Lomitapide

Lomitapide
Names
Trade namesJuxtapid (US), Lojuxta (EU)
Other namesAEGR-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
Clinical data
Drug classMicrosomal triglyceride transfer protein (MTTP) inhibitor[1]
Main usesHomozygous familial hypercholesterolemia (HoFH)[1]
Side effectsDiarrhea, nausea, heartburn, abdominal pain, increased intestinal gas[1]
WHO AWaReUnlinkedWikibase error: ⧼unlinkedwikibase-error-statements-entity-not-set⧽
Routes of
use		By mouth (capsules)
External links
AHFS/Drugs.comMonograph
Legal
License data
Legal status
Chemical and physical data
FormulaC39H37F6N3O2
Molar mass693.734 g·mol−1
3D model (JSmol)
SMILES
  • FC(F)(F)c5ccc(cc5)-c1ccccc1C(=O)NC4CCN(CC4)CCCCC2(C(=O)NCC(F)(F)F)c3ccccc3-c6ccccc26
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) ☒N
  • Key:MBBCVAKAJPKAKM-UHFFFAOYSA-N ☒N

Lomitapide , sold under the brand name Juxtapid and Lojuxta , is a medication used to treat homozygous familial hypercholesterolemia (HoFH).[1] It is used together with diet and other measures.[1] Effects related to life expectancy and heart disease are unclear.[3] It is taken by mouth.[1]

Common side effects include diarrhea, nausea, heartburn, abdominal pain, and increased intestinal gas.[1] Serious side effects may include liver problems and fat soluble vitamin deficiency.[1] Use in pregnancy may harm the baby.[4] It works by blocking microsomal triglyceride transfer protein.[1]

Lomitapide was approved for medical use in the United States in 2012 and Europe in 2013.[3][1] In the United Kingdom a dose of 20 mg per day costs the NHS about £17,800 for 4 weeks as of 2021.[4] This amount in the United States costs about 48,600 USD.[5]

Medical uses

Dosage

It is taken at a dose of 5 to 60 mg per day.[4]

Side effects

In a Phase III study, lomitapide led to elevated aminotransferase levels and fat accumulation in the liver.[6]

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.[6]

On 24 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)."[7][8]

References

  1. 1 2 3 4 5 6 7 8 9 10 11 "Lojuxta EPAR". European Medicines Agency (EMA). Archived from the original on 30 December 2020. Retrieved 27 January 2021.
  2. ↑ "Juxtapid- lomitapide mesylate capsule". DailyMed. Archived from the original on 20 January 2021. Retrieved 27 January 2021.
  3. 1 2 "Lomitapide Monograph for Professionals". Drugs.com. Archived from the original on 22 January 2021. Retrieved 24 November 2021.
  4. 1 2 3 BNF 81: March-September 2021. BMJ Group and the Pharmaceutical Press. 2021. p. 223. ISBN 978-0857114105.
  5. ↑ "Juxtapid Prices, Coupons & Patient Assistance Programs". Drugs.com. Archived from the original on 14 March 2016. Retrieved 24 November 2021.
  6. 1 2 Cuchel M, Bloedon LT, Szapary PO, Kolansky DM, Wolfe ML, Sarkis A, et al. (January 2007). "Inhibition of microsomal triglyceride transfer protein in familial hypercholesterolemia". The New England Journal of Medicine. 356 (2): 148–56. doi:10.1056/NEJMoa061189. PMID 17215532.
  7. ↑ "FDA Approves Juxtapid for Homozygous Familial Hypercholesteolemia". 26 December 2012. Archived from the original on 29 December 2012. Retrieved 1 January 2013.
  8. ↑ "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.
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