suvorexant: an orexin receptor antagonist; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
suvorexant : An aromatic amide obtained by formal condensation of the carboxy group of 5-methyl-2-(2H-1,2,3-triazol-2-yl)benzoic acid with the secondary amino group of 5-chloro-2-[(5R)-5-methyl-1,4-diazepan-1-yl]-1,3-benzoxazole. An orexin receptor antagonist used for the management of insomnia. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]
| ID Source | ID |
|---|---|
| PubMed CID | 24965990 |
| CHEMBL ID | 1083659 |
| CHEBI ID | 82698 |
| SCHEMBL ID | 1586289 |
| MeSH ID | M0549250 |
| Synonym |
|---|
| suvorexant; mk 4305 |
| HY-10807 |
| CAS:1030377-33-3;MK-4305 |
| gtpl2890 |
| mk 4305 |
| belsomra |
| mk-4305 |
| suvorexant |
| mk4305 |
| chebi:82698 , |
| CHEMBL1083659 , |
| [(7r)-4-(5-chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2h-1,2,3-triazol-2-yl)phenyl]methanone |
| bdbm50318701 |
| D10082 |
| belsomra (tn) |
| suvorexant (jan/usan) |
| methanone, ((7r)-4-(5-chloro-2-benzoxazolyl)hexahydro-7-methyl-1h-1,4-diazepin-1-yl)(5-methyl-2-(2h-1,2,3-triazol-2-yl)phenyl)- |
| unii-081l192fo9 |
| ((7r)-4-(5-chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl)(5-methyl-2-(2h-1,2,3-triazol-2-yl)phenyl)methanone |
| 1030377-33-3 |
| suvorexant [usan:inn] |
| 081l192fo9 , |
| (4-(5-chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl)(5-methyl-2-(2h-1,2,3-triazol-2-yl)phenyl)methanone |
| BCP0726000197 |
| belsomra component suvorexant |
| suvorexant [usan] |
| suvorexant [orange book] |
| suvorexant [vandf] |
| suvorexant [mi] |
| suvorexant [who-dd] |
| suvorexant component of belsomra |
| suvorexant [inn] |
| suvorexant [jan] |
| CS-0614 |
| AKOS022185167 |
| suv , |
| SCHEMBL1586289 |
| 5-chloro-2-[(5r)-5-methyl-4-[5-methyl-2-(2h-1,2,3-triazol-2-yl)benzoyl]-1,4-diazepan-1-yl]-1,3-benzoxazole |
| AC-30276 |
| FT-0697203 |
| DTXSID90145616 , |
| DB09034 |
| J-690010 |
| mfcd22377755 |
| EX-A211 |
| JYTNQNCOQXFQPK-MRXNPFEDSA-N |
| AS-74879 |
| SW219649-1 |
| suvorexant (mk-4305) |
| (r)-(4-(5-chlorobenzo[d]oxazol-2-yl)-7-methyl-1,4-diazepan-1-yl)(5-methyl-2-(2h-1,2,3-triazol-2-yl)phenyl)methanone. |
| Q7650517 |
| AMY337 |
| dtxcid0068107 |
| suvorexantum |
| n05cm19 |
Suvorexant (Belsomra) is an orexin receptor antagonist with Food and Drug Administration (FDA) approval for the treatment of adult insomnia. It improves sleep onset and maintenance as well as subjective measures of quality of sleep.
Over 1 year, 362 (69%) of 521 patients treated with suvorexant experienced any adverse events compared with 164 (64%) of 258 treated with placebo.
| Excerpt | Reference | Relevance |
|---|---|---|
| " This second column in the series focuses on the metabolism of each of the 3 drugs by the cytochrome P450 enzyme CYP3A, guidance for using these agents in combination with drugs that are CYP3A inhibitors or inducers, and how to adjust dosing in patients with comorbid conditions such as hepatic or renal impairment." | ( Comparative Pharmacology of the 3 Marketed Dual Orexin Antagonists-Daridorexant, Lemborexant, and Suvorexant-Part 2. Principal Drug Metabolizing Enzyme, Drug-Drug Interactions, and Effects of Liver and Renal Impairment on Metabolism. Preskorn, SH, 2023) | 1.13 |
| Excerpt | Reference | Relevance |
|---|---|---|
| " Suvorexant (MK-4305) is a potent, selective, and orally bioavailable antagonist of OX(1)R and OX(2)R currently under clinical investigation as a novel therapy for insomnia." | ( Promotion of sleep by suvorexant-a novel dual orexin receptor antagonist. Breslin, MJ; Coleman, PJ; Cox, CD; Cui, D; Doran, SM; Fox, SV; Garson, SL; Gotter, AL; Harrell, CM; Reiss, DR; Renger, JJ; Stevens, J; Tannenbaum, PL; Winrow, CJ, 2011) | 1.59 |
| " These batches were evaluated in a relative bioavailability clinical study in healthy volunteers." | ( Development of In Vitro-In Vivo Correlation for Amorphous Solid Dispersion Immediate-Release Suvorexant Tablets and Application to Clinically Relevant Dissolution Specifications and In-Process Controls. Hermans, A; Kesisoglou, F; Miller, J; Neu, C; Palcza, J; Yee, KL, 2015) | 0.64 |
Suvorexant was generally well tolerated after single and multiple dosing for 14 days. Dosed orally SuvoreXant significantly and dose-dependently reduced locomotor activity and promoted sleep in rats (10, 30, and 100 mg/kg), dogs (1 and 3 mg/ kg), and rhesus monkeys.
