BI 113823

BI 113823 is a potent and selective small molecule antagonist of the bradykinin B1 receptor. It was developed by Boehringer Ingelheim as an orally available drug candidate primarily for the treatment of osteoarthritis and chronic pain conditions. Preclinical studies demonstrated that BI 113823 exhibits high affinity for both human and rat B1 receptors, with no significant activity at the bradykinin B2 receptor or other related targets. The compound has shown analgesic effects in animal models of inflammatory pain, such as those induced by complete Freund's adjuvant, and can reduce mechanical hyperalgesia via both peripheral and spinal mechanisms. Additionally, it has been shown to reduce post-infarction cardiac remodeling in rats following myocardial infarction, attenuate acute lung injury in sepsis models, decrease inflammatory cytokine production (e.g., TNF-α, IL-1β), lower neutrophil influx into tissues, and improve survival after severe polymicrobial sepsis. Despite promising preclinical results and completion of phase I trials for osteoarthritis in Germany, further clinical development appears to have been discontinued[1][2][3][4][5][6][7][8].