First-in-Human Trial Will Evaluate Safety of Pan-Genotypic Protease Inhibitor in Both Healthy Subjects and Genotype 1 or 3 HCV-Infected Patients
NEW HAVEN, Conn., May 25, 2011 (GLOBE NEWSWIRE) -- Achillion Pharmaceuticals, Inc. (Nasdaq:ACHN), a leader in the discovery and development of small molecule drugs to combat the most challenging infectious diseases, today announced that the Company has begun dosing in a Phase 1 clinical trial of ACH-2684, a novel pan-genotypic protease inhibitor being developed for the treatment of chronic hepatitis C virus (HCV) infection.
The Phase 1 clinical study is a randomized, double-blind, placebo-controlled trial to investigate the safety, tolerability, pharmacokinetic profile and antiviral activity of ACH-2684. The trial consists of three segments including assessment of single ascending oral doses in healthy volunteers, a 14 day multiple ascending doses segment in healthy volunteers, and evaluation of 3 days of oral ascending repeat doses in subjects with either genotype 1 or genotype 3 hepatitis C infection. The trial will take place in the United States and is designed to enroll up to 78 healthy volunteers and up to 40 HCV-infected patients.
"This first-in-human clinical trial will be instrumental in establishing the safety profile of ACH-2684 in humans," stated Elizabeth A. Olek, D.O., Vice President and Chief Medical Officer of Achillion. "It will also provide Achillion with important preliminary efficacy data against HCV genotypes 1 and 3, and help us to select doses for subsequent clinical development."
"We are very excited to take ACH-2684 into the clinic and advance what we hope will be a unique pan-genotypic, once-daily protease inhibitor," said Michael D. Kishbauch, President and Chief Executive Officer of Achillion. "Furthermore, we expect to shortly launch the 12-week segment of the Phase 2 trial of our lead ACH-1625 protease inhibitor, as well as a Phase 1 trial of our ACH-2928 NS5A inhibitor. We believe we remain poised to deliver a trio of important HCV clinical milestones near the end of this year, namely, 12-week EVR results on ACH-1625 and human proof-of-concept data on both ACH-2684 and ACH-2928. These are all important components in our ultimate strategy of becoming a leader in the development of HCV combination therapies involving our protease and NS5A inhibitors."
ACH-2684 is a pan-genotypic HCV protease inhibitor designed and synthesized based on crystal structures of enzyme/inhibitor complex. ACH-2684 is a macro-cyclic, non-covalent, reversible inhibitor of NS3 protease. In preclinical studies, ACH-2684 demonstrated pico-molar potency, excellent pharmacokinetic properties and safety profile at high drug exposures. ACH-2684 also exhibits rapid and extensive partitioning to the liver, as well as high liver/plasma ratios in preclinical studies. ACH-2684 has shown pico-molar potency against NS3 protease that is specific to HCV. It is active against the 6 known genotypes of HCV and exhibits equipotent activity against HCV genotypes 1a and 1b at an IC50 of approximately 100 picomolar. The drug candidate was discovered internally and is being advanced by Achillion.
The hepatitis C virus is the most common cause of viral hepatitis, which is an inflammation of the liver. It is currently estimated that more than 170 million people are infected with HCV worldwide and The American Association of Liver Disease estimates that up to 80% of individuals become chronically infected following exposure to the virus. If left untreated, chronic hepatitis can lead to permanent liver damage, which can result in the development of liver cancer, liver failure or death. Few therapeutic options currently exist for the treatment of HCV infection. The current standard of care is limited by its specificity for certain types of HCV, significant side-effect profile, and injectable route of administration.
About Achillion Pharmaceuticals
Achillion is an innovative pharmaceutical company dedicated to bringing important new treatments to patients with infectious disease. Achillion's proven discovery and development teams have advanced multiple product candidates with novel mechanisms of action. Achillion is focused on solutions for the most challenging problems in infectious disease including hepatitis C and resistant bacterial infections. For more information on Achillion Pharmaceuticals, please visit www.achillion.com or call 1-203-624-7000.