Development of an antagonist of the inducible B1 Receptor

Jerini is developing an orally-available small molecule bradykinin B1 receptor antagonist to treat conditions associated with inflammation and/or pain. The B1R is not expressed under normal conditions, but is rapidly induced under pathophysiological conditions such as tissue damage or inflammation. This makes the B1R a particularly attractive drug target. Activation of the B1R produces a range of pro-inflammatory effects, including edema, pain and promotion of blood-borne leukocyte trafficking. In view of the severe conditions associated with overshooting and thus pathological inflammation and pain, both acute and chronic, there is great potential for novel compounds that are effective in selectively blocking the activation of B1 receptors.

References:

JB Calixto, R Medeiros, ES Fernandes, J. Ferreira, DA Cabrini, MM Campos, Kinin B1 receptors: key G-protein coupled receptors and their role in inflammatory and painful processes. BrJPharmacol. 2004 143:808-818

LMF Leeb-Lundberg, F Marceau, W Müller-Esterl, DJ Pettibone, B Zuraw International Union of Pharmacology: Classification of the Kinin Receptor Family: from Molecular Mechanisms to Pathophysiological Consequences. PharacolRev. 2005 57:27-77 Top