Movatterモバイル変換


[0]ホーム

URL:


Jump to content
WikipediaThe Free Encyclopedia
Search

Sunobinop

From Wikipedia, the free encyclopedia
Chemical compound

Pharmaceutical compound
Sunobinop
Clinical data
Other namesIMB-115
Drug classNociceptin receptor agonist
Identifiers
  • 4-[(1R,5S)-9-[(1S,5S)-3-bicyclo[3.3.1]nonanyl]-9-azabicyclo[3.3.1]nonan-3-yl]-3-oxoquinoxaline-2-carboxylic acid
CAS Number
PubChemCID
ChemSpider
UNII
ChEMBL
Chemical and physical data
FormulaC26H33N3O3
Molar mass435.568 g·mol−1
3D model (JSmol)
  • O=C(O)C1=NC=2C=CC=CC2N(C1=O)C3CC4N(C(CCC4)C3)C5CC6CCCC(C5)C6
  • 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 namesV117957;IMB-115) is a high affinity small moleculenociceptin receptor partial agonist.[1]

As of February 2024, it is under clinical investigation for the treatment ofinsomnia/alcohol use disorder,interstitial cystitis, andoveractive bladder syndrome.[2][3] It was previously also under investigation for the treatment offibromyalgia.[1]

Pharmacology

[edit]

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 kappaopioid receptors, and is a low affinity weak partial agonist at human delta opioid receptors.[4]

Clinical trials

[edit]

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

[edit]

References

[edit]
  1. ^ab"Sunobinop - Shionogi/Imbrium Therapeutics".AdisInsight. Springer Nature Switzerland AG.
  2. ^ab"Pipeline".Imbrium Therapeutics. RetrievedMay 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. RetrievedMay 1, 2024.
μ-opioid
(MOR)
Agonists
(abridged;
full list)
Antagonists
δ-opioid
(DOR)
Agonists
Antagonists
κ-opioid
(KOR)
Agonists
Antagonists
Nociceptin
(NOP)
Agonists
Antagonists
Others
Retrieved from "https://en.wikipedia.org/w/index.php?title=Sunobinop&oldid=1315534772"
Categories:
Hidden categories:

[8]ページ先頭

©2009-2025 Movatter.jp