Array BioPharma Inc. (Nasdaq: ARRY) announced that its first-in-class MEK inhibitor for the treatment of inflammatory diseases, ARRY-438162, has met its primary objectives in a single ascending dose clinical study involving 20 healthy volunteers. These results were presented by Array?s President and Chief Scientific Officer, Kevin Koch, Ph.D., at the 14th International Inflammation Research Association Conference in Cambridge, Maryland.
In this setting, ARRY-438162 significantly inhibited IL-1β and TNFα production after ex-vivo stimulation of clinical samples. IL-1β was inhibited 50% to greater than 95% in samples where the drug concentration in plasma exceeded 50 ng/mL. An interim analysis in the ongoing multiple ascending dose portion of the study indicates that ARRY-438162 demonstrates linear increases in exposure with increasing dose and has presented no serious adverse events through 14 days of continuous dosing. The Company will conduct a full analysis of safety, pharmacokinetics and efficacy data upon completion of the study. These preliminary results support Array?s plans to advance its clinical program into rheumatoid arthritis patients this fall.
?Potent cytokine inhibition from an orally active drug through a novel mechanism represents a major achievement for the ARRY-438162 clinical program,? said Dr. Koch. ?These data provide strong support for advancing this first-in-class drug into patients to evaluate its efficacy against a broad range of inflammatory disease.?
Clinical Study Design
The Phase 1 trial is a randomized, placebo-controlled, double-blind, dose escalation study to assess the safety, tolerability, pharmacokinetics and pharmacodynamics of ARRY-438162. Both parts of this study are being conducted in healthy volunteers with 1 to 14 days of once-daily or twice-daily dosing.
About Inflammatory Disease
Inflammation is a natural biologic response to injury or infectious attack to the human body. Unregulated inflammation results in a broad range of conditions, most of which are classified by the tissue or organ where the inflammation occurs. These conditions include rheumatoid arthritis (RA) in the joint, psoriasis in the skin, chronic obstructive pulmonary disease in the lung, fibrotic disease in the liver and kidney, Crohn?s disease in the intestine, congestive hear failure and arteriosclerosis in the arteries, among others. Currently, some of the most effective treatments for these diseases are injectable protein therapeutics, which have significant cost and patient compliance issues. IV-dosed protein therapeutics currently on the market ? such as Enbrel?, Remicade?, Humira? and Kineret? ? bind to and/or modulate the activity of the inflammatory cytokines TNF-α or IL-1 and are utilized for the treatment of RA, psoriasis and Crohn?s disease. The TNF inhibition market alone, which is dominated by these therapeutics, is expected to grow from $9 billion in 2005 to $17 billion in 2010, according to analyst estimates.
About ARRY-438162 / MEK for Inflammation
MEK is an enzyme that regulates the biosynthesis of the inflammatory cytokines TNF, IL-6 and IL-1. Array scientists have discovered potent MEK inhibitors that interfere with these biosynthetic processes. We have previously advanced one MEK inhibitor, ARRY-886, into clinical development for the treatment of cancer. Given our experience with the safety profile of MEK inhibitors, we believe inhibition of MEK will have broad applications in diseases driven by IL-1 and TNF. ARRY-438162, an orally active MEK inhibitor, has shown significant efficacy and is well tolerated in preclinical models of human arthritis and other inflammatory diseases. We initiated Phase 1 clinical testing in normal, healthy volunteers in April 2006.
About Array BioPharma:
Array BioPharma Inc. is a biopharmaceutical company focused on the discovery, development and commercialization of targeted small molecule drugs to treat life threatening and debilitating diseases. Our proprietary drug development pipeline is focused on the treatment of cancer and inflammatory disease and includes clinical candidates that are designed to regulate therapeutically important targets. In addition, leading pharmaceutical and biotechnology companies collaborate with Array to discover and develop drug candidates across a broad range of therapeutic areas.