Therapeutic potential of icatibant (HOE-140, JE-049).
There is now a substantial body of work implicating bradykinin, an endogenous peptide neurohormone, in the pathophysiology of a variety of inflammatory conditions in man. Icatibant (HOE-140, JE-049), a highly selective antagonist at the bradykinin B2 receptor, blocks the vasodilatation and increased vascular permeability associated with exogenous bradykinin administration both in experimental models and in vivo in man. Recent attention has focused on the therapeutic potential of icatibant in a number of human disease states. The most promising of these is hereditary angioedema in which Phase III clinical trials have recently been completed and regulatory approval is currently being sought in Europe and the USA. A therapeutic role for icatibant has also been proposed in several other human conditions including drug-induced angioedema, airways disease, thermal injury, refractory ascites in patients with liver cirrhosis, and acute pancreatitis, although this work remains largely experimental.
Cruden
Nicholas L M
NL
University of Edinburgh, Centre for Cardiovascular Science, Chancellor's Building, 49 Little France Crescent, Little France, Edinburgh EH164SB, UK. nick.cruden@ed.ac.uk
Newby
David E
DE
D054179:Angioedemas, Hereditary / Q000188:drug therapy* / Q000503:physiopathology; D001920:Bradykinin / Q000031:analogs & derivatives* / Q000494:pharmacology / Q000627:therapeutic use; D065094:Bradykinin B2 Receptor Antagonists; D006801:Humans; D016234:Kallikrein-Kinin System / Q000502:physiology; D012140:Respiratory Tract Diseases / Q000188:drug therapy* / Q000503:physiopathology
D065094:Bradykinin B2 Receptor Antagonists; C065679:icatibant; D001920:Bradykinin