SB/CDRI4/105, a Selective and Peripheral Kappa Opioid Receptor Agonist for Chemotherapy Induced Peripheral Neuropathic Pain

• A highly selective, peripherally restricted, and extremely G-protein-biased κ-opioid receptor (KOR) agonist
• Demonstrates robust analgesic efficacy in preclinical models of peripheral neuropathic pain, with effects comparable to or better than the FDA-approved drug duloxetine

• SB/CDRI4/105 is a novel and highly G-protein-biased KOR (κ-opioid receptor) agonist, exhibiting high affinity (IC₅₀ < 10 nM) and demonstrating a >100-fold bias toward G-protein-dependent signaling over β-arrestin-mediated pathways.
• Efficacy studies in rodent models of chemotherapy-induced peripheral neuropathy (CIPN) have shown that SB/CDRI4/105 is highly effective in alleviating hyperalgesia and allodynia, the hallmark symptoms of neuropathic pain.
• Importantly, the efficacy of SB/CDRI4/105 is comparable to or better than duloxetine, the only FDA-approved drug currently available for the treatment of CIPN

• Free from sedation, motor impairments, and shows no hERG liability
• No acute toxicity observed at doses up to 10 times the effective dose in Sprague-Dawley (SD) rats