Chemistry:List of investigational chronobiotics

From HandWiki
Short description: Investigational chronobiotic drugs
This is a dynamic list and may never be able to satisfy particular standards for completeness. You can help by expanding it with reliably sourced entries.

This is a list of investigational chronobiotics, or drugs that are currently under development for clinical use as chronobiotics—that is, for the treatment of circadian rhythm sleep disorders—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 It is likely to become outdated with time.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

  • Solriamfetol (ADX-N05; ARL-N05; JZP-110; SKL-N05; Sunosi) – norepinephrine–dopamine reuptake inhibitor (NDRI) and trace amine-associated receptor 1 (TAAR1) agonist[1]

Phase 2

  • Lemborexant (LEM; Dayvigo; E-2006) – orexin OX1 and OX2 receptor antagonist[2]

Preclinical

  • CT-1500 (CT1500) – adenosine A1 and A2A receptor antagonist[3][4]

Not under development

No development reported

  • TIK-301 (LY-156735; PD-6735; 6-chloro-β-methylmelatonin) – melatonin MT1 and MT2 receptor agonist and serotonin 5-HT2B and 5-HT2C receptor antagonist[5]

Discontinued

  • BIIB-118 (PF-5251749; PF-05251749) – casein kinase 1 epsilon (CK1ε) and delta (CK1δ) inhibitor[6]
  • LML-134 (LML134) – histamine H3 receptor antagonist[7]
  • Ramelteon (Rozerem; TAK-375) – melatonin MT1 and MT2 receptor agonist[8]

Clinically used drugs

Approved drugs

  • Armodafinil (Nuvigil) – atypical dopamine reuptake inhibitor – specifically for shift work sleep disorder[9]
  • Modafinil (Provigil) – atypical dopamine reuptake inhibitor – specifically for shift work sleep disorder[9][10][11]
  • Tasimelteon (BMS-214778; Hetlioz; VEC-162) – melatonin MT1 and MT2 receptor agonist[12]

Off-label drugs

See also

References

  1. ↑ "Solriamfetol - Jazz Pharmaceuticals/SK Biopharmaceuticals - AdisInsight". https://adisinsight.springer.com/drugs/800030225. 
  2. ↑ "Lemborexant - Eisai - AdisInsight". https://adisinsight.springer.com/drugs/800035210. 
  3. ↑ "CT 1500 - AdisInsight". https://adisinsight.springer.com/drugs/800065840. 
  4. ↑ "The regulation of circadian entrainment in mice by the adenosine the A 2A /A 1 receptor antagonist CT1500". Front Physiol 13. 2022. doi:10.3389/fphys.2022.1085217. PMID 36605898. 
  5. ↑ "LY 156735 - AdisInsight". https://adisinsight.springer.com/drugs/800016852. 
  6. ↑ "BIIB 118 - AdisInsight". https://adisinsight.springer.com/drugs/800042502. 
  7. ↑ "LML 134 - AdisInsight". https://adisinsight.springer.com/drugs/800041905. 
  8. ↑ "Ramelteon - Takeda - AdisInsight". https://adisinsight.springer.com/drugs/800014547. 
  9. ↑ 9.0 9.1 9.2 "Pharmacological interventions for sleepiness and sleep disturbances caused by shift work". Cochrane Database Syst Rev 2014 (8). August 2014. doi:10.1002/14651858.CD009776.pub2. PMID 25113164. 
  10. ↑ "Modafinil: a review of its use in excessive sleepiness associated with obstructive sleep apnoea/hypopnoea syndrome and shift work sleep disorder". CNS Drugs 19 (9): 785–803. 2005. doi:10.2165/00023210-200519090-00005. PMID 16142993. 
  11. ↑ "Approved and investigational uses of modafinil: an evidence-based review". Drugs 68 (13): 1803–1839. 2008. doi:10.2165/00003495-200868130-00003. PMID 18729534. 
  12. ↑ "Tasimelteon - Vanda Pharmaceuticals - AdisInsight". https://adisinsight.springer.com/drugs/800024285. 
  13. ↑ "Aripiprazole is effective for treatment of delayed sleep phase syndrome". Clin Neuropharmacol 37 (4): 123–124. 2014. doi:10.1097/WNF.0000000000000035. PMID 24992089. 
  14. ↑ "Low dose of aripiprazole advanced sleep rhythm and reduced nocturnal sleep time in the patients with delayed sleep phase syndrome: an open-labeled clinical observation". Neuropsychiatr Dis Treat 14: 1281–1286. 2018. doi:10.2147/NDT.S158865. PMID 29849459. 
  15. ↑ "Clinical Sleep-Wake Disorders II: Focus on Insomnia and Circadian Rhythm Sleep Disorders". Handb Exp Pharmacol. Handbook of Experimental Pharmacology 253: 261–276. 2019. doi:10.1007/164_2017_40. ISBN 978-3-030-11270-7. PMID 28707143. 
  16. ↑ "Comparative Review of Approved Melatonin Agonists for the Treatment of Circadian Rhythm Sleep-Wake Disorders". Pharmacotherapy 36 (9): 1028–1041. September 2016. doi:10.1002/phar.1822. PMID 27500861. 
  17. ↑ "Practice parameters for the clinical evaluation and treatment of circadian rhythm sleep disorders. An American Academy of Sleep Medicine report". Sleep 30 (11): 1445–1459. November 2007. doi:10.1093/sleep/30.11.1445. PMID 18041479. 
  18. ↑ Morgenthaler, Timothy; Kolla; Auger (2012). "Circadian rhythm sleep disorders". ChronoPhysiology and Therapy: 19. doi:10.2147/CPT.S21937. ISSN 2230-2026. 
  19. ↑ "Circadian Rhythm Sleep-Wake Disorders". Psychiatr Clin North Am 38 (4): 805–823. December 2015. doi:10.1016/j.psc.2015.07.012. PMID 26600110. 




Retrieved from "https://handwiki.org/wiki/index.php?title=Chemistry:List_of_investigational_chronobiotics&oldid=4189374"