| Excerpt | Relevance | Reference |
|---|---|---|
| " Dosed orally Suvorexant significantly and dose-dependently reduced locomotor activity and promoted sleep in rats (10, 30, and 100 mg/kg), dogs (1 and 3 mg/kg), and rhesus monkeys (10 mg/kg)." | ( Promotion of sleep by suvorexant-a novel dual orexin receptor antagonist. Breslin, MJ; Coleman, PJ; Cox, CD; Cui, D; Doran, SM; Fox, SV; Garson, SL; Gotter, AL; Harrell, CM; Reiss, DR; Renger, JJ; Stevens, J; Tannenbaum, PL; Winrow, CJ, 2011) | 1.04 |
| " Drug levels are higher in women and obese people; hence, dosing should be conservative in obese women." | ( Profile of suvorexant in the management of insomnia. Sutton, EL, 2015) | 0.81 |
| " This randomized, double-blind, placebo-controlled, sequential-panel, Phase 1 trial assessed the safety, tolerability, and pharmacokinetic data following single and multiple dosing of suvorexant in healthy men (aged 18-45 years)." | ( Safety, Tolerability, and Pharmacokinetics of Suvorexant: A Randomized Rising-Dose Trial in Healthy Men. Cabalu, T; Lewis, N; Liu, W; McCrea, J; Panebianco, D; Ramael, S; Wrishko, RE; Yee, KL, 2018) | 0.93 |
| "Suvorexant was generally well tolerated after single and multiple dosing for 14 days." | ( Safety, Tolerability, and Pharmacokinetics of Suvorexant: A Randomized Rising-Dose Trial in Healthy Men. Cabalu, T; Lewis, N; Liu, W; McCrea, J; Panebianco, D; Ramael, S; Wrishko, RE; Yee, KL, 2018) | 2.18 |
| " Zolpidem has been marketed in new dosage forms that include sublingual tablets and oral spray formulations." | ( New pharmacologic agents for insomnia and hypersomnia. Earl, DC; Van Tyle, KM, 2020) | 0.56 |
| "Recent advancements in the treatment of insomnia includes agents with novel mechanisms, new indications, and new dosage forms." | ( New pharmacologic agents for insomnia and hypersomnia. Earl, DC; Van Tyle, KM, 2020) | 0.56 |
| " This second column in the series focuses on the metabolism of each of the 3 drugs by the cytochrome P450 enzyme CYP3A, guidance for using these agents in combination with drugs that are CYP3A inhibitors or inducers, and how to adjust dosing in patients with comorbid conditions such as hepatic or renal impairment." | ( Comparative Pharmacology of the 3 Marketed Dual Orexin Antagonists-Daridorexant, Lemborexant, and Suvorexant-Part 2. Principal Drug Metabolizing Enzyme, Drug-Drug Interactions, and Effects of Liver and Renal Impairment on Metabolism. Preskorn, SH, 2023) | 1.13 |
| Role | Description |
|---|---|
| central nervous system depressant | A loosely defined group of drugs that tend to reduce the activity of the central nervous system. |
| orexin receptor antagonist | An antagonist that binds to and deactivates orexin receptors. |
| [role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
| Class | Description |
|---|---|
| 1,3-benzoxazoles | Compounds based on a fused 1,3-oxazole and benzene bicyclic ring skeleton. |
| triazoles | An azole in which the five-membered heterocyclic aromatic skeleton contains three N atoms and two C atoms. |
| diazepine | |
| aromatic amide | An amide in which the amide linkage is bonded directly to an aromatic system. |
| organochlorine compound | An organochlorine compound is a compound containing at least one carbon-chlorine bond. |
| [compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Orexin receptor type 1 | Homo sapiens (human) | IC50 (µMol) | 0.0873 | 0.0060 | 0.0445 | 0.1990 | AID1139801; AID1279973; AID1432659; AID482636 |
| Orexin receptor type 1 | Homo sapiens (human) | Ki | 0.0010 | 0.0003 | 0.2876 | 3.1623 | AID1139799; AID1582239; AID1724828; AID482633; AID482634; AID765089 |
| Orexin receptor type 2 | Homo sapiens (human) | IC50 (µMol) | 0.0613 | 0.0004 | 0.5185 | 8.1000 | AID1139802; AID1249289; AID1279959; AID1432660; AID482637 |
| Orexin receptor type 2 | Homo sapiens (human) | Ki | 0.0027 | 0.0002 | 0.3771 | 3.7810 | AID1139800; AID1166953; AID1582240; AID482635; AID765090 |
| Orexin receptor type 1 | Mus musculus (house mouse) | Ki | 0.0017 | 0.0017 | 0.0017 | 0.0017 | AID774767 |
| Orexin receptor type 2 | Mus musculus (house mouse) | Ki | 0.0087 | 0.0087 | 0.0087 | 0.0087 | AID774766 |
| Substance-K receptor | Cavia porcellus (domestic guinea pig) | Ki | 0.0003 | 0.0003 | 1.8502 | 3.7000 | AID482635 |
| Sigma non-opioid intracellular receptor 1 | Rattus norvegicus (Norway rat) | Ki | 0.0004 | 0.0003 | 0.2671 | 5.0700 | AID765090 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| G protein-coupled receptor activity | Orexin receptor type 1 | Homo sapiens (human) |
| protein binding | Orexin receptor type 1 | Homo sapiens (human) |
| orexin receptor activity | Orexin receptor type 1 | Homo sapiens (human) |
| peptide hormone binding | Orexin receptor type 1 | Homo sapiens (human) |
| peptide binding | Orexin receptor type 1 | Homo sapiens (human) |
| protein binding | Orexin receptor type 2 | Homo sapiens (human) |
| neuropeptide receptor activity | Orexin receptor type 2 | Homo sapiens (human) |
| orexin receptor activity | Orexin receptor type 2 | Homo sapiens (human) |
| peptide hormone binding | Orexin receptor type 2 | Homo sapiens (human) |
| peptide binding | Orexin receptor type 2 | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| plasma membrane | Orexin receptor type 1 | Homo sapiens (human) |
| synapse | Orexin receptor type 1 | Homo sapiens (human) |
| plasma membrane | Orexin receptor type 1 | Homo sapiens (human) |
| plasma membrane | Orexin receptor type 2 | Homo sapiens (human) |
| synapse | Orexin receptor type 2 | Homo sapiens (human) |
| plasma membrane | Orexin receptor type 2 | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID482645 | Volume of distribution at steady state in dog at 0.5 mg/kg, iv | 2010 | Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14 | Discovery of the dual orexin receptor antagonist [(7R)-4-(5-chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the treatment of insomnia. |
| AID482850 | Selectivity for human OX2R over human OX1R | 2010 | Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14 | Discovery of the dual orexin receptor antagonist [(7R)-4-(5-chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the treatment of insomnia. |
| AID1279955 | Tmax in human plasma | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2 | Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia. |
| AID1280069 | Effect on sleep parameter in insomnia patient assessed as total sleep time at 40 mg, po measured on night 1 by polysomnography | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2 | Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia. |
| AID482650 | Tmax in dog at 3 mg/kg, po | 2010 | Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14 | Discovery of the dual orexin receptor antagonist [(7R)-4-(5-chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the treatment of insomnia. |
| AID1280059 | Effect on sleep parameter in insomnia patient assessed as latency to persistent sleep time at 10 mg, po measured on night 1 by polysomnography | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2 | Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia. |
| AID1280083 | Effect on sleep parameter in insomnia patient assessed as total sleep time at 40 mg, po measured on night 28 by polysomnography | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2 | Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia. |
