Completion of the tolerance study with single doses of CER-209
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No problem of safety and tolerability related to the drug candidate
The pharmacokinetics observed supports a once-daily CER-209
The study of tolerance to multiple doses is now ready to be launched
Toulouse, FRANCE, Ann Arbor, USA, 7 June 2017, 19: 00 Cerenis Therapeutics (FR0012616852 CEREN Eligible PEA PME), a biopharmaceutical company dedicated to the discovery and development of innovative therapies based on the metabolism of lipids for the treatment of cardiovascular and metabolic diseases, today announces positive results of Phase I of CER-209 in a single dose in the treatment of Hepatitis Fat Non-Alcoholic (NAFLD) and nonalcoholic steatohepatitis (NASH).
The objective of the tolerance study with single doses conducted in the United States was to evaluate the safety, tolerability and the pharmacokinetic profile of CER-209 when taken orally as a single dose. Increasing doses of 1, 3 ,10 and 30 mg have been tested on 24 subjects, treated in 4 cohorts of 6 patients. In each cohort, 4 subjects were treated with the drug candidate to the study, while the other 2 received placebo.
“The positive results of the tolerability study after intake of single doses allow us to proceed to the next step in the clinical development of CER-209, namely, the study of safety and tolerability after taking multiple doses. In the absence of solutions of treatment of NAFLD and NASH, CER-209 could play a major role in the treatment of fatty liver disease and atherosclerosis. The major advantage of CER-209 in the treatment of NAFLD and NASH lies in its ability to promote the recognition of HDL and the elimination of lipids by the liver, via the activation of the natural pathways of metabolic through the receptor P2Y13. In addition, the confirmation of the pharmacokinetic profile of CER-209, which allows a once-daily oral, is a very good news for the adoption of the treatment by patients, ” says Dr. Jean-Louis Is the founder and ceo of Cerenis.
CER-209, an agonist of the receptor P2Y13, is well suited to the treatment of NAFLD and NASH.
The NAFLD, a precursor of NASH, is a major health problem, since this was now seen as the disease of the liver the most common in the western world, impacting at a global level for nearly 30% of the population1. Epidemiological studies demonstrate that cardiovascular risk is increased in patients with steatohepatitis, and cardiovascular diseases combined represent the leading causes of death in patients with a steatosis of the foie1,2.
1 Source: World Journal of Hepatology
Frankish S. M. et al., Journal of Hepatology, 2016, vol. 65, 425-443
2 World J Gastroenterol 2015 June 14; 21(22): 6820-6834
In these preclinical models, CER-209 causes a marked reduction in steatohepatitis as determined by a reduction destaux of cholesterol, triglycerides and fatty acids in the liver compared to placebo. In addition, CER-209 induces diminutionsimportantes liver enzymes (ALT and AST) in the plasma. These effects suggest the restoration of the integrity of the liver and show the great potential of CER-209 for the treatment of liver diseases such as NAFLD and NASH, while reducing the risk of cardiovascular disease associated with it. CER-209, which exerts its beneficial effect on steatosis of the liver via a specific action on the route of elimination of cholesterol, has a strong potential for the treatment of NAFLD and NASH.
About receptor P2Y13
The receptor P2Y13 is a member of the well-known family of P2Y receptors, including the P2Y12 receptor, the target of drugs to success such that the agent is anti-thrombotic Clopidogrel (Plavix®). The impairment of the receptor P2Y13 in preclinical models translates to a reduction of secretions of biliary lipid, their elimination and that of bile acids in the stool.
The deficiency leads to a dysfunction of return transport of cholesterol (or RLT) from macrophages to feces. The activation of the receptor P2Y13 by small molecules, acting as ligands, stimulates the elimination of HDL in the blood plasma as well as the recognition of HDL by the liver, thereby increasing the secretion of lipids and biliary stimulant in the aggregate, the RLT3.
3 Goffinet Dr et al, PLoS ONE 2014;9:e95807
CER-209 is the first drug candidate in its category, the agonists of the receptor P2Y13. CER-209 is a specific agonist of the receptor P2Y13 and it does not interact with the P2Y12 receptor. Preclinical studies have shown that CER-209 increases the recognition of HDL by the liver and improves the return transport of cholesterol (RLT), ultimately leading to the regression of the atheromatous plaque. Due to effects favourable metabolic effects on the liver during preclinical experiments, the CER-209 could provide a new mechanism for the treatment of Hepatitis Fat Non-Alcoholic (NAFLD) and nonalcoholic steatohepatitis (NASH).
About Cerenis : www.cerenis.com
Cerenis Therapeutics Holding company is a biopharmaceutical company dedicated to the discovery and development of innovative therapies based on the metabolism of lipids for the treatment of cardiovascular and metabolic diseases. The HDL is the mediator’s primary return transport of cholesterol (or RLT), the only metabolic pathway by which the cholesterol in excess is removed from arteries and transported to the liver for elimination from the body. Cerenis is developing a portfolio of therapies HDL, including mimetics of HDL particles to treat the genetic defects in HDL, as well as molecules that increase the number of HDL particles in patients who have little for the treatment of atherosclerosis and related metabolic diseases associated such as the Hepatitis Fatty Non-Alcoholic (NAFLD) and nonalcoholic steatohepatitis (NASH).
Cerenis is well-positioned to become one of the leaders of the market of therapies based on the metabolism of lipids with a rich portfolio of programs in development.
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