Date: 2011-09-15
Type of information: Initiation of preclinical development
phase: 1
Announcement: treatment of the first patient
Company: Phenex Pharmaceuticals (Germany)
Product: Px-102
Action
mechanism: Px-102 is a potent, fully-synthetic and non-steroidal FXR agonist. The Farnesoid X Receptor (FXR) is a bile acid receptor which when activated by Px-102 has a profound positive impact on cholesterol, triglyceride and glucose metabolism in liver and intestine. As was already demonstrated in several publications and Phenex-proprietary animal studies the FXR agonist Px-102 potently reduces intestinal uptake of neutral lipids and cholesterol and at the same time enhances the excretion of these lipid species. In addition, Px-102 improves hepatic insulin sensitivity and shows massive hepatoprotective effects in animal models of liver cirrhosis or fibrosis. It is this combination of potent metabolic and liver protective effects that makes Px-102 an ideal candidate for the treatment of Non-Alcoholic Steatohepatitis (NASH). Inflammation and beginning fibrosis are the hallmarks in people with NASH-livers which affects a subset of individuals who have developed a fatty liver due to an unhealthy lifestyle and overweight. The prevalence of NASH is estimated to approach 5% of the total population in industrialized countries. NASH markedly increases the likelihood to develop liver cancer or end stage liver cirrhosis.
Disease: NASH (non-alcoholic steatohepatitis) and other liver diseases
Therapeutic area: Metabolic diseases - Liver diseases
Country:
Trial details:
Latest
news: Phenex Pharmaceuticals has announced the start of a first-in-man Phase I study with its clinical drug candidate Px-102, a synthetic non-steroidal FXR agonist. The volunteers of the first dose level received the drug and showed no signs of discomfort or other adverse effects. This Phase I first-in-man study will be escalated from the initial dose over seven dose levels to obtain information about the tolerance and pharmacokinetics of Px-102 in healthy volunteers. Following this first Phase I study Phenex plans to run a multiple ascending dose Phase I study where the same parameters will be observed during several days of multiple administrations.
The Phase I studies for Px-102 will be finished by early 2012. If all requirements are met, Phenex then plans to test Px-102 in a Phase II study in patients with Metabolic Syndrome and Non-Alcoholic Fatty Liver Disease
(NAFLD) to confirm if the potent therapeutic effects such as lipid lowering, improvement of insulin sensitivity and reduction of markers for liver damage which were observed in several animal studies can be reproduced in human patients