| AID1280080 | Effect on sleep parameter in insomnia patient assessed as sleep efficiency at 40 mg, po measured on night 28 by polysomnography | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2 | Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia. |
| AID774763 | Fraction unbound in C57BL/6 mouse brain at 50 mg/kg, po after 1 hr by LC-MS/MS analysis | 2013 | Journal of medicinal chemistry, Oct-10, Volume: 56, Issue:19 | Identification of a novel series of orexin receptor antagonists with a distinct effect on sleep architecture for the treatment of insomnia. |
| AID774767 | Antagonist activity at mouse OX1 receptor expressed in CHO cells assessed as inhibition of orexin A-induced Ca2+ accumulation after 1 hr by Fluo-4-AM staining-based FLIPR assay | 2013 | Journal of medicinal chemistry, Oct-10, Volume: 56, Issue:19 | Identification of a novel series of orexin receptor antagonists with a distinct effect on sleep architecture for the treatment of insomnia. |
| AID1432680 | Sleep promoting activity in Sprague-Dawley rat assessed as effect on rapid eye movement sleep time at 90 mg/kg, po measured over 2 hrs by electroencephalogram method | 2017 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 27, Issue:6 | Discovery of novel substituted octahydropyrrolo[3,4-c]pyrroles as dual orexin receptor antagonists for insomnia treatment. |
| AID1139799 | Displacement of [3H]radioligand from human orexin-1 receptor expressed in CHO cells after 3 hrs by scintillation counting analysis | 2014 | Bioorganic & medicinal chemistry letters, May-01, Volume: 24, Issue:9 | Discovery of dual orexin receptor antagonists with rat sleep efficacy enabled by expansion of the acetonitrile-assisted/diphosgene-mediated 2,4-dichloropyrimidine synthesis. |
| AID1889302 | Permeability in pig LLC-PK1 cells | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3 | Dose Number as a Tool to Guide Lead Optimization for Orally Bioavailable Compounds in Drug Discovery. |
| AID1249288 | Antagonist activity at human orexin 1 receptor Ile408-Val mutant expressed in CHO cells assessed as inhibition of orexin-A-induced intracellular calcium level after 60 mins by FLIPR assay | 2015 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 25, Issue:21 | Discovery of diazepane amide DORAs and 2-SORAs enabled by exploration of isosteric quinazoline replacements. |
| AID1889298 | Aqueous solubility of the compound in FaSSIF | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3 | Dose Number as a Tool to Guide Lead Optimization for Orally Bioavailable Compounds in Drug Discovery. |
| AID482636 | Antagonist activity at human OX1R expressed in CHO cells assessed as inhibition of orexin-A-induced intracellular calcium mobilization after 5 mins by FLIPR assay | 2010 | Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14 | Discovery of the dual orexin receptor antagonist [(7R)-4-(5-chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the treatment of insomnia. |
| AID482820 | Ratio of drug level in CSF to plasma in rat at 0.25 to 2 mg/kg, iv after 30 mins | 2010 | Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14 | Discovery of the dual orexin receptor antagonist [(7R)-4-(5-chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the treatment of insomnia. |
| AID1280007 | Effect on sleep parameter in po dosed dog by EEG analysis | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2 | Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia. |
| AID482840 | Drug level in human OX2R overexpressing transgenic rat CSF at 1.34 mg/kg, iv after 30 mins | 2010 | Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14 | Discovery of the dual orexin receptor antagonist [(7R)-4-(5-chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the treatment of insomnia. |
| AID1280063 | Effect on sleep parameter in insomnia patient assessed as latency to persistent sleep time at 20 mg, po measured on night 1 by polysomnography | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2 | Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia. |
| AID1192081 | Half life in human | 2015 | Bioorganic & medicinal chemistry, Mar-15, Volume: 23, Issue:6 | Discovery and in vitro and in vivo profiles of N-ethyl-N-[2-[3-(5-fluoro-2-pyridinyl)-1H-pyrazol-1-yl]ethyl]-2-(2H-1,2,3-triazol-2-yl)-benzamide as a novel class of dual orexin receptor antagonist. |
| AID482845 | Genotoxicity in Salmonella Typhimurium by Ames test | 2010 | Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14 | Discovery of the dual orexin receptor antagonist [(7R)-4-(5-chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the treatment of insomnia. |
| AID1279954 | Apparent permeability of the compound | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2 | Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia. |
| AID1280061 | Effect on sleep parameter in insomnia patient assessed as total sleep time at 10 mg, po measured on night 1 by polysomnography | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2 | Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia. |
| AID1280068 | Effect on sleep parameter in insomnia patient assessed as wake after sleep onset time at 40 mg, po measured on night 1 by polysomnography | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2 | Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia. |
| AID482841 | In vivo occupancy of human OX2R ubiquitously overexpressed in transgenic rat at 30 mg/kg/day, iv after 30 mins | 2010 | Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14 | Discovery of the dual orexin receptor antagonist [(7R)-4-(5-chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the treatment of insomnia. |
| AID1139802 | Antagonist activity at human orexin-2 receptor expressed in CHO cells assessed as inhibition of Ala-6, 12-induced responses by FLIPR assay | 2014 | Bioorganic & medicinal chemistry letters, May-01, Volume: 24, Issue:9 | Discovery of dual orexin receptor antagonists with rat sleep efficacy enabled by expansion of the acetonitrile-assisted/diphosgene-mediated 2,4-dichloropyrimidine synthesis. |
| AID482634 | Displacement of [3H]N-cyclobutyl-5-methyl-N-(2-(1-methyl-1H-benzo[d]imidazol-2-ylthio)ethyl)-2-(2H-1,2,3-triazol-2-yl)benzamide from human OX1R expressed in CHO cells after 20 hrs by scintillation counting | 2010 | Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14 | Discovery of the dual orexin receptor antagonist [(7R)-4-(5-chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the treatment of insomnia. |
| AID1582239 | Displacement of [3H]4-(2,6-Difluoro-4-methoxybenzyl)-2-(5,6-dimethoxypyridin-3-yl)-2H-1,2,4-benzothiadiazin-3(4H)-one 1,1-dioxide from human wild-type OX1 receptor expressed in baculovirus infected Sf21 insect cell membranes measured after 90 mins by liqu | 2020 | Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4 | Comparison of Orexin 1 and Orexin 2 Ligand Binding Modes Using X-ray Crystallography and Computational Analysis. |
| AID1280001 | Clearance in iv dosed rat | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2 | Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia. |
| AID1279959 | Antagonist activity at OX2R (unknown origin) | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2 | Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia. |
| AID1279986 | Plasma protein binding in human | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2 | Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia. |
