In the first study reported, patients with high cholesterol on stable doses of statins were treated with ISIS 301012 for five weeks. Patients who received 300 mg of ISIS 301012 in this study achieved a 51% reduction in LDL-cholesterol (LDL-C), a 42% reduction in total cholesterol, and a 41% reduction in triglycerides (TG) beyond the levels achieved with statins alone.
In addition, in these studies ISIS 301012 continued to demonstrate a strong safety profile – as a single agent and when co-administered with statins – in every dose cohort presented.
“These are quite remarkable results that are very encouraging for further development of ISIS 301012. These new data demonstrate pronounced lipid-lowering effects of ISIS 301012, both as a single agent and as an add-on to statin therapy. Further, the drug appears to have a positive safety profile,” according to John Kastelein, chairman, Department of Vascular Medicine at the Academic Medical Center, the Netherlands.
“A significant percentage of at-risk patients are simply not meeting LDL-C targets with current lipid-lowering drugs, so there is a growing need for therapies that can be added to statins to achieve additional reductions in atherogenic lipids,” added Dr Kastelein.
ISIS 301012 is also currently being evaluated in phase II dose escalation studies in patients with homozygous and heterozygous familial hypercholesterolemia (FH). Data from these trials are expected late in 2006 or early 2007. ISIS 301012 has been granted orphan drug status for the treatment of homozygous FH.