Scientists have discovered a molecule that is highly active in inhibiting the intestinal absorption of lipids, making it an excellent candidate for fighting dyslipidemia and associated cardiac events, especially in diabetics. According to WHO, about 230 million people suffer from Type II diabetes worldwide, with estimations projecting these figures will rise to 400 million by 2025. Around 40% of type 2 diabetes patients suffer from dyslipidemia, including hypertriglyceridemia.

Arteria SA, today announced that it has obtained highly promising results in preclinical non-regulatory studies for its AP-5258 molecule, an inhibitor of the CD36 receptor and that it intends to start regulatory studies.

During pre-clinical in vivo tests using a very substantial dose of AP-5258 molecule, the inhibitor demonstrated high intestinal activity, blocking the transfer of postprandial triglycerides.

Taken orally the molecule potentially reduces postprandial hypertriglyceridemia (high blood fat levels of triglycerides after eating) and protects patients from diabetic dyslipidemia.

After consuming food, the body produces postprandial plasmatic triglycerides, known as the most powerful markers of cardiac events, particularly amongst diabetic women. 19.2% of patients who suffer from both hyperglycemia (high blood sugar) and hypertriglyceridemia (high blood fat) suffer from coronary disease.

Few therapies exist to tackle these conditions and those available, i.e. fibrates and ezetimibe, are subjects of controversy regarding their side effects and efficacy. Drugs in an advanced stage of development are based on targets that were discovered a long time ago and seem to have significant side effects, especially on the liver.

Recently, the CD36 receptor was discovered, which is a new and promising therapeutic target. Researchers have established that the expression of the CD36 receptor is associated with metabolic diseases such as Type II diabetes or atherogenesis. There are only few companies worldwide who possess a molecule that targets the CD36 receptor, one of them being Arteria, whose AP-5258 is administered orally, is non-toxic and therefore at an advanced development stage.

Professor Gérard Marguerie, chief scientific officer at Arteria explains:

“Animal pharmacology and toxicity tests on our AP-5258 molecule are extremely promising. We have been able to link this molecule with a target, the CD36 receptor, identify its mechanism of action and determine the measurable biological parameter, postprandial triglycerides. The fact that we have identified the intestine as the action site of the molecule will enable us to devise and implement an accelerated and simplified development program.”

According to Global Market Research in 2010, the market was valued at $9 billion in 2009 with a projected growth rate of 6% in 2016.

Jean-Louis Falco, chairman and chief executive officer of Arteria commented:

“The entry of our molecule AP-5258 into the development phase is a great endorsement of our therapeutic focus. We are now looking for partnering agreements to accelerate the development process for this molecule and for other patented entities in our product portfolio.”

Written by Petra Rattue