| AID482839 | Drug level in human OX2R overexpressing transgenic rat brain at 1.34 mg/kg, iv after 30 mins | 2010 | Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14 | Discovery of the dual orexin receptor antagonist [(7R)-4-(5-chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the treatment of insomnia. |
| AID774758 | Induction of sleep in C57BL/6 mouse assessed as increase in non-rapid eye movement at 50 mg/kg, po measured during 4 hrs by EEG/EMG analysis relative to vehicle-treated control | 2013 | Journal of medicinal chemistry, Oct-10, Volume: 56, Issue:19 | Identification of a novel series of orexin receptor antagonists with a distinct effect on sleep architecture for the treatment of insomnia. |
| AID482821 | Ratio of drug level in brain to plasma in rat at 10 mg/kg, po after 1 hr | 2010 | Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14 | Discovery of the dual orexin receptor antagonist [(7R)-4-(5-chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the treatment of insomnia. |
| AID1280076 | Effect on sleep parameter in insomnia patient assessed as total sleep time at 10 mg, po measured on night 28 by polysomnography | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2 | Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia. |
| AID482646 | Terminal half life in dog at 0.5 mg/kg, iv | 2010 | Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14 | Discovery of the dual orexin receptor antagonist [(7R)-4-(5-chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the treatment of insomnia. |
| AID482648 | Cmax in dog at 3 mg/kg, po | 2010 | Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14 | Discovery of the dual orexin receptor antagonist [(7R)-4-(5-chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the treatment of insomnia. |
| AID1432659 | Antagonist activity at human orexin 1 receptor expressed in HEK293 cells assessed as inhibition of orexin-induced calcium mobilization after 60 mins by FLIPR assay | 2017 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 27, Issue:6 | Discovery of novel substituted octahydropyrrolo[3,4-c]pyrroles as dual orexin receptor antagonists for insomnia treatment. |
| AID1280084 | Effect on sleep parameter in insomnia patient assessed as sleep efficiency at 80 mg, po measured on night 28 by polysomnography | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2 | Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia. |
| AID482823 | Lipophilicity, log P of the compound | 2010 | Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14 | Discovery of the dual orexin receptor antagonist [(7R)-4-(5-chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the treatment of insomnia. |
| AID1280065 | Effect on sleep parameter in insomnia patient assessed as total sleep time at 20 mg, po measured on night 1 by polysomnography | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2 | Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia. |
| AID1279997 | Plasma protein binding in rat | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2 | Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia. |
| AID482833 | Antiinsomnic activity in Sprague-Dawley rat assessed as increase in delta sleep duration at 30 mg/kg/day, po measured with 3 to 4 hrs post last dose | 2010 | Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14 | Discovery of the dual orexin receptor antagonist [(7R)-4-(5-chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the treatment of insomnia. |
| AID482835 | Cmax in Sprague-Dawley rat CSF at 30 mg/kg/day, po | 2010 | Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14 | Discovery of the dual orexin receptor antagonist [(7R)-4-(5-chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the treatment of insomnia. |
| AID1279999 | Substrate activity at human Pgp assessed as efflux ratio | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2 | Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia. |
| AID765090 | Binding affinity to orexin receptor 2 (unknown origin) | 2013 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17 | Selective orexin receptor antagonists. |
| AID1237015 | Half life in human | 2015 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 25, Issue:15 | Recent trends in orexin research--2010 to 2015. |
| AID1280082 | Effect on sleep parameter in insomnia patient assessed as wake after sleep onset time at 40 mg, po measured on night 28 by polysomnography | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2 | Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia. |
| AID482832 | Antiinsomnic activity in Sprague-Dawley rat assessed as increase in rapid-eye movement at 30 mg/kg/day, po measured with 3 to 4 hrs post last dose | 2010 | Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14 | Discovery of the dual orexin receptor antagonist [(7R)-4-(5-chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the treatment of insomnia. |
| AID1166953 | Displacement of [125I]-Orexin A from human OX2R expressed in CHO cells after 30 mins by topcount analysis | 2014 | Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21 | Design, synthesis, and structure-activity relationships of a series of novel N-aryl-2-phenylcyclopropanecarboxamide that are potent and orally active orexin receptor antagonists. |
| AID482654 | Oral bioavailability in rat at 10 mg/kg | 2010 | Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14 | Discovery of the dual orexin receptor antagonist [(7R)-4-(5-chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the treatment of insomnia. |
| AID1249292 | Bioactivation of compound in rat liver microsomes assessed as AUC of GSH-adduct formation at 10 uM after 60 mins by HRMS analysis relative to labetalol | 2015 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 25, Issue:21 | Discovery of diazepane amide DORAs and 2-SORAs enabled by exploration of isosteric quinazoline replacements. |
| AID1280081 | Effect on sleep parameter in insomnia patient assessed as latency to persistent sleep time at 40 mg, po measured on night 28 by polysomnography | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2 | Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia. |
| AID1139800 | Displacement of [3H]radioligand from human orexin-2 receptor expressed in CHO cells after 3 hrs by scintillation counting analysis | 2014 | Bioorganic & medicinal chemistry letters, May-01, Volume: 24, Issue:9 | Discovery of dual orexin receptor antagonists with rat sleep efficacy enabled by expansion of the acetonitrile-assisted/diphosgene-mediated 2,4-dichloropyrimidine synthesis. |
| AID1280000 | Receptor occupancy at OX2R in rat brain assessed as drug level in plasma | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2 | Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia. |
| AID774764 | Drug uptake in C57BL/6 mouse blood at 50 mg/kg after 1 hr by LC-MS/MS analysis | 2013 | Journal of medicinal chemistry, Oct-10, Volume: 56, Issue:19 | Identification of a novel series of orexin receptor antagonists with a distinct effect on sleep architecture for the treatment of insomnia. |
| AID482640 | Terminal half life in rat at 2 mg/kg, iv | 2010 | Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14 | Discovery of the dual orexin receptor antagonist [(7R)-4-(5-chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the treatment of insomnia. |
