Valiloxybate

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 receptor agonist; GHB receptor agonist; Hypnotic
ATC code
  • None
Identifiers
  • 4-[(2S)-2-amino-3-methylbutanoyl]oxybutanoic acid
CAS Number
PubChem CID
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 name XW-10172) is an extended-release prodrug of γ-hydroxybutyrate (GHB; oxybate) which is under development for the treatment of narcolepsy.[1][3][4][5][6] It is also being investigated for treatment of excessive daytime sleepiness (EDS) in people with Parkinson's disease.[7] The drug is taken orally once per night.[1][4][5][8][6]

Pharmacology

It is an amino acid (L-valine) ester prodrug of GHB,[6][2] which itself acts as a GABAB and GHB receptor agonist.[9][10] Relative to administration of GHB itself, valiloxybate showed a delayed time to peak levels and an extended duration 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 short elimination half-life.[12][13][14] In addition, unlike sodium oxybate, valiloxybate contains no sodium or cation, and hence avoids excessive sodium intake.[6][15]

History

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

See also

References

  1. ^ a b c d e "Valiloxybate". AdisInsight. 28 September 2025. Retrieved 30 September 2025.
  2. ^ a b "VALILOXYBATE". Inxight Drugs. Retrieved 30 September 2025.
  3. ^ "Valiloxibic acid". AdisInsight. 28 July 2022. Retrieved 30 September 2025.
  4. ^ a b Roth 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. ^ a b Abad 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. ^ a b c d e f Canafax 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. Retrieved 30 September 2025.
  7. ^ a b Wolff 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. Retrieved 30 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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