Dose-Dependent Reductions in LDL-C with ISIS 301012, An Antisense Inhibitor of Apolipoprotein B

摘要

ISIS 301012 is an antisense drug that inhibits synthesis of human apolipoprotein B (apoB), the principal apolipoprotein of LDL-C and its metabolic precursors, VLDL and IDL. A compelling activity profile has emerged in Phase 1 and Phase 2 studies in which ISIS 301012 has been shown to promote dose-dependent and durable reductions in circulating concentrations of apoB and LDL-C as well as other atherogeriic lipids and lipoproteins. At this congress, we presented data from two Phase 2 dose-ranging studies in which ISIS 301012 was administered as monotherapy or as add-on to statin therapy in subjects with primary hypercholesterolemia. Results of an open-label Phase 2 study in subjects with homozygous familial hypercholesterolemia (FH) were also presented.