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Latest revision as of 22:29, 28 January 2026
Investigational restless legs syndrome drugs
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 It is likely to become outdated with time.
- Ferric carboxymaltose (Ferinject; Injectafer; Iron-dextri-maltose; Iroprem; Renegy; VIT-45; Z-213) – iron replacement [1]
- BP-14979 (BP-1.4979) – dopamine D3 receptor partial agonist [2]
- Ropinirole transdermal (Haruropi Tape; HP-3000) – dopamine D2-like receptor agonist [3]
Not under development
[edit]
No development reported
[edit]
- NLS-2 (NLS2) – iron replacement [6]
- Research programme: cannabinoid-based therapeutics – Axim Biotechnologies (Cannabidiol/Gabapentin; Cannbleph) – various actions [7]
- 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
[edit]
- 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]
- Benzodiazepines (GABAA receptor positive allosteric modulators) (e.g., clonazepam)[4][5]
- Dopamine precursors (indirect dopamine receptor agonists) (e.g., carbidopa/levodopa)[4][5]
- Dopamine D2-like receptor agonists (e.g., cabergoline, pergolide)[5][4]
- Gabapentinoids (α2δ subunit-containing voltage-gated calcium channel ligands) (e.g., gabapentin, pregabalin)[5][4]
- Iron supplements (e.g., ferrous sulfate)[5][4][7][8]
- Opioids (μ-opioid receptor agonists) (e.g., tramadol, codeine, morphine, oxycodone, hydrocodone, methadone, buprenorphine) (only in severe and treatment-refractory cases)[5][4][9]
- Others (e.g., amantadine, baclofen, bupropion, cannabis/cannabinoids, carbamazepine, clonidine, corticosteroids, dipyridamole, ketamine, lamotrigine, levetiracetam, orphenadrine, oxcarbazepine, perampanel, physostigmine, rasagiline, rifaximin, selegiline, topiramate, valproic acid)[5][4][10][11][12][13][14]
- ^ de Biase S, Valente M, Gigli GL (2016). “Intractable restless legs syndrome: role of prolonged-release oxycodone-naloxone”. Neuropsychiatr Dis Treat. 12: 417–425. doi:10.2147/NDT.S81186. PMC 4770072. PMID 26966363.
- ^ Frampton JE (June 2015). “Oxycodone/Naloxone PR: A Review in Severe Refractory Restless Legs Syndrome”. CNS Drugs. 29 (6): 511–518. doi:10.1007/s40263-015-0254-y. PMID 26135898.
- ^ 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. ISSNÂ 1927-7733.
- ^ a b c d e f g Silber MH, Buchfuhrer MJ, Earley CJ, Koo BB, Manconi M, Winkelman JW (July 2021). “The Management of Restless Legs Syndrome: An Updated Algorithm”. Mayo Clin Proc. 96 (7): 1921–1937. doi:10.1016/j.mayocp.2020.12.026. PMID 34218864.
- ^ a b c d e f g Winkelman JW, Berkowski JA, DelRosso LM, Koo BB, Scharf MT, Sharon D, Zak RS, Kazmi U, Carandang G, Falck-Ytter Y, Shelgikar AV, Trotti LM, Walters AS (January 2025). “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. doi:10.5664/jcsm.11392. PMC 11701280. PMID 39324664.
- ^ Earley CJ, Jones BC, Ferré S (October 2022). “Brain-iron deficiency models of restless legs syndrome”. Exp Neurol. 356 114158. doi:10.1016/j.expneurol.2022.114158. PMC 9357217. PMID 35779614.
- ^ Avni T, Reich S, Lev N, Gafter-Gvili A (May 2019). “Iron supplementation for restless legs syndrome – A systematic review and meta-analysis”. Eur J Intern Med. 63: 34–41. doi:10.1016/j.ejim.2019.02.009. PMID 30798983.
- ^ Silber MH, Becker PM, Buchfuhrer MJ, Earley CJ, Ondo WG, Walters AS, Winkelman JW (January 2018). “The Appropriate Use of Opioids in the Treatment of Refractory Restless Legs Syndrome”. Mayo Clin Proc. 93 (1): 59–67. doi:10.1016/j.mayocp.2017.11.007. PMID 29304922.
- ^ Yeh PG, Spruyt K, DelRosso LM, Walters AS (2023). “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 7. doi:10.5334/tohm.739. PMCÂ 9983500. PMIDÂ 36873914.
- ^ Burini A, Pellitteri G, Merlino G, Nilo A, Tereshko Y, Dolso P, Gigli GL, Valente M (October 2024). “Current and emerging pharmaceutical strategies for the treatment and management of restless legs syndrome”. Expert Rev Neurother. 24 (10): 997–1009. doi:10.1080/14737175.2024.2385947. PMID 39082506.
- ^ Riccardi S, Ferri R, Garbazza C, Miano S, Manconi M (April 2023). “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. doi:10.5664/jcsm.10440. PMC 10071388. PMID 36692194.
- ^ Bayard M, Bailey B, Acharya D, Ambreen F, Duggal S, Kaur T, Rahman ZU, Roller K, Tudiver F (2011). “Bupropion and restless legs syndrome: a randomized controlled trial”. J Am Board Fam Med. 24 (4): 422–428. doi:10.3122/jabfm.2011.04.100173. PMID 21737767.
- ^ Ghorayeb I (2021). “Cannabis for Restless Legs Syndrome”. Cannabinoids and Sleep. Adv Exp Med Biol. Vol. 1297. pp. 173–181. doi:10.1007/978-3-030-61663-2_13. ISBN 978-3-030-61662-5. PMID 33537945.
