List of investigational sleep apnea drugs

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This is a list of investigational sleep apnea drugs, or drugs that are currently under development for clinical use in the treatment of sleep apnea 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 It is likely to become outdated with time.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

• Aroxybutynin/atomoxetine (AD-109; atomoxetine/aroxybutynin) – combination of aroxybutynin (muscarinic acetylcholine receptor antagonist/anticholinergic) and atomoxetine (norepinephrine reuptake inhibitor)
• Mazdutide (IBI-362; LY-3305677; OXM-3) – glucagon-like peptide-1 (GLP-1) receptor agonist and glucagon receptor agonist – obesity-related sleep apnea
• Orforglipron (LY-3502970; OWL-833) – glucagon-like peptide-1 (GLP-1) receptor agonist – obesity-related sleep apnea
• Retatrutide (LY-3437943) – glucagon-like peptide-1 (GLP-1) receptor agonist, glucagon receptor agonist, and gastric inhibitory polypeptide (GIP) receptor agonist – obesity-related sleep apnea

Phase 2/3

• Acetazolamide/dronabinol (IHL-42X) – combination of acetazolamide (carbonic anhydrase inhibitor) and dronabinol (cannabinoid receptor agonist)

Phase 2

• AD-036 – undefined mechanism of action
• Atomoxetine/mineralocorticoid receptor antagonist (atomoxetine/antimineralocorticoid; AD-113) – combination of atomoxetine (norepinephrine reuptake inhibitor) and a mineralocorticoid receptor antagonist
• Atomoxetine/trazodone (trazodone/atomoxetine; AD-504) – combination of atomoxetine (norepinephrine reuptake inhibitor) and trazodone (various actions/hypnotic)
• BAY-2586116 – potassium channel blocker
• CX-1739 – ampakine (AMPA receptor positive allosteric modulator)
• Dronabinol low-dose (tetrahydrocannabinol; THC; PP-001) – cannabinoid CB₁ and CB₂ receptor agonist
• Dronabinol/palmitoylethanolamide (SCI-110; THX-OSA01; THX-RS01; THX-110; THX-TS01; THC/PEA) – combination of dronabinol (cannabinoid receptor agonist) and palmitoylethanolamine (various actions)
• Lorundrostat (MLS-101; MT-4129) – aldosterone synthase (CYP11B2) inhibitor
• Phentermine/topiramate (Qnexa; Qsiva; Qsymia; topiramate/phentermine; VI-0521) – combination of phentermine (norepinephrine releasing agent) and topiramate (various actions)
• Research programme: Sleep disordered breathing therapeutics - Shinogi-Apnimed Sleep Science – undefined mechanisms of action
• SASS-001 – purinergic P2X3 receptor antagonist
• Sivopixant (S-600918) – purinergic P2X3 receptor antagonist
• Sulthiame (SASS-002; sulthiame; Sultia; sultiame) – carbonic anhydrase inhibitor
• Trazodone/viloxazine (AD-816; viloxazine/trazodone) – combination of trazodone (various actions/hypnotic) and viloxazine (norepinephrine reuptake inhibitor)

Phase 1

• BAY-2925976 (KRP-S124) – α_2C-adrenergic receptor antagonist
• Gal-475 – chemoreceptor cell modulator
• MOS-118 (AVE-0118) – potassium channel blocker

Not under development

No development reported

• Atomoxetine/orexin antagonist (AD-182) – combination of atomoxetine (norepinephrine reuptake inhibitor) and an orexin receptor antagonist
• Daridorexant (ACT-541468; nemorexant; Quviviq) – orexin OX₁ and OX₂ receptor antagonist
• Lemborexant (Dayvigo; E-2006; LEM) – orexin OX₁ and OX₂ receptor antagonist
• Research programme: AMPA receptor agonists - RespireRx (ampakines; CX compounds) – ampakines (AMPA receptor positive allosteric modulators) and brain-derived neurotrophic factor (BDNF) stimulants
• Research programme: sleep apnoea therapeutics - Apnimed – undefined mechanism of action
• Seltorexant (JNJ-42847922; JNJ-7922; MIN-202) – orexin OX₂ receptor antagonist
• Vornorexant (ORN-0829; TS-142) – orexin OX₁ and OX₂ receptor antagonist

