lomitapide

Ligand id: 7439

Name: lomitapide

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Structure and Physico-chemical Properties

2D Structure
Calculated Physico-chemical Properties
Hydrogen bond acceptors 5
Hydrogen bond donors 2
Rotatable bonds 14
Topological polar surface area 61.44
Molecular weight 693.28
XLogP 13.87
No. Lipinski's rules broken 2

Molecular properties generated using the CDK

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).
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