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MK-0686 is a small molecule bradykinin B1 receptor antagonist developed by Merck & Co for the treatment of neuropathic pain and inflammation. It was designed to have good central nervous system (CNS) penetration and demonstrated oral efficacy in preclinical models of hyperalgesia. The drug reached phase II clinical trials for indications including osteoarthritis, postoperative pain, and postherpetic neuralgia but failed to demonstrate efficacy at this stage. Mechanistically, it acts by blocking the bradykinin B1 receptor, which is implicated in sustaining chronic inflammatory and pain responses.
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