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 It is likely to become outdated with time.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
Phase 2 Lemborexant (LEM; Dayvigo; E-2006) – orexin OX1 and OX2 receptor antagonist
Preclinical CT-1500 (CT1500) – adenosine A1 and A2A receptor antagonist
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
Discontinued BIIB-118 (PF-5251749; PF-05251749) – casein kinase 1 epsilon (CK1ε) and delta (CK1δ) inhibitor LML-134 (LML134) – histamine H3 receptor antagonist Ramelteon (Rozerem; TAK-375) – melatonin MT1 and MT2 receptor agonist
Clinically used drugs Approved drugs Armodafinil (Nuvigil) – atypical dopamine reuptake inhibitor – specifically for shift work sleep disorder Modafinil (Provigil) – atypical dopamine reuptake inhibitor – specifically for shift work sleep disorder Tasimelteon (BMS-214778; Hetlioz; VEC-162) – melatonin MT1 and MT2 receptor agonist
Off-label drugs Antipsychotics (e.g., aripiprazole) Hypnotics (e.g., antihistamines, trazodone, orexin receptor antagonists, benzodiazepines, Z-drugs) Melatonin receptor agonists (e.g., melatonin, ramelteon, agomelatine) Vitamins (e.g., vitamin B12) Wakefulness-promoting agents and stimulants (e.g., caffeine, modafinil, armodafinil)
See also Chronobiotic List of investigational drugs List of investigational insomnia drugs List of investigational narcolepsy and hypersomnia drugs
References
External links AdisInsight - Springer