| AID482639 | Volume of distribution at steady state in rat at 2 mg/kg, iv | 2010 | Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14 | Discovery of the dual orexin receptor antagonist [(7R)-4-(5-chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the treatment of insomnia. |
| AID1663203 | Half-life in human plasma at 40 mg,po administered once daily | 2020 | Bioorganic & medicinal chemistry, 07-01, Volume: 28, Issue:13 | Discovery of ORN0829, a potent dual orexin 1/2 receptor antagonist for the treatment of insomnia. |
| AID482638 | Clearance in rat at 2 mg/kg, iv | 2010 | Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14 | Discovery of the dual orexin receptor antagonist [(7R)-4-(5-chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the treatment of insomnia. |
| AID774760 | Induction of sleep in C57BL/6 mouse assessed as increase in total sleep time at 50 mg/kg, po measured during 5 hrs by EEG/EMG analysis relative to vehicle-treated control | 2013 | Journal of medicinal chemistry, Oct-10, Volume: 56, Issue:19 | Identification of a novel series of orexin receptor antagonists with a distinct effect on sleep architecture for the treatment of insomnia. |
| AID1280067 | Effect on sleep parameter in insomnia patient assessed as latency to persistent sleep time at 40 mg, po measured on night 1 by polysomnography | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2 | Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia. |
| AID1249291 | Bioactivation of compound in human liver microsomes assessed as AUC of GSH-adduct formation at 10 uM after 60 mins by HRMS analysis relative to labetalol | 2015 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 25, Issue:21 | Discovery of diazepane amide DORAs and 2-SORAs enabled by exploration of isosteric quinazoline replacements. |
| AID1279998 | Plasma protein binding in dog | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2 | Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia. |
| AID1139801 | Antagonist activity at human orexin-1 receptor expressed in CHO cells assessed as inhibition of Ala-6, 12-induced responses by FLIPR assay | 2014 | Bioorganic & medicinal chemistry letters, May-01, Volume: 24, Issue:9 | Discovery of dual orexin receptor antagonists with rat sleep efficacy enabled by expansion of the acetonitrile-assisted/diphosgene-mediated 2,4-dichloropyrimidine synthesis. |
| AID1280057 | Terminal half life in human plasma | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2 | Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia. |
| AID1280002 | Half life in iv dosed rat | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2 | Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia. |
| AID1280004 | Half life in iv dosed dog | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2 | Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia. |
| AID774765 | Drug uptake in C57BL/6 mouse brain at 50 mg/kg after 1 hr by LC-MS/MS analysis | 2013 | Journal of medicinal chemistry, Oct-10, Volume: 56, Issue:19 | Identification of a novel series of orexin receptor antagonists with a distinct effect on sleep architecture for the treatment of insomnia. |
| AID1280086 | Effect on sleep parameter in insomnia patient assessed as wake after sleep onset time at 80 mg, po measured on night 28 by polysomnography | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2 | Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia. |
| AID774761 | Effect on locomotion in C57BL/6 mouse assessed as reduction of motility at 50 mg/kg, po measured up to 4 hrs | 2013 | Journal of medicinal chemistry, Oct-10, Volume: 56, Issue:19 | Identification of a novel series of orexin receptor antagonists with a distinct effect on sleep architecture for the treatment of insomnia. |
| AID482834 | Antiinsomnic activity in Sprague-Dawley rat assessed as decrease in light sleep duration at 30 mg/kg/day, po measured with 3 to 4 hrs post last dose | 2010 | Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14 | Discovery of the dual orexin receptor antagonist [(7R)-4-(5-chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the treatment of insomnia. |
| AID1280005 | Oral bioavailability in rat | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2 | Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia. |
| AID1280075 | Effect on sleep parameter in insomnia patient assessed as wake after sleep onset time at 10 mg, po measured on night 28 by polysomnography | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2 | Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia. |
| AID1279952 | GSH activity assessed as GSH adduct formation by measuring GSH/IS ratio | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2 | Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia. |
| AID1280060 | Effect on sleep parameter in insomnia patient assessed as wake after sleep onset time at 10 mg, po measured on night 1 by polysomnography | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2 | Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia. |
| AID1597745 | Half life in human at 5 to 20 mg | 2019 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16 | Sleep modulating agents. |
| AID1582240 | Displacement of [3H]4-(2,6-Difluoro-4-methoxybenzyl)-2-(5,6-dimethoxypyridin-3-yl)-2H-1,2,4-benzothiadiazin-3(4H)-one 1,1-dioxide from human wild-type OX2 receptor expressed in baculovirus infected Sf21 insect cell membranes measured after 90 mins by liqu | 2020 | Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4 | Comparison of Orexin 1 and Orexin 2 Ligand Binding Modes Using X-ray Crystallography and Computational Analysis. |
| AID482836 | Drug level in Sprague-Dawley rat CSF at 30 mg/kg/day, po | 2010 | Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14 | Discovery of the dual orexin receptor antagonist [(7R)-4-(5-chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the treatment of insomnia. |
| AID1279956 | Effect on sleep parameter in po dosed rat by EEG analysis | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2 | Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia. |
| AID482848 | Plasma protein binding in rat | 2010 | Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14 | Discovery of the dual orexin receptor antagonist [(7R)-4-(5-chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the treatment of insomnia. |
| AID1280066 | Effect on sleep parameter in insomnia patient assessed as sleep efficiency at 40 mg, po measured on night 1 by polysomnography | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2 | Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia. |
| AID482843 | Chemical stability in pH-dependent solution | 2010 | Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14 | Discovery of the dual orexin receptor antagonist [(7R)-4-(5-chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the treatment of insomnia. |
| AID482637 | Antagonist activity at human OX2R expressed in CHO cells assessed as inhibition of orexin-A-induced intracellular calcium mobilization after 5 mins by FLIPR assay | 2010 | Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14 | Discovery of the dual orexin receptor antagonist [(7R)-4-(5-chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the treatment of insomnia. |
| AID1280006 | Oral bioavailability in dog | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2 | Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia. |
