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Xenova Publishes Data on Novel Low Molecular Weight Anti-Thrombosis
Compound
XR5118 Enhances Clot Lysis Activity in Preclinical Model Without Causing Bleeding Risks
SLOUGH, United Kingdom, April 8 /PRNewswire/ -- Xenova Group PLC announced today the publication of research on the company's novel inhibitors of plasminogen activator-1 (PAI-1). In the current issue of "Fibrinolysis and Proteolysis" (Vol. 11, No. 1), a team of scientists from Xenova and University College, London, UK reported for the first time that the ability of a low molecular weight research compound, XR5118, to change the balance between formation and dissolution of blood clots "in vivo" correlated with two clinical markers tissue plasminogen activator (tPA) and plasminogen activator inhibitor-1 (PAI-1).
Dr. Peter A. Charlton, Ph.D., Director of Molecular Pharmacology and his team at Xenova showed that intravenous infusion of XR5118 prevents blood vessels occlusion in a preclinical "in vivo" model of arterial thrombosis. In this model, XR5118 did not increase the bleeding time, the major side effect of currently available drugs. Furthermore,
XR5118 had no effect on global "in vitro" tests of haemostasis with blood taken from human volunteers.
"Our research in preclinical models demonstrates that a novel inhibitor of PAI can enhance the clearance of blood clots without the usual side effects, such as excessive bleeding, associated with current available treatments," said Dr. Charlton. "Along with our U.S. subsidiary, MetaXen, we are continuing the optimization and development of the lead compound XR5118, as well as other novel PAI inhibitors."
tPA is the major physiological activator of blood clot clearance. tPA initiates the breakdown of the fibrin protein in blood clots and clears them from blood vessels. PAI-1 prevents tPA from performing its role, thus contributing to the onset of thrombotic conditions. Many clinical researchers propose that elevated levels of PAI-1, which result in reduced fibrinolytic capacity, is a major risk factor in a variety of thromboembolic disorders. Xenova is investigating several
PAI inhibitors, including the XR5118 series, as potential treatments for thrombosis.
Blood clots, or thrombi, are involved in a wide range of cardiovascular diseases including deep vein thrombosis (DVT), unstable angina (UA), certain types of stroke and acute myocardial infarction (MI). According to recent estimates, there were approximately 500,000 new cases of DVT, 500,000 to 1,000,000 new cases of UA and 1,500,000 cases of acute MI in the United States in 1993.
Xenova is an emerging biopharmaceutical company specializing in the discovery and development of new small molecule drugs originally derived from naturally occurring micro-organisms, such as fungi and bacteria, and from plants and plant extracts. The Company has developed an integrated group of proprietary platform technologies to
rapidly and efficiently identify candidate compounds, or leads, for new drugs from such natural sources. SOURCE Xenova Group plc |
