Synonyms: AEGR-733 | BMS-201038 | Juxtapid® | Lojuxta®
lomitapide is an approved drug (FDA (2012), EMA (2013))
Compound class:
Synthetic organic
Comment: Lomitapide is a lipid-lowering agent for the treatment of familial hypercholesterolemia.
Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖View more information in the IUPHAR Pharmacology Education Project: lomitapide |
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No information available. |
Summary of Clinical Use |
Approved to lower total cholesterol in patients with homozygous familial hypercholesterolemia (HoFH). Clinical formulations contain lomitapide mesylate (PubChem CID 11274333). |
Mechanism Of Action and Pharmacodynamic Effects |
Mechanistically lomatipide inhibits microsomal triglyceride transfer protein (MTTP, P55157). MTTP is required for the transport of triglyceride, cholesteryl ester, and phospholipid between phospholipid surfaces in the endoplasmic reticulum and this activity is required for the synthesis of apolipoprotein B (apo B). Lomatipide-induced reduction of apoB reduces VLDL and chylomicron formation and thus reduces LDL-cholesterol levels. Note that the microsomal triglyceride transfer protein is a heterodimer, composed of MTTP and protein disulfide isomerase (PDI, of which there are many isoforms). |
External links |
For extended ADME data see the following: Electronic Medicines Compendium (eMC) Drugs.com European Medicines Agency (EMA) |