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Sunobinop
Chemical compound From Wikipedia, the free encyclopedia
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Sunobinop (developmental code names V117957; IMB-115) is a high affinity small molecule nociceptin receptor partial agonist.[1]
As of February 2024, it is under clinical investigation for the treatment of insomnia/alcohol use disorder, interstitial cystitis, and overactive bladder syndrome.[2][3] It was previously also under investigation for the treatment of fibromyalgia.[1]
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Pharmacology
Sunobinop has nanomolar affinity (Ki) and efficacy (EC50) at human recombinant nociceptin/orphanin-FQ peptide (NOP) receptors. It has a high degree of functional selectivity for the NOP receptor. Sunobinop is a low affinity antagonist at human mu and kappa opioid receptors, and is a low affinity weak partial agonist at human delta opioid receptors.[4]
Clinical trials
Sunobinop was generally well tolerated in 3 studies involving 70 healthy subjects at doses that ranged from 0.6 to 30 mg. The most prominent adverse event was dose-dependent sedation/somnolence, which was more common at doses greater than 10 mg. In these studies, most of the absorbed sunobinop was excreted unchanged via rapid renal elimination.[5]
The safety and effectiveness of sunobinop has not been evaluated by the FDA. There is no guarantee that sunobinop will successfully complete development or gain FDA approval.[2]
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See also
References
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