CB-189,625

CB-189,625 is a small molecule antagonist of the bradykinin B1 receptor (B1R) that was developed by Cerep for the treatment of acute and chronic pain. Unlike the constitutively expressed B2 receptor, the B1 receptor is typically induced and upregulated in response to tissue injury, inflammation, and certain chronic pain states, making it a selective target for analgesic intervention with potentially fewer side effects. CB-189,625 underwent Phase 1 clinical evaluation, including a randomized, double-blind, placebo-controlled ascending multiple-dose study in healthy male volunteers to assess its safety, tolerability, and pharmacokinetics. Despite reaching clinical stages, development of the compound appears to have been discontinued, as no recent clinical activity or pipeline mentions have been recorded since the mid-2000s.