期刊
CURRENT OPINION IN LIPIDOLOGY
卷 24, 期 3, 页码 246-250出版社
LIPPINCOTT WILLIAMS & WILKINS
DOI: 10.1097/MOL.0b013e32836139df
关键词
homozygous familial hypercholesterolemia; lomitapide; microsomal triglyceride transfer protein; MTP inhibitors
资金
- Aegerion Pharmaceuticals
Purpose of review Microsomal triglyceride transfer protein (MTP) is a key protein in the secretion of apolipoprotein B-containing lipoproteins. Its pharmacological inhibition is associated with a decrease in LDL cholesterol (LDL-C) and triglycerides. However, the clinical use of MTP inhibitors has been uncertain because of the gastrointestinal adverse events and the increase in liver fat content observed during their administration. Recent findings Lomitapide, a systemic MTP inhibitor, significantly reduces LDL-C in homozygous familial hypercholesterolemia (hoFH) when administered concurrently with other lipid-lowering therapies, including apheresis. Its lipid-lowering effect is additive to that of existing drugs. In the presence of an up-titration regiment and low-fat diet, lomitapide is generally well tolerated and liver fat accumulation stabilizes after the initial increase. Elevation of alanine aminotranferase levels greater than 3 times the upper limit of normal can be managed successfully with temporary dose reduction. Drug-drug interaction studies show that concomitant treatment of lomitapide with other lipid-lowering drugs is generally safe. Based on these findings, lomitapide was recently approved for the treatment of hoFH as add-on therapy. Summary MTP inhibition is a valuable therapeutic approach for hoFH. Long-term safety consequences of liver fat accumulation will need to be assessed.
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