Arteria to Carry Out Regulatory Preclinical Studies in the Field of Postprandial Hypertriglyceridemia Following Excellent Initial Results

Arteria SA has announced that it has obtained highly promising results in preclinical non-regulatory studies for its AP-5258 molecule, an inhibitor of the CD36 receptor. It also announces its intention to begin regulatory studies.

In pre-clinical in vivo tests carried out, the inhibitor showed high intestinal activity, blocking the transfer of postprandial triglycerides, with a very significant dose effect.

The molecule, administered orally, has the potential to reduce postprandial hypertriglyceridemia and to protect patients from diabetic dyslipidemia.

Postprandial plasmatic triglycerides are produced after consuming food. They are recognized as one of the most powerful markers of cardiac events, especially among diabetic women.

The prevalence of coronary illness is 19.2 per cent in patients who have both hyperglycemia (high blood sugar) and hypertriglyceridemia (high blood fat). Doctors have few weapons to combat these conditions.

Those on the market are few (eg fibrates and ezetimibe) and are the subject of controversy over side effects and efficacy.

Drugs in an advanced stage of development are based on targets identified many years ago and appear to have significant side effects, particularly on the liver.

A new and promising therapeutic target has emerged recently - the CD36 receptor. Scientists have demonstrated that the expression of the CD36 receptor is linked to associated metabolic diseases such as Type II diabetes or atherogenesis.

Arteria is one of the few companies in the world to have a molecule that targets the CD36 receptor, is administered orally, is non-toxic and is at such an advanced stage of development.

“Animal pharmacology and toxicity tests on our AP-5258 molecule are extremely promising,” said professor Gérard Marguerie, chief scientific officer at Arteria.

Marguerie continued, “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.”

There are some 230 million Type II diabetes patients worldwide (400 million by 2025 according to WHO). Around 40 per cent of these suffer from dyslipidemia, including hypertriglyceridemia.

The market was valued at USD nine billion in 2009 with a projected growth rate of six per cent in 2016 (source: Global Market Research 2010).

“The entry of our molecule AP-5258 into the development phase is a great endorsement of our therapeutic focus,” said Jean-Louis Falco, chairman and chief executive officer of Arteria.

Falco continued, “We are now looking for partnering agreements to accelerate the development process for this molecule and for other patented entities in our product portfolio.”