Sunobinop

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Clinical data
Other namesIMB-115
Drug classNociceptin receptor agonist
Identifiers
IUPAC name
  • 4-nonanyl]-9-azabicyclononan-3-yl]-3-oxoquinoxaline-2-carboxylic acid
CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
Chemical and physical data
FormulaC26H33N3O3
Molar mass435.568 g·mol−1
3D model (JSmol)
SMILES
  • O=C(O)C1=NC=2C=CC=CC2N(C1=O)C3CC4N(C(CCC4)C3)C5CC6CCCC(C5)C6
InChI
  • InChI=1S/C26H33N3O3/c30-25-24(26(31)32)27-22-9-1-2-10-23(22)29(25)21-14-18-7-4-8-19(15-21)28(18)20-12-16-5-3-6-17(11-16)13-20/h1-2,9-10,16-21H,3-8,11-15H2,(H,31,32)/t16-,17-,18-,19+,21?/m0/s1
  • Key:COTYYZPYDJKKIS-MCXOOUIESA-N

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

As of Feb 2024, it is under clinical investigation for the treatment of insomnia/alcohol use disorder, interstitial cystitis, and overactive bladder syndrome. It was previously also under investigation for the treatment of fibromyalgia.

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.

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.

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.

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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