NEW PLATELET INHIBITORS

ARTERIAL THROMBOTIC DISEASES ARE THE LEADING CAUSE OF DEATH IN THE UNITED STATES, WITH IMMENSE SOCIOECONOMIC AND PSYCHOLOGICAL IMPACTS. DRUGS THAT CAN EFFICACIOUSLY REDUCE OR ELIMINATE THESE DISEASES ARE OF GREAT CLINICAL IMPORTANCEAND SHOULD HAVE MAJOR COMMERCIAL APPLICATIONS. UNFORTUNATELY, EFFICACIOUS DRUGS ARE LIMITED. THROMBO DIAGNOSTIC, INC., HAS IDENTIFIED ANTIPLATELET PROPERTIES IN THE ETHANOL-SOLUBLE FRACTION OF A CHINESE FUNGUS, CORDYCEPS SINENSIS. THE FRACTION EXHIBITED INHIBITORY ACTIVITY AGAINST PLATELET AGGREGATION AND SECRETION. ITS INHIBITORY EFFECT APPEARS TO BE INDEPENDENT OF THROMBOXANE A2 AND MAY BE RELATED TO CAMP ELEVATION. IT IS PLANNED TO PURIFY THE ACTIVE COMPONENT, EVALUATE ITS BIOLOGICAL ACTIVITY, ELUCIDATE ITS MECHANISM OF ACTION, AND ASSESS ITS ANTITHROMBOTIC EFFICACY. THE PHASE I STUDY WILL DETERMINE THE FEASIBILITY OF THE PURIFYING PROCEDURES AND TESTING ANTIPLATELET PROPERTIES. ASEQUENCE OF SOLVENT-SOLVENT EXTRACTIONS WILL SEGREGATE ACTIVE COMPOUNDS ON THE BASIS OF THEIR POLARITY INTO ONE OR TWO HIGHLY ENRICHED FRACTIONS. THE INHIBITORY EFFECT OF THE CONCENTRATED FRACTIONS ON PLATELET AGGREGATION AND SECRETION WILL BE EVALUATED IN A LUMIAGGREGOMETER. THE FRACTIONS WILL THEN BE PROCESSED TO ISOLATE THE ACTIVE COMPONENT. THE FULL DEVELOPMENT OF THE ACTIVE COMPONENT INTO ANTITHROMBOTIC DRUGS WILL OCCUR IN PHASE II AND SUBSEQUENT CLINICAL STUDIES.