INVOLVEMENT OF THE NA-ATPASE AND ITS INHIBITORS IN CARDIOVASCULAR-DISEASES(,K+)

Na+,K+-ATPase inhibitors have been shown to be effective in the treatm ent of congestive heart failure and cardiac arrhythmias. The Digitalis Investigation Group (DIG) trial has demonstrated that long-term digox in treatment improves symptoms of congestive heart failure and the qua lity of life in patients and, unlike cyclic adenosine monophosphatase (cAMP) dependent positive inotropes, does not have a negative effect o n survival. Recently, evidence has been provided that the Na+,K+-ATPas e may also be functionally modulated by endogenous inhibitors, such as ouabain-like factor (OLF). Elevated OLF levels have been documented i n pathological conditions, such as cardiovascular disorders and partic ular genetic or essential forms of human hypertension. Na+,K+-ATPase a nd OLF could represent a novel pharmacological target for the treatmen t of those forms of hypertension sustained by this mechanism. This rev iew will cover patenting activity in this field of research and will f ocus on the more significant patents published over the last-five year s.