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List of investigational chronobiotics

Investigational chronobiotic drugs From Wikipedia, the free encyclopedia

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 It is likely to become outdated with time.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

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