Chemistry:List of investigational restless legs syndrome drugs

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Short description: Investigational restless legs syndrome drugs
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This is a list of investigational restless legs syndrome drugs, or drugs that are currently under development for clinical use for the treatment of restless legs syndrome (RLS) but are not yet approved.

Chemical/generic names are listed first, with developmental code names, synonyms, and brand names in parentheses. The format of list items is "Name (Synonyms) – Mechanism of Action [Reference]".

This list was last comprehensively updated in September 2025. It is likely to become outdated with time.

Under development

Phase 3

  • Ferric carboxymaltose (Ferinject; Injectafer; Iron-dextri-maltose; Iroprem; Renegy; VIT-45; Z-213) – iron replacement [1]

Phase 2

  • BP-14979 (BP-1.4979) – dopamine D3 receptor partial agonist [2]
  • Ropinirole transdermal (Haruropi Tape; HP-3000) – dopamine D2-like receptor agonist [3]

Preclinical

  • ATH-399A (DWP-307399; HL-192) – nuclear receptor subfamily 4 group A member 2 (NR4A2) agonist [4]

Not under development

Suspended

  • Aplindore (DAB-452; Palindore; SLS-006; WAY-DAB-452) – dopamine D2-like receptor agonist [5]

No development reported

  • NLS-2 (NLS2) – iron replacement [6]
  • Research programme: cannabinoid-based therapeutics - Axim Biotechnologies (Cannabidiol/Gabapentin; Cannbleph) – various actions [7]

Discontinued

  • Entacapone (Comtan; Comtess; OR-611) – catechol O-methyltransferase (COMT) inhibitor [8]
  • IPX-159 – undefined mechanism of action [9]
  • Istradefylline (KW-6002; Nourianz; Nouriast) – adenosine A2A receptor antagonist [10]
  • Pregabalin (CI-1008; isobutylgaba; Lyrica; PD-144723) – gabapentinoid (α2δ subunit-containing voltage-gated calcium channel ligand) [11]
  • Radafaxine (GW-353162; (2S,3S)-hydroxybupropion) – norepinephrine–dopamine reuptake inhibitor (NDRI) [12]
  • Research programme: dopamine receptor agonists - DarPharma (DAR-0300) – dopamine receptor agonist [13] [14]
  • Safinamide (EMD-1195686; Equfina; FCE-26743; ME-2125; NW-1015; Onstryv; PNU-151774; Xadago; ZP-034) – monoamine oxidase MAO-B inhibitor and other actions [15]

Clinically used drugs

Approved drugs

  • Gabapentin enacarbil (ASP-8825; GSK-1838262; Horizant; Regnite; Solzira; XP-13512) – gabapentinoid (α2δ subunit-containing voltage-gated calcium channel ligand) [16]
  • Oxycodone/naloxone (naloxone/oxycodone; Targin; Targinact; Targiniq) – combination of oxycodone (μ-opioid receptor agonist) and naloxone (orally inactive opioid receptor antagonist) (only in severe and treatment-refractory cases) [17][1][2][3]
  • Pramipexole (BI-Sifrol; Daquiran; Mirapex; Mirapexin; Pexola; Sifrol; SND-919) – dopamine D2-like receptor agonist [18]
  • Ropinirole (Adartrel; Repreve; Requip; Ropinirole IR) – dopamine D2-like receptor agonist [19]
  • Rotigotine transdermal (Leganto; N-0437; N-0923; Neupro; Nubrenza; SPM-962) – dopamine D2-like receptor agonist [20]

Off-label drugs

See also

References

  1. ↑ "Intractable restless legs syndrome: role of prolonged-release oxycodone-naloxone". Neuropsychiatr Dis Treat 12: 417–425. 2016. doi:10.2147/NDT.S81186. PMID 26966363. 
  2. ↑ "Oxycodone/Naloxone PR: A Review in Severe Refractory Restless Legs Syndrome". CNS Drugs 29 (6): 511–518. June 2015. doi:10.1007/s40263-015-0254-y. PMID 26135898. 
  3. ↑ Gemignani, Franco; Parrino, Liborio; Melpignano, Andrea; Milioli, Giulia; Riccardi, Silvia (2016). "Restless legs syndrome: a new entity of neuropathic pain? Treatment with prolonged release oxycodone/naloxone combination". Journal of Parkinsonism and Restless Legs Syndrome: 23. doi:10.2147/JPRLS.S77560. ISSN 1927-7733. 
  4. ↑ 4.0 4.1 4.2 4.3 4.4 4.5 4.6 "The Management of Restless Legs Syndrome: An Updated Algorithm". Mayo Clin Proc 96 (7): 1921–1937. July 2021. doi:10.1016/j.mayocp.2020.12.026. PMID 34218864. 
  5. ↑ 5.0 5.1 5.2 5.3 5.4 5.5 5.6 "Treatment of restless legs syndrome and periodic limb movement disorder: an American Academy of Sleep Medicine systematic review, meta-analysis, and GRADE assessment". J Clin Sleep Med 21 (1): 153–199. January 2025. doi:10.5664/jcsm.11392. PMID 39324664. 
  6. ↑ "A Historical Overview of the Role of Benzodiazepines including Clonazepam in the Treatment of Adult Restless Legs Syndrome and Periodic Limb Movements in Sleep". Tremor Other Hyperkinet Mov (N Y) 14. 2024. doi:10.5334/tohm.824. PMID 38708125. 
  7. ↑ "Brain-iron deficiency models of restless legs syndrome". Exp Neurol 356. October 2022. doi:10.1016/j.expneurol.2022.114158. PMID 35779614. 
  8. ↑ "Iron supplementation for restless legs syndrome - A systematic review and meta-analysis". Eur J Intern Med 63: 34–41. May 2019. doi:10.1016/j.ejim.2019.02.009. PMID 30798983. 
  9. ↑ "The Appropriate Use of Opioids in the Treatment of Refractory Restless Legs Syndrome". Mayo Clin Proc 93 (1): 59–67. January 2018. doi:10.1016/j.mayocp.2017.11.007. PMID 29304922. 
  10. ↑ "A Narrative Review of the Lesser Known Medications for Treatment of Restless Legs Syndrome and Pathogenetic Implications for Their Use". Tremor Other Hyperkinet Mov (N Y) 13. 2023. doi:10.5334/tohm.739. PMID 36873914. 
  11. ↑ "Current and emerging pharmaceutical strategies for the treatment and management of restless legs syndrome". Expert Rev Neurother 24 (10): 997–1009. October 2024. doi:10.1080/14737175.2024.2385947. PMID 39082506. 
  12. ↑ "Pharmacological responsiveness of periodic limb movements in patients with restless legs syndrome: a systematic review and meta-analysis". J Clin Sleep Med 19 (4): 811–822. April 2023. doi:10.5664/jcsm.10440. PMID 36692194. 
  13. ↑ "Bupropion and restless legs syndrome: a randomized controlled trial". J Am Board Fam Med 24 (4): 422–428. 2011. doi:10.3122/jabfm.2011.04.100173. PMID 21737767. 
  14. ↑ "Cannabis for Restless Legs Syndrome". Cannabinoids and Sleep. Adv Exp Med Biol. 1297. 2021. pp. 173–181. doi:10.1007/978-3-030-61663-2_13. ISBN 978-3-030-61662-5. 




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