Surface Logix presents positive trial data on dyslipidemia
drug candidate that is being developed for the treatment of
abnormal levels of lipids in the bloodstream - a condition that
affects approximately 10 per cent of the global population.
The drug candidate SLx-4090, is a novel Microsomal Triglyceride Transfer Protein (MTP) inhibitor designed to act in the gastrointestinal (GI) tract to prevent the transport of fats through the intestinal wall.
Intestinal selectivity allows activity against fat uptake while avoiding toxicity at other sites of MTP expression including the liver, heart, testis, ovary, and eye.
Increasing prevalence and medical need for lipid-modifying drugs has been observed in obese patients and patients with type 2 diabetes, as a high proportion of type 2 diabetic patients have abnormal concentrations of lipoproteins.
In the US, Japan and Europe, it is estimated that there are more than 240m people with abnormal lipoprotein levels. Of these, more than 55m are estimated to have low high-density lipoprotein (HDL) and/or high triglyceride levels.
Results of the latest drug trial were presented at the American Heart Association's Scientific Sessions 2006 conference being held November 12 - 15 in Chicago, Illinois.
Dr. William Prince, Chief Development Officer at Surface Logix, detailed a Phase 1 study, in which subjects received single oral doses of either SLx-4090 or placebo.
Nine dose levels were included and subjects were monitored for adverse events. Pharmacokinetic and pharmacodynamic sampling was performed out to 24 hours post dose to measure plasma lipid and lipoprotein concentrations after dietary consumption.
The initial Phase 1 trial indicated that SLx-4090 was well tolerated, with no serious adverse events reported, and demonstrated a significant impact (>60 per cent) on lowering triglyceride levels compared to placebo.
"It is exciting that this novel compound performed so well in this Phase 1 study," said Prince.
"Consistent with our preclinical results, no drug was detected in the plasma at doses up to 800mg and no adverse events occurred that were distinguishable from placebo. This is particularly notable, as it has historically been difficult to design an MTP inhibitor that acts selectively in the gastrointestinal tract with no adverse impact on liver or liver function."
Based on the results of this study, Surface Logix intend to advance SLx-4090 into a Phase 1b repeat-dose study, due to be completed by December 2006,
"We will commence Phase 2a studies directed at patients with dyslipidemia complicated by high triglyceride levels early in 2007," said Jim Mahoney, President and Chief Executive Officer of Surface Logix.
"Based on the impact of SLx-4090 in lowering LDL-cholesterol and raising HDL-cholesterol in preclinical studies, we strongly believe that a safe, efficacious, enterocyte-specific MTP inhibitor could play a significant role in the marketplace by providing clinicians another route to manage lipid disorders for patients that do not respond to currently available treatment options."
Surface Logix added they were also exploring the use of SLx-4090 in other metabolic disorders, including obesity and diabetes.