhibitorsfluoreneslipid-lowering-agentsorganofluoridesorphan-drugsortho-phenylene-compoundspiperidinestrifluoroethyl-compounds4-(trifluoromethyl)phenyl-compounds