science

List of investigational insomnia drugs

List of investigational insomnia drugs is a science topic covered in the lgStudy science library. This page brings together a partial reference excerpt, illustrations, worked examples, real-world applications and a short study plan, so you can understand List of investigational insomnia drugs rather than just read about it. In short: This is a list of investigational insomnia drugs, or drugs that are currently under development for clinical use for the treatment of insomnia but are not yet approved. They may also be referred to as investigational hypnotics.

Key takeaways

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Reference excerpt

This is a list of investigational insomnia drugs, or drugs that are currently under development for clinical use for the treatment of insomnia but are not yet approved. They may also be referred to as investigational hypnotics. 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 It is likely to become outdated with time.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

Preregistration Tasimelteon (Hetlioz; BMS-214778; VEC-162) – melatonin MT1 and MT2 receptor agonist

Phase 3 Brexpiprazole (Rexulti; Lu-AF41156; OPC-34712; OPDC-34712) – atypical antipsychotic (non-selective monoamine receptor modulator) Cannabidiol soft-gel (CBD soft-gel; CBD-TPM) — cannabinoid and various actions Diphenhydramine/lorazepam/zolpidem (SM-1; SM1) – combination of diphenhydramine (antihistamine and anticholinergic), lorazepam (benzodiazepine and GABAA receptor positive allosteric modulator), and zolpidem (nonbenzodiazepine/Z-drug and GABAA receptor positive allosteric modulator) Zuranolone (BIIB-125; S-812217; SAGE-217; SGE-797; Zurzuvae) – GABAA receptor positive allosteric modulator and neurosteroid

Phase 2 Dexmedetomidine buccal (RE-03) — α2-adrenergic receptor agonist Lumateperone (Caplyta; ITI-007; ITI-722) – atypical antipsychotic (non-selective monoamine receptor modulator) Pimavanserin (Nuplazid; ACP-103; BVF-048) – serotonin 5-HT2A receptor antagonist Piromelatine (Neu-P11) – melatonin MT1 and MT2 receptor agonist, serotonin 5-HT1A and 5-HT1D receptor agonist, and serotonin 5-HT2B receptor antagonist Seltorexant (JNJ-42847922; JNJ-7922; MIN-202) – orexin OX2 receptor antagonist Sunobinop (IMB-115; IT-1315; RSC117957; S-117957; V-117957) – nociceptin receptor agonist Trazodone extended-release (AF-1161; DDS-04A; Oleptro; Triticum AC; Trittico) – serotonin 5-HT1A receptor partial agonist, serotonin 5-HT2A and 5-HT2C receptor antagonist, α1- and α2-adrenergic receptor antagonist, weak serotonin reuptake inhibitor, and other actions

Phase 1/2 SVT-4A1011 – microbiome modulator and live microbial therapeutic

Phase 1 Ramelteon controlled-release – melatonin MT1 and MT2 receptor agonist

Preclinical APSTZD (APS-TZD) – undefined mechanism of action HS-10506 – orexin OX2 receptor antagonist TPT-0601 – fatty acid amide hydrolase (FAAH) inhibitor YZG-331 – adenosine receptor agonist

Research Trazodone (TrazoFlex-24; TrazoFlex-CR; TrazoFlex) – serotonin 5-HT1A receptor partial agonist, serotonin 5-HT2A and 5-HT2C receptor antagonist, α1- and α2-adrenergic receptor antagonist, weak serotonin reuptake inhibitor, and other actions

Phase unknown Midazolam sublingual film – GABAA receptor positive allosteric modulator and benzodiazepine OP-010 (OP010) – undefined mechanism of action Zolpidem extended-release – GABAA receptor positive allosteric modulator and nonbenzodiazepine/Z-drug

Not under development

Suspended Osemozotan (MKC-242; MN-305) – serotonin 5-HT1A receptor agonist

No development reported Filorexant (MK-6096) – orexin OX1 and OX2 receptor antagonist HEC-83518 – orexin receptor antagonist IN-AQUL-001 – undefined mechanism of action JNJ-48816274 – orexin OX2 receptor antagonist Lirequinil (RO-413696) – GABAA receptor positive allosteric modulator and nonbenzodiazepine/benzoquinolizinone Lorediplon (GF-015535-00) – GABAA receptor positive allosteric modulator and nonbenzodiazepine/pyrazolopyrimidine MK-1064 – orexin OX2 receptor antagonist Research programme: psychophysiological insomnia therapeutics - Neurim Pharmaceuticals – melatonin and serotonin receptor agonists Zolpidem topical gel (TR-396) – GABAA receptor positive allosteric modulator and nonbenzodiazepine/Z-drug