| AID482822 | Ratio of drug level in CSF to plasma in rat at 10 mg/kg, po after 1 hr | 2010 | Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14 | Discovery of the dual orexin receptor antagonist [(7R)-4-(5-chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the treatment of insomnia. |
| AID482653 | Tmax in rat at 10 mg/kg, po | 2010 | Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14 | Discovery of the dual orexin receptor antagonist [(7R)-4-(5-chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the treatment of insomnia. |
| AID482831 | Antiinsomnic activity in Sprague-Dawley rat assessed as decrease in active wake duration at 30 mg/kg/day, po measured with 3 to 4 hrs post last dose | 2010 | Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14 | Discovery of the dual orexin receptor antagonist [(7R)-4-(5-chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the treatment of insomnia. |
| AID1280062 | Effect on sleep parameter in insomnia patient assessed as sleep efficiency at 20 mg, po measured on night 1 by polysomnography | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2 | Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia. |
| AID1280058 | Effect on sleep parameter in insomnia patient assessed as sleep efficiency at 10 mg, po measured on night 1 by polysomnography | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2 | Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia. |
| AID1279973 | Antagonist activity at OX1R (unknown origin) | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2 | Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia. |
| AID774766 | Antagonist activity at mouse OX2 receptor expressed in HEK cells assessed as inhibition of orexin A-induced Ca2+ accumulation after 1 hr by Fluo-4-AM staining-based FLIPR assay | 2013 | Journal of medicinal chemistry, Oct-10, Volume: 56, Issue:19 | Identification of a novel series of orexin receptor antagonists with a distinct effect on sleep architecture for the treatment of insomnia. |
| AID1280071 | Effect on sleep parameter in insomnia patient assessed as latency to persistent sleep time at 80 mg, po measured on night 1 by polysomnography | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2 | Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia. |
| AID1279964 | Effect on sleep parameter in insomnia patient assessed as wake after sleep onset time at 20 mg, po measured on night 28 by polysomnography | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2 | Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia. |
| AID482647 | AUC in dog at 3 mg/kg, po | 2010 | Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14 | Discovery of the dual orexin receptor antagonist [(7R)-4-(5-chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the treatment of insomnia. |
| AID482846 | Cardiotoxicity in dog | 2010 | Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14 | Discovery of the dual orexin receptor antagonist [(7R)-4-(5-chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the treatment of insomnia. |
| AID1724830 | Displacement of [3H]-EMPA from human orexin 2 receptor expressed in CHO cells incubated for 2 hrs by whole cell radioligand binding assay | 2020 | Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19 | Structure-Based Discovery of Novel Ligands for the Orexin 2 Receptor. |
| AID1280074 | Effect on sleep parameter in insomnia patient assessed as latency to persistent sleep time at 10 mg, po measured on night 28 by polysomnography | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2 | Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia. |
| AID1280072 | Effect on sleep parameter in insomnia patient assessed as wake after sleep onset time at 80 mg, po measured on night 1 by polysomnography | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2 | Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia. |
| AID482635 | Displacement of [3H](S)-N-(2-(1H-pyrrol-1-yl)phenyl)-1-(2-(1-methyl-1H-benzo[d]imidazol-2-ylthio)acetyl)pyrrolidine-2-carboxamide from human OX2R expressed in CHO cells after 3 hrs by scintillation counting | 2010 | Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14 | Discovery of the dual orexin receptor antagonist [(7R)-4-(5-chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the treatment of insomnia. |
| AID1279945 | Effect on sleep parameter in insomnia patient assessed as total sleep time at 80 mg, po measured on night 28 by polysomnography | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2 | Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia. |
| AID1432682 | Sleep promoting activity in Sprague-Dawley rat assessed as increase in slow wave sleep time at 90 mg/kg, po measured over 2 hrs by electroencephalogram method | 2017 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 27, Issue:6 | Discovery of novel substituted octahydropyrrolo[3,4-c]pyrroles as dual orexin receptor antagonists for insomnia treatment. |
| AID482842 | Thermal stability of the compound | 2010 | Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14 | Discovery of the dual orexin receptor antagonist [(7R)-4-(5-chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the treatment of insomnia. |
| AID1279963 | Effect on sleep parameter in insomnia patient assessed as total sleep time at 80 mg, po measured on night 1 by polysomnography | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2 | Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia. |
| AID482837 | In vivo occupancy of human OX2R ubiquitously overexpressed in iv dosed transgenic rat after 30 mins | 2010 | Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14 | Discovery of the dual orexin receptor antagonist [(7R)-4-(5-chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the treatment of insomnia. |
| AID482651 | AUC in rat at 10 mg/kg, po | 2010 | Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14 | Discovery of the dual orexin receptor antagonist [(7R)-4-(5-chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the treatment of insomnia. |
| AID1280078 | Effect on sleep parameter in insomnia patient assessed as latency to persistent sleep time at 20 mg, po measured on night 28 by polysomnography | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2 | Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia. |
| AID1280073 | Effect on sleep parameter in insomnia patient assessed as sleep efficiency at 10 mg, po measured on night 28 by polysomnography | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2 | Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia. |
| AID482849 | Plasma protein binding in human | 2010 | Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14 | Discovery of the dual orexin receptor antagonist [(7R)-4-(5-chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the treatment of insomnia. |
| AID1280079 | Effect on sleep parameter in insomnia patient assessed as total sleep time at 20 mg, po measured on night 28 by polysomnography | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2 | Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia. |
| AID482644 | Clearance in dog at 0.5 mg/kg, iv | 2010 | Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14 | Discovery of the dual orexin receptor antagonist [(7R)-4-(5-chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the treatment of insomnia. |
