APD791 for Arterial Thrombosis
Our lead anti-thrombotic drug candidate, APD791, has completed Phase 1a and Phase 1b clinical trials. The Phase 1 trials were primarily intended to evaluate the safety and tolerability of single and multiple-ascending doses of APD791. In addition, we also evaluated the pharmacokinetics and pharmacodynamics of APD791. In the Phase 1 trials, APD791 was generally well tolerated and dose-dependent inhibition of serotonin-mediated amplification of platelet aggregation was demonstrated. APD791 was rapidly absorbed and exposures were related to dose. Results from these trials further support APD791's novel mechanism of action and the preclinical data.
APD791 is a novel, oral and selective inverse agonist of the 5-HT2A serotonin receptor. Serotonin activation of the 5-HT2A receptor on platelets and vascular smooth muscle tissue is thought to play an important role in events leading to thrombosis, and elevated serotonin levels have been associated with increased cardiovascular risk. Normally, when a platelet is activated by one of a number of factors such as thrombin or collagen, the platelet releases serotonin, which, based on preclinical studies, promotes platelet aggregation, vasoconstriction and intimal hyperplasia. By blocking activation of the 5-HT2A receptor on platelets and in other cardiovascular tissues, APD791 may curb these serotonin-mediated effects in the clinical setting, thereby reducing or preventing thrombosis. We believe APD791 represents a new approach to reducing the risk of arterial thromboembolic disease.
The American Heart Association estimates that in the United States over 14.4 million people alive in 2006 had survived either a myocardial infarction or a stroke. To reduce the risk of future events, many patients receive daily anti-thrombotic therapy. Worldwide sales of Plavix®, a leading anti-thrombotic marketed by Bristol-Myers Squibb and sanofi-aventis, totaled $7.3 billion in 2007, making it the second best selling drug in any therapeutic category.
(This page was last updated: January 5th, 2010. Additional information regarding Arena is available in its SEC filings.)
