mipomersen sodium) Injection 200 mg/mL KYNAMRO is an oligonucleotide inhibitor of
apolipoprotein B-100 synthesis indicated as an adjunct to lipid-lowering medications and diet to reduce low density lipoprotein-cholesterol (LDL-C), apolipoprotein B (apo B), total cholesterol (TC), and non-high density lipoprotein-cholesterol (non-HDL-C) in patients with homozygous familial hypercholesterolemia (HoFH).
VLDL is assembled on
apolipoprotein B-100 (apoB100) and comprises 50% TG, 20% cholesterol esters, 15% phospholipids and 15% protein.
LDL contains a core of hydrophobic lipid, mostly cholesteryl ester, a shell of phospholipids, and single molecule of the large protein
apolipoprotein B-100 (apo B).
We investigated the potential role and mechanism of action of an indole-based compound, indole-3-carbinol (I3C), on
apolipoprotein B-100 (apoB) production using HepG2 cells.
7 Total cholesterol, mg/dl 194 [+ or -] 47 189 [+ or -] 57 LDL-cholesterol, mg/dl 125 (64-1006) 119 (61-1042) HDL-cholesterol, mg/dl 41 [+ or -] 6 41 [+ or -] 9 Triglyceride, mg/dl 132(43-331) 139 (67-466) Lipoprotein (a), mg/dl 35 (10-174) 31 (2-112) Apolipoprotein A-1, mg/dl 124 [+ or -] 27 129 [+ or -] 34
Apolipoprotein B-100, mg/dl 116(52-222) 107 (63-161) Homocysteine, [micro]mol/l 13.
Mipomersen, formerly ISIS 301012, is a lipid-lowering drug targeting
apolipoprotein B-100.
The analysis also showed that the ratio of total cholesterol to HDL cholesterol was at least as good for predicting the risk of the ocurrence of cardiovascular events as was the ratio of
apolipoprotein B-100 to HDL lipoprotein cholesterol (JAMA 2005;294:326-33).
There were no significant changes in serum total cholesterol, triglyceride, LDL-cholesterol, HDL-cholesterol or
apolipoprotein B-100 concentrations with black tea ingestion.
Familial defective
apolipoprotein B-100 (FDB) and familial hypercholesterolemia (FH) are common causes of monogenic primary hypercholesterolemia.
Another subunit of lipoprotein(a), called
apolipoprotein B-100, already has been fingered as a culprit in atherosclerosis (SN: 2/7/87, p.
Isis Pharmaceutical Compound: ISIS 301012, a second-generation antisense inhibitor of
apolipoprotein B-100 (ApoB), which has demonstrated potent, prolonged dose-dependant reduction of ApoB, cholesterol, low- density lipoprotein (LDL-C) and very low-density lipoprotein (VLDL) in Phase 1 trials.
Complete deficiency of the low-density lipoprotein receptor is associated with increased
apolipoprotein B-100 production.