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by | Dec 19, 2023 | Monarda

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Sunobinop (developmental code names V117957; IMB-115) is a high affinity small molecule nociceptin receptor partial agonist.[1]

As of Feb 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]

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]

See also

References

  1. ^ a b "Sunobinop - Shionogi/Imbrium Therapeutics". AdisInsight. Springer Nature Switzerland AG.
  2. ^ a b "Pipeline". Imbrium Therapeutics. Retrieved May 1, 2024.
  3. ^ WO application 2018020418, Harris SC, Kapil RP, Kyle DJ, Whiteside G, "Treatment and prevention of sleep disorders", published 2018-02-01, assigned to Purdue Pharma L.P. 
  4. ^ Whiteside GT, Kyle DJ, Kapil RP, Cipriano A, He E, Zhou M, et al. (January 2024). "The nociceptin/orphanin FQ receptor partial agonist sunobinop promotes non-REM sleep in rodents and patients with insomnia". The Journal of Clinical Investigation. 134 (1). doi:10.1172/JCI171172. PMC 10760950. PMID 37883189.
  5. ^ Cipriano A, Kapil RP, Zhou M, Shet MS, Whiteside GT, Willsie SK, et al. (March 13, 2024). "Safety, Tolerability, and Pharmacokinetics of Single- and Multiple-Ascending Doses of Sunobinop in Healthy Participants". Clinical Pharmacology in Drug Development. doi:10.1002/cpdd.1394. Retrieved May 1, 2024.


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