The results of the study confirm that the agonist FXR EYP001 is safe and well tolerated in healthy subjects and demonstrate a commitment to organic of the nuclear receptor FXR.
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The development of EYP001 advance according to the initial plan for chronic hepatitis B, and other indications in the liver diseases are also explored, such as NASH (nonalcoholic Fatty liver disease).
Lyon, June 13, 2017 – ENYO Pharma SA, a biopharmaceutical company focusing currently on the development of treatments against viral infections, today announced that its clinical trial of Phase 1a single-and multiple-ascending doses evaluating its molecule EYP001 in healthy subjects has just ended. The results show that EYP001 is safe and well tolerated at all doses studied in 80 subjects. The analysis of safety, pharmacokinetics (PK) and pharmacodynamics (PD) are in agreement both with the biology set of FXR’s and with the results obtained by other compounds currently in early development for NASH. In particular, the levels and profile changes in the plasma levels of C4 (7ahydroxy4cholesten3one) and fibroblast growth factor 19 (FGF19) are consistent for a agonist of FXR in the range of doses between 60 mg and 500 mg administration dose for 15 days. These clinical results have been presented at the international conference on the liver in Amsterdam earlier this year (EASL). In addition, the in vitro data presented, have confirmed that EYP001 inhibits the release of particles of HBV in the same way as Tenofovir (TFV) or Entecavir (ETV), with an additive effect when they are combined. Finally, EYP001 only inhibits the production of viral proteins (HBsAg and HBeAg), reduced the cccDNA and pgRNA, whereas the mono-treatments TFV and ETV will have a negligible effect on these markers HBV in vitro.
EYP001 is a synthetic agonist of the receptor farnésoide X (FXR) with a favorable profile for oral therapy. The first phase 1 study was designed to determine the safety, tolerance and pharmacokinetics of EYP001 in healthy subjects. Another Phase 1 study is underway to evaluate the safety, effect of food and the PK of EYP001 in subjects with chronic hepatitis B infection.
Jacky Vonderscher, Ph.D., Director-General of ENYO Pharma ltd., commented : “We are very pleased with the profile emerging from EYP001 following our first Phase 1 trial. We are looking forward to bring the compound in other clinical phases, and believe that EYP001 has the potential to be also studied in other indications such as fatty liver disease non-alcoholic (NASH). ”
“The clinical program EYP001 has demonstrated an excellent profile of safety and tolerability. Using a new approach to analysis ECG (digitally enriched), we have also demonstrated that EYP001 does not impact the QT. This supports our desire to move quickly toward effectiveness trials, while advancing with all the regulatory needs associated with it. ” adds Pietro Scalfaro, M. D., Medical Director at ENYO Pharma SA.
About EYP001 and FXR
ENYO Pharma ltd. has obtained an exclusive and worldwide license for all indications of Poxel SA on the patents of a family of molecules agonists of FXR. EYP001 is a small molecule of different structure of bile acids, acting on the nuclear hormone receptor FXR in a human. It is developed for oral administration to patients with chronic infection by the Hepatitis b virus EYP001 interferes with the replication of HBV after its entry in the liver by affecting the activity transcriptionelle of the cccADN. Activation of FXR by EYP001 offers the potential of removing the most effective of the virus, paving the way to a real healing of the sick. The class of agonists of FXR has recently gained attention in the hepatobiliary diseases and metabolic disorders. Activation of FXR has a favorable effect on the regeneration of the liver and its effect in the prevention of liver fibrosis has already been demonstrated in rodent and in humans. FXR is a promising new target for drugs with multiple activities on viral replication and its persistence and regulates many metabolic pathways. In particular, it controls the fate of the bile acids in the liver and the intestine and influence the insulin sensitivity of the tissues in which it is highly expressed and also has an impact on lipid metabolism. Several agonists of FXR are currently in development for the treatment of NASH and primary biliary cirrhosis (PBC).
According to the WHO, more than 350 million people are chronically infected with the Hepatitis B virus and are waiting for a treatment, half located in Asia. Despite an improvement in the vaccination coverage, nearly 300 million people are still chronically infected by 2030, putting them in front of the major risk of developing liver cirrhosis and liver cancer. Currently approved drugs for the treatment of HBV chronic (PEG-interferon, and derivatives nucléot(s)idiques Tenofovir and Entecavir) suppress the presence of the virus in the blood, but are not in capacity to heal the patients as the virus continues its course destructive to the cells of the liver.
About the technology platform for ENYO Pharma SA – http://www.enyopharma.com/science/principle/
About ENYO Pharma SA – http://www.enyopharma.com/
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