Healthcare Industry News: TRACLEER
News Release - December 11, 2006
Actelion-1 -- First Tissue-Targeting Endothelin Receptor Antagonist -- in Phase III for Pulmonary HypertensionALLSCHWIL, Switzerland, Dec. 11, 2006 (HSMN NewsFeed) -- Actelion Ltd (Swiss:ATLN.SW ) announced today that it has initiated a comprehensive Phase III program for Actelion-1, the first tissue targeting endothelin receptor antagonist (ERA). Initially, development will focus on pulmonary hypertension (PH), with other cardiopulmonary indications expected to follow.
Martine Clozel, MD and Head of Drug Discovery (Pharmacology and Preclinical Development) commented: ``Actelion-1 was rationally designed and optimized to act in tissues. This is fundamental because endothelin is produced in the tissues and the endothelin receptors are located mostly in tissues.(1)''
Martine Clozel added: ``We have established efficacy and tolerability of Actelion-1 in a Phase II program that included a trial in essential hypertension. Effects in essential hypertension are good indicators of pharmacodynamics and establish the dose-effect relationship. Actelion-1 demonstrated a greater effect on blood pressure reduction compared to both placebo and to enalapril, with tolerability comparable to placebo and the standard findings for the ERA class in terms of potential liver signals. I am especially encouraged that there were no cases of peripheral edema, as this observation lends basic support to the tissue-targeting approach.''
Martine Clozel concluded: ``I believe that Actelion-1, with its high potency and its demonstrated efficacy, has the potential to substantially impact long-term disease outcome in a wide range of cardiopulmonary diseases.''
The now-initiated Phase III program is not only the first in the enlarged indication Pulmonary Hypertension (PH), but also the first that will evaluate morbidity/mortality benefits as the primary investigational goal. This pivotal program is expected to last for several years. Actelion is also undertaking a large-scale clinical pharmacology program to support both the PH program as well as potential future development programs for Actelion-1 in other cardiopulmonary indications.
Jean-Paul Clozel, MD and Chief Executive Officer, commented: ``With Actelion-1, we are capitalizing on almost 20 years of ground-breaking research by our team in the field of endothelin research.''
Jean-Paul Clozel added: ``Actelion-1 highlights once again the innovative output by 220 researchers that have also pioneered many other breakthroughs in fields such as orexin receptor antagonism, renin inhibition and selective S1P1 agonism.''
(1) Martine Clozel and Lewis J. Rubin: The Endothelin System in
Cardiopulmonary Disease. Friedrich Reinhardt Verlag Basel, 2004.
Actelion-1 is a tissue-targeting Endothelin Receptor Antagonist that has been discovered in an in-house research program. Through complete blockade of tissular endothelin, Actelion-1 is expected to protect tissue from the damaging effect of elevated endothelin, specifically in the cardiovascular system. In pre-clinical studies, Actelion-1 also exhibited effects suggesting that it maintains the integrity of the vascular wall and improves long-term outcome. Accordingly, Actelion-1 may provide therapeutic benefit in a wide range of cardiovascular indications.
About Actelion-1 in Phase II
The Phase II program included a double-blind, placebo- and active- controlled, multicenter, parallel group, dose finding study in 379 patients with mild essential hypertension. Four doses of Actelion-1 (0.3, 1, 3 and 10mg) and enalapril (20mg), all once daily for eight weeks were each evaluated versus placebo. Preliminary analysis suggests that the higher three doses were active, with the treatment effect of the two higher doses of Actelion-1 significantly better than placebo and better than enalapril at trough, i.e. 24 hours after drug intake.
Actelion-1 was well tolerated across all four doses. The overall frequency of adverse events was similar to those observed in the placebo group. As a member of the class of endothelin receptor antagonist, Actelion-1 may potentially exhibit known class effects such as a propensity for elevated liver enzymes. In this study, there were five cases of increased liver enzymes above three times the upper limit of normal. They were evenly distributed over all four doses of Actelion-1 (1,2,1,1). In three cases, there were concomitant disease states (pancreatic cancer, anesthesia for prostatectomy and urinary tract infection treated with antibiotics) that complicate interpretation of those changes.
Following completion of data analysis, Actelion expects full results to become available through publication in a peer-reviewed scientific journal.
The company will provide more information on Actelion-1 and its many other projects in Research and Development at the forthcoming Actelion Day on Thursday, February 22, 2007 in Allschwil/Switzerland (formal invitation to follow in early January 2007).
Actelion Ltd. is a biopharmaceutical company with its corporate headquarters in Allschwil/Basel, Switzerland. Actelion's first drug TRACLEER(r), an orally available dual endothelin receptor antagonist, has been approved as a therapy for pulmonary arterial hypertension. Actelion markets TRACLEER(r) through its own subsidiaries in key markets worldwide, including the United States (based in South San Francisco), the European Union, Japan, Canada, Australia and Switzerland. At the end of September 2006, TRACLEER(r) was commercially available in 35 countries worldwide. Actelion, founded in late 1997, is a leading player in innovative science related to the endothelium -- the single layer of cells separating every blood vessel from the blood stream. Actelion's over 1,200 employees focus on the discovery, development and marketing of innovative drugs for significant unmet medical needs. Actelion shares are traded on the SWX Swiss Exchange (ticker symbol: ATLN).
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