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Labradimil is a synthetic nine-amino acid peptide analogue of bradykinin that functions as a selective bradykinin B2 receptor agonist. It was developed to transiently and reversibly increase the permeability of the blood-brain barrier (BBB) by stimulating B2 receptors on the vascular endothelium, which triggers the opening of tight junctions. The drug's primary therapeutic intent was to facilitate the delivery of co-administered chemotherapeutic agents, such as carboplatin, into the central nervous system for the treatment of malignant gliomas and other brain tumors. Although it progressed to Phase 3 clinical trials, it failed to show a statistically significant improvement in patient outcomes, leading to the discontinuation of its development by Alkermes.
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