Bradykinin antagonists: present progress and future prospects

Bradykinin (BK) antagonist peptides have been powerful tools for delineatin g roles of kinins in both normal and pathological physiology and offer prom ise of drug development for a variety of inflammatory conditions and cancer s. At the present time, potent peptide antagonists are available that are e ither specific for BK B1 or B2 receptors, or are effective on both receptor classes. Non-peptide BK B2 antagonists are now being announced and are und er investigation in several companies. The best peptide B1-B2 peptide antag onist is stable against all kininases, is orally available, and has a very long lifetime in vivo. Certain dimers of this antagonist, as well as severa l smaller molecules,are active against several cancers, both in vitro and i n vivo. (C) 1999 Elsevier Science B.V. All rights reserved.