Discontinued

• AVE-0657 – sodium–hydrogen antiporter inhibitor
• Danavorexton (TAK-925) – orexin OX₂ receptor agonist
• Dexloxiglumide (CR-2017) – cholecystokinin A (CCK_A) receptor antagonist
• Gefapixant (AF-219; Gefzuris; Lyfnua; MK-7264; R-1646; RG-1646; RO-4926219) – purinergic P2X3 receptor antagonist
• Itriglumide (CR-2945) – cholecystokinin B (CCK_B) receptor antagonist
• Sleep apnoea therapeutic (TASK channel blocker) – potassium channel blocker

Clinically used drugs

Approved drugs

• Tirzepatide (LY-3298176; Mounjaro; Zepbound) – glucagon-like peptide-1 (GLP-1) receptor agonist and gastric inhibitory polypeptide (GIP) receptor agonist – obesity-related sleep apnea

Off-label drugs

• Acetazolamide (Diamox) – carbonic anhydrase inhibitor ^[1]
• Atomoxetine (Strattera) – norepinephrine reuptake inhibitor (NRI) ^{[2] [3]}
• Eszopiclone (Lunesta) – GABA_A receptor positive allosteric modulator and nonbenzodiazepine/Z-drug ^{[3] [2]}
• Oxybutynin (Ditropan) – muscarinic acetylcholine receptor antagonist (anticholinergic) ^[2]
• Pimavanserin (Nuplaizid) – serotonin 5-HT_2A receptor antagonist ^[3]
• Sodium oxybate (GHB; Xyrem) – GABA_B receptor agonist and GHB receptor agonist ^[2]
• Trazodone (Desyrel) – various actions ^[3]
• Weight-loss drugs (e.g., liraglutide, semaglutide) – obesity-related sleep apnea ^{[4] [5]}

See also

• Lists of investigational drugs

References

1. Schmickl CN, Landry SA, Orr JE, Chin K, Murase K, Verbraecken J, Javaheri S, Edwards BA, Owens RL, Malhotra A (December 2020). "Acetazolamide for OSA and Central Sleep Apnea: A Comprehensive Systematic Review and Meta-Analysis". Chest. 158 (6): 2632–2645. doi:10.1016/j.chest.2020.06.078. PMC   7768933 . PMID   32768459.
2. Nobre ML, Sarmento AC, de Oliveira PF, Wanderley FF, Diniz Júnior J, Gonçalves AK (2024). "Pharmacological treatment for obstructive sleep apnea: A systematic review and meta-analysis". Clinics (Sao Paulo). 79 100330. doi:10.1016/j.clinsp.2024.100330. PMC   10869242 . PMID   38341903.
3. Luu S, Chan DE, Marshall NS, Phillips CL, Grunstein RR, Yee BJ (September 2025). "Pharmacotherapy for obstructive sleep apnea: a critical review of randomized placebo-controlled trials". Sleep Med Rev. 84 102169. doi:10.1016/j.smrv.2025.102169. PMID   40974973.
4. El-Solh AA, Gould E, Aibangbee K, Jimerson T, Hartling R (January 2025). "Current perspectives on the use of GLP-1 receptor agonists in obesity-related obstructive sleep apnea: a narrative review". Expert Opin Pharmacother. 26 (1): 51–62. doi:10.1080/14656566.2024.2437525. PMID   39621418.
5. Marra S, Arnaldi D, Nobili L (November 2019). "The pharmacotherapeutic management of obstructive sleep apnea". Expert Opin Pharmacother. 20 (16): 1981–1991. doi:10.1080/14656566.2019.1652271. PMID   31487204.

External links

• AdisInsight - Springer