SLX-4090 – AN ENTEROCYTE-SPECIFIC MICROSOMAL TRIGLYCERIDE TRANSFER PROTEIN INHIBITOR

SLx-4090 is a first-in-class inhibitor of enterocytic microsomal triglyceride transfer protein (MTP), designed to treat metabolic and cardiovascular diseases while overcoming the toxicity issues inherent in systemic MTP inhibition. Taken orally, SLx-4090 targets MTP only in enterocytes of the small intestine, thus blocking a key step in the adsorption of dietary triglycerides and cholesterol into the lymphatic circulation. Because SLx-4090 does not enter the systemic circulation, it avoids the mechanistic toxicities of systemic MTP inhibition, such as fatty liver, seen with other MTP inhibitors.

To date, SLx-4090 has been evaluated in 3 clinical trials. Phase 1a and Phase 1b studies established an excellent profile in terms of enteric pK, safety, and dose response. Phase 2a studies demonstrated efficacy in lowering plasma levels of postprandial triglycerides and LDL-cholesterol as well as demonstrating trends in weight loss and diabetes markers. A 90 day Phase 2b trial in dyslipidemia, obesity and diabetes was initiated in early 2009 and is currently enrolling.