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BL-1110 is an orally administered small-molecule toll-like receptor 4 (TLR4) antagonist being developed for the prevention and treatment of opioid-induced neuropathic pain and hyperalgesia. It was invented at the University of Colorado Boulder and subsequently licensed for development by BioLineRx, which positioned the compound to block activation of TLR4 on glial cells by opioid analgesics, thereby dampening pro‑inflammatory signaling thought to underlie opioid-induced pain sensitization and tolerance.[1][3] Preclinical work has focused on its ability to interfere with the non-classical, glial-mediated pronociceptive actions of opioids without impairing their canonical µ-opioid receptor–mediated analgesia, with the goal of improving the safety and long‑term efficacy of opioid therapy.[1][3]
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