Dezima's CETP Inhibitor For Dyslipidemia Shows Positive Results in Phase 2 Trial
By C. Rajan, contributing writer
Dutch biotech company, Dezima Pharma, last week announced that it received very positive results for its cholesterol drug TA-8995, in its Phase 2b TULIP clinical trial. The drug candidate, TA-8995, was tested both as monotherapy and in combination with statins for treating dyslipidemia.
TA-8995 is a novel Cholesteryl Ester Transfer Protein (CETP) inhibitor, which works by lowering levels of LDL ('bad cholesterol') while increasing the levels of the preferred HDL.
The TULIP Phase 2 trial was a randomized, double-blind, placebo controlled study, conducted with 364 patients across Denmark and the Netherlands. The study investigated the effects of TA-8995 on a wide range of established cardiovascular disease biomarkers, over a dosing period of three months.
The drug gave excellent results in meeting the primary endpoint, which was lowering LDL and raising HDL, as well as demonstrating strong clinical effects on cholesterol efflux and lipoprotein. TA-8995 also showed excellent efficacy and safety profile, along with favorable pharmacokinetics.
John Kastelein, CSO and co-founder of Dezima said, "The results emphasize that TA-8995 robustly lowers all atherogenic lipoproteins, LDL-C, the entity of non HDL-C, apoB as well as Lp(a), compatible with very significant reductions of cardiovascular risk."
Last year, Dezima licensed the CETP inhibitor program from Mitsubishi Tanabe Pharma Corporation (MTPC) with TA-8995 as the lead product. Subsequently, the company raised $18.6 million in venture and loan financing to help develop the CETP program and push the lead product through the Phase 2 study.
CETP inhibitors are in development by several major pharma companies as cholesterol drugs. Dezima's TA-8995 so far appears to be the most potent CETP inhibitor, and puts it in competition with the other leading CETP inhibitors, including Eli Lilly's Evacetrapib and Merck's Anacetrapib.
Rob de Ree, CEO of Dezima said, "These results are clearly very exciting. Compared to other CETP inhibitors, TA-8995 combines the highest levels of efficacy seen on lipid parameters with a 20-fold lower dose. Combined with the excellent safety and favorable pharmacokinetic profile this positions TA-8995 as the best-in-class CETP inhibitor as we move towards Phase 3."
Elevated levels of lipoproteins lead to heart conditions, such as myocardial infarction, aortic stenosis, coronary heart disease, and stroke. CETP facilitates the transfer of cholesterol from HDL to other lipoproteins including LDL, in exchange for triglycerides. Reduced activity of CETP by pharmaceutical means results in increased HDL and decreased LDL levels. This makes CETP inhibitors an attractive treatment option for dyslipidemic conditions.
Dyslipidemia is a modifiable risk factor for cardiovascular disease and is marked by abnormal serum lipid levels. The current treatment options leave room for improvement, as about 60 percent of patients experience a cardiovascular event even after treatment. According to Dezima, the market for dyslipidemic drugs was over $25 billion in 2010.