List of investigational sleep apnea drugs

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 It is likely to become outdated with time.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) [1]
  • Mazdutide (IBI-362; LY-3305677; OXM-3) – glucagon-like peptide-1 (GLP-1) receptor agonist and glucagon receptor agonist – obesity-related sleep apnea [2]
  • Orforglipron (LY-3502970; OWL-833) – glucagon-like peptide-1 (GLP-1) receptor agonist – obesity-related sleep apnea [3]
  • 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 [4]

Phase 2/3

  • Acetazolamide/dronabinol (IHL-42X) – combination of acetazolamide (carbonic anhydrase inhibitor) and dronabinol (cannabinoid receptor agonist) [5]

Phase 2

  • AD-036 – undefined mechanism of action [6]
  • Atomoxetine/mineralocorticoid receptor antagonist (atomoxetine/antimineralocorticoid; AD-113) – combination of atomoxetine (norepinephrine reuptake inhibitor) and a mineralocorticoid receptor antagonist [7]
  • Atomoxetine/trazodone (trazodone/atomoxetine; AD-504) – combination of atomoxetine (norepinephrine reuptake inhibitor) and trazodone (various actions/hypnotic) [8]
  • BAY-2586116 – potassium channel blocker [9]
  • CX-1739 – ampakine (AMPA receptor positive allosteric modulator) [10]
  • Dronabinol low-dose (tetrahydrocannabinol; THC; PP-001) – cannabinoid CB1 and CB2 receptor agonist [11]
  • Dronabinol/palmitoylethanolamide (SCI-110; THX-OSA01; THX-RS01; THX-110; THX-TS01; THC/PEA) – combination of dronabinol (cannabinoid receptor agonist) and palmitoylethanolamine (various actions) [12]
  • Lorundrostat (MLS-101; MT-4129) – aldosterone synthase (CYP11B2) inhibitor [13]
  • Phentermine/topiramate (Qnexa; Qsiva; Qsymia; topiramate/phentermine; VI-0521) – combination of phentermine (norepinephrine releasing agent) and topiramate (various actions) [14]
  • Research programme: Sleep disordered breathing therapeutics - Shinogi-Apnimed Sleep Science – undefined mechanisms of action [15]
  • SASS-001 – purinergic P2X3 receptor antagonist [16]
  • Sivopixant (S-600918) – purinergic P2X3 receptor antagonist [17]
  • Sulthiame (SASS-002; sulthiame; Sultia; sultiame) – carbonic anhydrase inhibitor [18]
  • Trazodone/viloxazine (AD-816; viloxazine/trazodone) – combination of trazodone (various actions/hypnotic) and viloxazine (norepinephrine reuptake inhibitor) [19]

Phase 1

  • BAY-2925976 (KRP-S124) – α2C-adrenergic receptor antagonist [20]
  • Gal-475 – chemoreceptor cell modulator [21]
  • MOS-118 (AVE-0118) – potassium channel blocker [22]

Not under development

No development reported

  • Atomoxetine/orexin antagonist (AD-182) – combination of atomoxetine (norepinephrine reuptake inhibitor) and an orexin receptor antagonist [23]
  • Daridorexant (ACT-541468; nemorexant; Quviviq) – orexin OX1 and OX2 receptor antagonist [24]
  • Lemborexant (Dayvigo; E-2006; LEM) – orexin OX1 and OX2 receptor antagonist [25]
  • Research programme: AMPA receptor agonists - RespireRx (ampakines; CX compounds) – ampakines (AMPA receptor positive allosteric modulators) and brain-derived neurotrophic factor (BDNF) stimulants [26]
  • Research programme: sleep apnoea therapeutics - Apnimed – undefined mechanism of action [27]
  • Seltorexant (JNJ-42847922; JNJ-7922; MIN-202) – orexin OX2 receptor antagonist [28]
  • Vornorexant (ORN-0829; TS-142) – orexin OX1 and OX2 receptor antagonist [29]

Discontinued

  • AVE-0657 – sodium–hydrogen antiporter inhibitor [30]
  • Danavorexton (TAK-925) – orexin OX2 receptor agonist [31]
  • Dexloxiglumide (CR-2017) – cholecystokinin A (CCKA) receptor antagonist [32]
  • Gefapixant (AF-219; Gefzuris; Lyfnua; MK-7264; R-1646; RG-1646; RO-4926219) – purinergic P2X3 receptor antagonist [33]
  • Itriglumide (CR-2945) – cholecystokinin B (CCKB) receptor antagonist [34]
  • Sleep apnoea therapeutic (TASK channel blocker) – potassium channel blocker [35]

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 [36]

Off-label drugs

See also

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. ^ a b c d 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. ^ a b c d 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.