Microsomal transfer protein inhibition in humans.

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