Discontinued ACT-462206 – orexin OX1 and OX2 receptor antagonist Adipiplon (NG-273) – GABAA receptor positive allosteric modulator ADX-10061 (NNC 01-0687; CEE-03-310; NNC-687) – dopamine D1 receptor antagonist Almorexant (ACT-078573) – orexin OX1 and OX2 receptor antagonist ANPH-101 – undefined mechanism of action Atagabalin (PD-0200390) – gabapentinoid (α2δ voltage-gated calcium channel ligand) Eplivanserin (Ciltyri; Sliwens; SR–46349; SR–46349B; SR–46615A) – serotonin 5-HT2A receptor antagonist Esmirtazapine (ORG-50081; SCH-900265; (S)-mirtazapine) – histamine H1 receptor antagonist, serotonin 5-HT2 receptor antagonist, and α2-adrenergic receptor antagonist Gaboxadol (LU-02030; LU-2-030; MK-0928; OV-101; THIP) – GABAA receptor agonist GT-2203 – histamine H3 receptor agonist Indiplon (NBI-34060) – GABAA receptor positive allosteric modulator and nonbenzodiazepine/pyrazolopyrimidine LY-2624803 (HY-10275) – histamine H1 receptor inverse agonist and serotonin 5-HT2A receptor antagonist Nabilone (Cesamet) – cannabinoid CB1 and CB2 receptor agonist NBI-75043 – antihistamine (histamine H1 receptor antagonist) Nelotanserin (APD-125; RVT-102) – serotonin 5-HT2A receptor antagonist NGD-962 (NGD 96-2) – GABAA receptor modulator Paliperidone (Invega; JNS-007ER; RO-76477; 9-hydroxyrisperidone) – atypical antipsychotic (non-selective monoamine receptor modulator) PD-0299685 (PF-299685) – gabapentinoid (α2δ voltage-gated calcium channel ligand) Pruvanserin (EMD-281014; LY-2422347; LSN-2411347) – serotonin 5-HT2A receptor antagonist Remimazolam (HR-7056; Byfavo) – GABAA receptor positive allosteric modulator and benzodiazepine Seganserin (R-56413) – serotonin 5-HT2A and 5-HT2C receptor antagonist Suvecaltamide (CX-8998; JZP-385; MK-8998) – T-type calcium channel inhibitor Tasipimidine (ODM-105) – α2A-adrenergic receptor agonist Tesamorelin (Egrifta; MDVTM; TH-9507; ThGRF 1-44) – growth hormone-releasing hormone (GHRH) receptor agonist Tiagabine (A-70569; CEP-6671; Gabitril; NO-050328; NO-328) – GABA transporter 1 (GAT-1) blocker and GABA reuptake inhibitor Triazolam intranasal (Hypnostat; TGAR01H) – GABAA receptor positive allosteric modulator and benzodiazepine Volinanserin (M-100907; MDL-100907) – serotonin 5-HT2A receptor antagonist

Formal development never or not yet started Histone deacetylase inhibitors (HDACi) (e.g., butyric acid (butyrate), tributyrin)

Clinically used drugs

Approved drugs

GABAA receptor positive allosteric modulators Benzodiazepines

… excerpt ends here. Continue reading the full article.

Worked examples

Example 1 — a first encounter with List of investigational insomnia drugs

Start with the simplest possible case. Write down what List of investigational insomnia drugs claims or describes in one sentence, then invent the smallest concrete situation in which that sentence is true. In science, the smallest case is usually a single object, a single equation or a single measurement. Check that every symbol or term in your sentence has a meaning in that case.

Example 2 — changing one variable

Take the situation from Example 1 and change exactly one quantity: double it, halve it, or set it to zero. Predict what should happen to List of investigational insomnia drugs before you calculate. Comparing your prediction with the result is the fastest way to find out whether you understand the idea or only the words.

Example 3 — an exam-style question

Typical questions about List of investigational insomnia drugs ask you to (a) state it precisely, (b) apply it to given data, and (c) explain a limitation. Practise writing all three answers in under five minutes; the third part is what separates a full-mark answer from an average one.

Applications of List of investigational insomnia drugs

In research: List of investigational insomnia drugs appears in science research whenever the underlying quantities have to be modelled precisely. Papers usually cite it as a starting assumption and then explore where it breaks down.
In technology and industry: Engineering practice reuses List of investigational insomnia drugs in design rules, simulations and safety margins. Knowing the idea lets you read a specification sheet and understand why the numbers look the way they do.
In the classroom: List of investigational insomnia drugs is common in secondary-school and first-year university syllabi. It links to neighbouring topics Hypnotics, Lists of investigational drugs, Sedatives, so understanding it makes those chapters shorter.
In everyday life: Look for List of investigational insomnia drugs outside the textbook — in sport, cooking, traffic, electronics or the sky above you. An example you found yourself is remembered far longer than one you were given.

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Frequently asked questions

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Read the excerpt, restate it from memory, then work through the examples and applications listed on this page. The five-step study plan above takes about twenty minutes.

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