ARRAY BIOPHARMA REPORTS POSITIVE DATA ON MEK INHIBITOR

Array BioPharma has 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. The company is developing the drug to treat arthritis and other inflammatory diseases. These results were presented at the International Inflammation Research Association Conference.

The Phase I 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 one to 14 days of once-daily or twice-daily dosing.

In this setting, ARRY-438162 significantly inhibited IL-1ß and TNFa production after ex-vivo stimulation of clinical samples. IL-1ß was inhibited 50 percent to greater than 95 percent in samples where the drug concentration in plasma exceeded 50 nanograms/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.

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. The company has previously advanced one MEK inhibitor, ARRY-886, into clinical development for the treatment of cancer. The company believes inhibition of MEK will have broad applications in diseases driven by IL-1 and TNF.