Lomitapide (AEGR-733; BMS-201038) mesylate is an orally active microsomal triglyceride transfer protein ( MTP ) inhibitor and a selective mTORC1 inhibitor with lipid-lowering activity and BBB permeability. Lomitapide mesylate significantly reduces plasma LDL levels by blocking the assembly and secretion of very-low-density lipoprotein ( VLDL ). Lomitapide mesylate inhibits mTORC1 in an ATP-dependent manner, thereby inducing AMPK -independent autophagic cell death and suppressing cancer cell growth and apoptosis . Lomitapide mesylate also enhances tumor infiltration of CD8 + T cells. In addition, Lomitapide mesylate inhibits HDAC , improves endothelial function, effectively alleviates vascular inflammation and oxidative stress, and exerts neuroprotective effects in a cerebral ischemia/reperfusion injury model. Lomitapide mesylate can be used in research on related diseases such as colorectal cancer , breast cancer , melanoma, ischemic stroke, and familial hypercholesterolemia.
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