This is a list of investigational chronobiotics, or drugs that are currently under development for clinical use as chronobioticsâÂÂthat is, for the treatment of circadian rhythm sleep disordersâÂÂbut 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) â 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 It is likely to become outdated with time.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) â norepinephrineâÂÂdopamine reuptake inhibitor (NDRI) and trace amine-associated receptor 1 (TAAR1) agonist
Phase 2
- Lemborexant (LEM; Dayvigo; E-2006) â orexin OX<sub>1</sub> and OX<sub>2</sub> receptor antagonist
Preclinical
- CT-1500 (CT1500) â adenosine A<sub>1</sub> and A<sub>2A</sub> receptor antagonist
Not under development
No development reported
- TIK-301 (LY-156735; PD-6735; 6-chloro-ò-methylmelatonin) â melatonin MT<sub>1</sub> and MT<sub>2</sub> receptor agonist and serotonin 5-HT<sub>2B</sub> and 5-HT<sub>2C</sub> receptor antagonist
Discontinued
- BIIB-118 (PF-5251749; PF-05251749) â casein kinase 1 epsilon (CK1õ) and delta (CK1ô) inhibitor
- LML-134 (LML134) â histamine H<sub>3</sub> receptor antagonist
- Ramelteon (Rozerem; TAK-375) â melatonin MT<sub>1</sub> and MT<sub>2</sub> receptor agonist
Clinically used drugs
Approved drugs
- Armodafinil (Nuvigil) â atypical dopamine reuptake inhibitor â specifically for shift work sleep disorder
- Modafinil (Provigil) â atypical dopamine reuptake inhibitor â specifically for shift work sleep disorder
- Tasimelteon (BMS-214778; Hetlioz; VEC-162) â melatonin MT<sub>1</sub> and MT<sub>2</sub> 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 B<sub>12</sub>)
- Wakefulness-promoting agents and stimulants (e.g., caffeine, modafinil, armodafinil)
See also
References
External links