| AID1280077 | Effect on sleep parameter in insomnia patient assessed as sleep efficiency at 20 mg, po measured on night 28 by polysomnography | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2 | Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia. |
| AID765089 | Binding affinity to orexin receptor 1 (unknown origin) | 2013 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17 | Selective orexin receptor antagonists. |
| AID1280003 | Clearance in iv dosed dog | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2 | Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia. |
| AID1432678 | Sleep promoting activity in Sprague-Dawley rat assessed as decrease in active wake time at 90 mg/kg, po measured over 2 hrs by electroencephalogram method | 2017 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 27, Issue:6 | Discovery of novel substituted octahydropyrrolo[3,4-c]pyrroles as dual orexin receptor antagonists for insomnia treatment. |
| AID482633 | Displacement of [3H](S)-N-(biphenyl-2-yl)-1-(2-(1-methyl-1H-benzo[d]imidazol-2-ylthio)acetyl)pyrrolidine-2-carboxamide from human OX1R expressed in CHO cells after 3 hrs by scintillation counting | 2010 | Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14 | Discovery of the dual orexin receptor antagonist [(7R)-4-(5-chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the treatment of insomnia. |
| AID1432660 | Antagonist activity at human orexin 2 receptor expressed in HEK293 cells assessed as inhibition of orexin-induced calcium mobilization after 60 mins by FLIPR assay | 2017 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 27, Issue:6 | Discovery of novel substituted octahydropyrrolo[3,4-c]pyrroles as dual orexin receptor antagonists for insomnia treatment. |
| AID482830 | Idiosyncratic toxicity in human liver microsomes assessed GSH-derived reactive electrophilic adduct formation at 10 uM after 60 mins by UPLC/HRMS analysis relative to labetalol | 2010 | Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14 | Discovery of the dual orexin receptor antagonist [(7R)-4-(5-chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the treatment of insomnia. |
| AID1724828 | Displacement of [3H]-SB67404 from human orexin 1 receptor expressed in CHO cells incubated for 2 hrs by whole cell radioligand binding assay | 2020 | Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19 | Structure-Based Discovery of Novel Ligands for the Orexin 2 Receptor. |
| AID482838 | Drug level in human OX2R overexpressing transgenic rat plasma at 1.34 mg/kg, iv after 30 mins | 2010 | Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14 | Discovery of the dual orexin receptor antagonist [(7R)-4-(5-chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the treatment of insomnia. |
| AID1249289 | Antagonist activity at human orexin 2 receptor expressed in CHO cells assessed as inhibition of orexin-A-induced intracellular calcium level after 60 mins by FLIPR assay | 2015 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 25, Issue:21 | Discovery of diazepane amide DORAs and 2-SORAs enabled by exploration of isosteric quinazoline replacements. |
| AID1280070 | Effect on sleep parameter in insomnia patient assessed as sleep efficiency at 80 mg, po measured on night 1 by polysomnography | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2 | Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia. |
| AID482658 | Ratio of drug level in brain to plasma in rat at 0.25 to 2 mg/kg, iv after 30 mins | 2010 | Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14 | Discovery of the dual orexin receptor antagonist [(7R)-4-(5-chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the treatment of insomnia. |
| AID482844 | Aqueous solubility of the compound | 2010 | Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14 | Discovery of the dual orexin receptor antagonist [(7R)-4-(5-chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the treatment of insomnia. |
| AID482652 | Cmax in rat at 10 mg/kg, po | 2010 | Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14 | Discovery of the dual orexin receptor antagonist [(7R)-4-(5-chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the treatment of insomnia. |
| AID1280085 | Effect on sleep parameter in insomnia patient assessed as latency to persistent sleep time at 80 mg, po measured on night 28 by polysomnography | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2 | Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia. |
| AID774759 | Induction of sleep in C57BL/6 mouse assessed as increase in rapid eye movement at 50 mg/kg, po measured during 4 hrs by EEG/EMG analysis relative to vehicle-treated control | 2013 | Journal of medicinal chemistry, Oct-10, Volume: 56, Issue:19 | Identification of a novel series of orexin receptor antagonists with a distinct effect on sleep architecture for the treatment of insomnia. |
| AID1280064 | Effect on sleep parameter in insomnia patient assessed as wake after sleep onset time at 20 mg, po measured on night 1 by polysomnography | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2 | Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia. |
| AID774755 | Induction of sleep in C57BL/6 mouse assessed as increased rapid eye movement sleep proportion at 50 mg/kg, po measured during 1 hr by EEG/EMG analysis relative to vehicle-treated control | 2013 | Journal of medicinal chemistry, Oct-10, Volume: 56, Issue:19 | Identification of a novel series of orexin receptor antagonists with a distinct effect on sleep architecture for the treatment of insomnia. |
| AID482649 | Oral bioavailability in dog at 3 mg/kg | 2010 | Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14 | Discovery of the dual orexin receptor antagonist [(7R)-4-(5-chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the treatment of insomnia. |
| AID1346418 | Human OX2 receptor (Orexin receptors) | 2010 | Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14 | Discovery of the dual orexin receptor antagonist [(7R)-4-(5-chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the treatment of insomnia. |
| AID1346381 | Human OX1 receptor (Orexin receptors) | 2010 | Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14 | Discovery of the dual orexin receptor antagonist [(7R)-4-(5-chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the treatment of insomnia. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 0 (0.00) | 29.6817 |
| 2010's | 125 (61.88) | 24.3611 |
| 2020's | 77 (38.12) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.
| This Compound (78.31) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 47 (21.96%) | 5.53% |
| Reviews | 44 (20.56%) | 6.00% |
| Case Studies | 14 (6.54%) | 4.05% |
| Observational | 5 (2.34%) | 0.25% |
| Other | 104 (48.60%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
| Trial | Phase | Enrollment | Study Type | Start Date | Status | ||
|---|---|---|---|---|---|---|---|
| A Single-Dose, Double-Blind, Placebo-Controlled, Randomized, Crossover Study to Determine the Abuse Potential of Single Oral Dose of Seltorexant Compared To Suvorexant and Zolpidem [NCT05106153] | Phase 1 | 127 participants (Actual) | Interventional | 2021-12-17 | Completed | ||
| Proof of Concept Study: Treatment of Restless Legs Syndrome With the Hypocretin Antagonist Suvorexant [NCT03755310] | Phase 2 | 43 participants (Anticipated) | Interventional | 2019-02-28 | Not yet recruiting | ||
