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Valiloxybate

From Wikipedia, the free encyclopedia

Pharmaceutical compound
Valiloxybate
Clinical data
Other namesValiloxibic acid; Valiloxybic acid; 4-((L-Valyl)oxy)butanoic acid; XW-10172; XW10172; XWL-008; XWL008
Routes of
administration
Oral[1]
Drug classGABAB receptoragonist;GHB receptoragonist;Hypnotic
ATC code
  • None
Identifiers
  • 4-[(2S)-2-amino-3-methylbutanoyl]oxybutanoic acid
CAS Number
PubChemCID
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
Chemical and physical data
FormulaC9H17NO4
Molar mass203.238 g·mol−1
3D model (JSmol)
  • CC(C)[C@@H](C(=O)OCCCC(=O)O)N
  • InChI=1S/C9H17NO4/c1-6(2)8(10)9(13)14-5-3-4-7(11)12/h6,8H,3-5,10H2,1-2H3,(H,11,12)/t8-/m0/s1
  • Key:RMGPNQKZEPTAOC-QMMMGPOBSA-N

Valiloxybate (INNTooltip International Nonproprietary Name,USANTooltip United States Adopted Name;[2] developmental code nameXW-10172) is anextended-releaseprodrug ofγ-hydroxybutyrate (GHB; oxybate) which is under development for the treatment ofnarcolepsy.[1][3][4][5][6] It is also being investigated for treatment ofexcessive daytime sleepiness (EDS) in people withParkinson's disease.[7] The drug is takenorally once per night.[1][4][5][8][6]

Pharmacology

[edit]

It is anamino acid (L-valine)ester prodrug of GHB,[6][2] which itself acts as aGABAB andGHB receptoragonist.[9][10] Relative to administration of GHB itself, valiloxybate showed a delayedtime to peak levels and an extendedduration of GHB exposure in humans.[6] It is said to maintain desired GHB levels for 6 to 7 hours.[11] This profile is compatible with once-nightly dosing,[6] in contrast to GHB itself which is typically administered twice per night due to its very shortelimination half-life.[12][13][14] In addition, unlikesodium oxybate, valiloxybate contains nosodium orcation, and hence avoids excessive sodium intake.[6][15]

History

[edit]

Valiloxybate is under development by XW labs or XWPharma.[1] As of September 2025, no recent development has been reported, but valiloxybate has reachedphase 1clinical trials for treatment of narcolepsy andphase 2 trials for treatment of sleeping problems in Parkinson's disease.[1][7]

See also

[edit]

References

[edit]
  1. ^abcde"Valiloxybate".AdisInsight. 28 September 2025. Retrieved30 September 2025.
  2. ^ab"VALILOXYBATE".Inxight Drugs. Retrieved30 September 2025.
  3. ^"Valiloxibic acid".AdisInsight. 28 July 2022. Retrieved30 September 2025.
  4. ^abRoth T (March 2025)."Therapeutic Use of γ-Hydroxybutyrate: History and Clinical Utility of Oxybates and Considerations of Once- and Twice-Nightly Dosing in Narcolepsy".CNS Drugs.39 (Suppl 1):37–51.doi:10.1007/s40263-024-01150-8.PMC 11950157.PMID 40111735.
  5. ^abAbad VC (2023). "Pharmacological options for narcolepsy: are they the way forward?".Expert Rev Neurother.23 (9):819–834.doi:10.1080/14737175.2023.2249234.PMID 37585269.
  6. ^abcdefCanafax D, Xiang W, Xiang JN (3 May 2021)."501 Clinical PK of XW10172 for Once Nightly Therapy in Patients with Narcolepsy or Sleep Disorders in Neurodegenerative Diseases"(PDF).Sleep.44 (Supplement_2):A197–A198.doi:10.1093/sleep/zsab072.500.ISSN 0161-8105. Retrieved30 September 2025.
  7. ^abWolff A, Schumacher NU, Pürner D, Machetanz G, Demleitner AF, Feneberg E, et al. (June 2023)."Parkinson's disease therapy: what lies ahead?".J Neural Transm (Vienna).130 (6):793–820.doi:10.1007/s00702-023-02641-6.PMC 10199869.PMID 37147404.
  8. ^Dauvilliers Y, Bogan RK, Šonka K, Partinen M, Foldvary-Schaefer N, Thorpy MJ (2022)."Calcium, Magnesium, Potassium, and Sodium Oxybates Oral Solution: A Lower-Sodium Alternative for Cataplexy or Excessive Daytime Sleepiness Associated with Narcolepsy".Nat Sci Sleep.14:531–546.doi:10.2147/NSS.S279345.PMC 8976528.PMID 35378745.
  9. ^Trombley TA, Capstick RA, Lindsley CW (December 2020). "DARK Classics in Chemical Neuroscience: Gamma-Hydroxybutyrate (GHB)".ACS Chem Neurosci.11 (23):3850–3859.doi:10.1021/acschemneuro.9b00336.PMID 31287661.
  10. ^Wellendorph P, Gauger SJ, Andersen JV, Kornum BR, Solbak SM, Frølund B (July 2025). "International Union of Basic and Clinical Pharmacology. CXX. γ-Hydroxybutyrate protein targets in the mammalian brain-beyond classic receptors".Pharmacol Rev.77 (4) 100064.doi:10.1016/j.pharmr.2025.100064.PMID 40449125.
  11. ^"XWPharma Announces Positive Results from Phase 1 Clinical Trials of XW10172, in Development as Once-Nightly Therapy for Sleep Disorders in Patients with Neurodegenerative Diseases".GlobeNewswire News Room (Press release). 14 June 2021. Retrieved30 September 2025.
  12. ^Robinson DM, Keating GM (2007). "Sodium oxybate: a review of its use in the management of narcolepsy".CNS Drugs.21 (4):337–354.doi:10.2165/00023210-200721040-00007.PMID 17381187.
  13. ^Staud R (August 2011). "Sodium oxybate for the treatment of fibromyalgia".Expert Opin Pharmacother.12 (11):1789–1798.doi:10.1517/14656566.2011.589836.PMID 21679091.
  14. ^Roth T, Dauvilliers Y, Bogan RK, Plazzi G, Black J (February 2024). "Effects of oxybate dose and regimen on disrupted nighttime sleep and sleep architecture".Sleep Med.114:255–265.doi:10.1016/j.sleep.2023.12.015.PMID 38244463.
  15. ^Abad VC (June 2023). "Calcium, magnesium, potassium, and sodium oxybates oral solution for cataplexy or excessive daytime sleepiness associated with narcolepsy".Expert Opin Pharmacother.24 (8):875–885.doi:10.1080/14656566.2023.2204187.PMID 37060579.


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