| A Phase 3 Multicenter, Randomized, Placebo-controlled, Double-blind Clinical Study to Evaluate the Efficacy and Safety of MK-4305 (Suvorexant) for Reducing Incidence of Delirium in Japanese Participants at High Risk of Delirium [NCT04571944] | Phase 3 | 203 participants (Actual) | Interventional | 2020-10-22 | Completed | ||
| A Double-blind, Randomized, Placebo-controlled Study to Determine the Efficacy of Suvorexant in the Treatment of Hot Flash-associated Insomnia in Midlife Women [NCT03034018] | Phase 4 | 60 participants (Actual) | Interventional | 2017-05-25 | Completed | ||
| Randomized, Double-blind, Double-dummy, Placebo- and Active-controlled, 6-way Cross-over Study to Evaluate the Abuse Potential of Single, Oral Doses of ACT-541468 in Healthy Recreational Drug Users [NCT03657355] | Phase 1 | 63 participants (Actual) | Interventional | 2018-09-07 | Completed | ||
| A Phase III Randomized, Placebo-Controlled Clinical Trial to Study the Safety and Efficacy of Suvorexant (MK-4305) for the Treatment of Insomnia in Subjects With Alzheimer's Disease [NCT02750306] | Phase 3 | 285 participants (Actual) | Interventional | 2016-05-23 | Completed | ||
| Sleep Quality and Amyloid-Beta Kinetics [NCT03077620] | 48 participants (Actual) | Interventional | 2016-11-30 | Completed | |||
| Suvorexant to Reduce Symptoms of Nicotine Use: A Double-blind, Placebo-controlled Study [NCT04234997] | Phase 2 | 20 participants (Anticipated) | Interventional | 2021-08-23 | Recruiting | ||
| A Multiple Dose Study to Evaluate Next Day Effects of MK-4305 on Driving Performance in Healthy Non-Elderly Subjects [NCT01311882] | Phase 1 | 28 participants (Actual) | Interventional | 2011-04-30 | Completed | ||
| A Double-Blind Sequential Parallel Study of Suvorexant (Belsomra) for the Treatment of Bipolar Depression With Insomnia [NCT03764683] | Phase 4 | 0 participants (Actual) | Interventional | 2019-02-26 | Withdrawn(stopped due to Study was terminated due to COVID-19.) | ||
| A Randomized, Double-Blind, Placebo-Controlled Study to Determine the Effect of Suvorexant (Belsomra®) on Sympathetic Neural Activity and Baroreflex Function in Patients With Chronic Insomnia [NCT03768713] | Phase 4 | 34 participants (Anticipated) | Interventional | 2019-04-18 | Recruiting | ||
| A Study to Evaluate the Effects of MK-4305 in Patients With Obstructive Sleep Apnea [NCT01300455] | Phase 1 | 26 participants (Actual) | Interventional | 2011-03-19 | Completed | ||
| A Phase III, Multicenter, Randomized, Double-Blind, Placebo-Controlled, Parallel-Group, Long Term Safety Study of MK-4305 in Patients With Primary Insomnia [NCT01021813] | Phase 3 | 781 participants (Actual) | Interventional | 2009-12-10 | Completed | ||
| A Study to Evaluate the Effects of MK-4305 in Patients With Chronic Obstructive Pulmonary Disease [NCT01293006] | Phase 1 | 25 participants (Actual) | Interventional | 2011-03-25 | Completed | ||
| The Impact of Suvorexant on Cognitive Function and Daytime Symptoms Among Community-dwelling Older Adults With Insomnia: A Placebo-controlled, Randomized Clinical Trial Using Remote Monitoring and Ecological Momentary Assessment [NCT05908526] | Phase 2 | 50 participants (Anticipated) | Interventional | 2023-10-09 | Recruiting | ||
| A Placebo-controlled, Double -Blind Randomised Trial of Suvorexant in the Management Comorbid Sleep Disorder and Alcohol Dependence [NCT03897062] | Phase 2 | 22 participants (Actual) | Interventional | 2019-08-26 | Terminated(stopped due to Recruitment problems during covid lockdowns resulted in Merck ceasing supply of suvorexant/placebo) | ||
| Efficacy of Suvorexant in Patients With Effectively Treated Restless Legs Syndrome and Persistent Chronic Insomnia: A Randomized Placebo-Controlled Crossover Trial [NCT04706091] | Phase 4 | 90 participants (Anticipated) | Interventional | 2021-08-12 | Active, not recruiting | ||
| The Efficacy of Suvorexant in the Residential Treatment of Patients With Substance Use Disorder and Insomnia: A Pilot Open Trial [NCT03412591] | Phase 2/Phase 3 | 28 participants (Actual) | Interventional | 2019-07-01 | Completed | ||
| Randomized Placebo-Controlled Crossover Trial of Suvorexant for Sleep in Children With Autism [NCT05546554] | Phase 2 | 26 participants (Anticipated) | Interventional | 2023-08-09 | Recruiting | ||
| Sleep Trial to Prevent Alzheimer's Disease [NCT04629547] | Phase 2 | 200 participants (Anticipated) | Interventional | 2022-05-25 | Recruiting | ||
| Dual-Orexin Antagonism as a Mechanism for Improving Sleep and Drug Abstinence in Opioid Use Disorder [NCT04262193] | Phase 2 | 120 participants (Anticipated) | Interventional | 2021-02-01 | Recruiting | ||
| Effects of the Orexin Receptor Antagonist Suvorexant on Sleep Architecture and Delirium in the Intensive Care Unit: A Multi-Centric Randomized Controlled Trial [NCT04092894] | Phase 4 | 120 participants (Anticipated) | Interventional | 2020-02-28 | Recruiting | ||
| Suvorexant and Trauma Related Insomnia [NCT02704754] | Phase 4 | 41 participants (Actual) | Interventional | 2016-05-01 | Completed | ||
| A Six Week, Randomized, Double-Blind Placebo-Controlled, Suvorexant Augmentation Study of Antidepressant Treatment of Major Depressive Disorder With Residual Insomnia [NCT02669030] | Phase 4 | 74 participants (Anticipated) | Interventional | 2017-03-01 | Recruiting | ||
| Orexin's Role in The Neurobiology of Substance Use Disorder [NCT05630781] | 140 participants (Anticipated) | Interventional | 2023-02-15 | Recruiting | |||
| A Double-blind, Crossover, Study to Compare the Hypnotic, Daytime Sleepiness/Fatigue, and Pain Effects of Nighttime Administration of Suvorexant 20 mg Versus Placebo in Patients With Fibromyalgia and Comorbid Insomnia [NCT02684136] | Phase 4 | 10 participants (Actual) | Interventional | 2016-02-01 | Terminated(stopped due to reduced ability to recruit sufficient number of patients) | ||
| Targeting Orexin to Treat Nicotine Dependence [NCT03999099] | Phase 1 | 45 participants (Anticipated) | Interventional | 2019-09-26 | Recruiting | ||
| Safety and Efficacy of Suvorexant for Opioid/Stimulant Co-use Among Individuals in Treatment for Opioid Use Disorder (OUD) [NCT05546515] | Phase 2 | 40 participants (Anticipated) | Interventional | 2022-12-01 | Recruiting | ||
| A Phase IIb, Multicenter, Randomized, Double-Blind Placebo-Controlled, 2-period Adaptive Crossover Polysomnography Study to Evaluate Safety and Efficacy of MK-4305 in Patients With Primary Insomnia [NCT00792298] | Phase 2 | 254 participants (Actual) | Interventional | 2008-11-05 | Completed | ||
| Suvorexant: A Dual Orexin Receptor Antagonist for Treating Sleep Disturbance inPosttraumatic Stress [NCT03642028] | Phase 4 | 144 participants (Anticipated) | Interventional | 2019-08-30 | Recruiting | ||
| A Phase III, Multicenter, Randomized, Double-Blind, Placebo-Controlled, Parallel Group Study to Evaluate the Safety and Efficacy of MK-4305 in Patients With Primary Insomnia - Study B [NCT01097629] | Phase 3 | 1,020 participants (Actual) | Interventional | 2010-05-03 | Completed | ||
| Measuring Acute Drug Demand in Humans [NCT05829655] | Early Phase 1 | 75 participants (Anticipated) | Interventional | 2023-08-08 | Recruiting | ||
| A Phase III, Multicenter, Randomized, Double-Blind, Placebo-Controlled, Parallel Group Study to Evaluate the Safety and Efficacy of MK-4305 in Patients With Primary Insomnia - Study A [NCT01097616] | Phase 3 | 1,023 participants (Actual) | Interventional | 2010-05-05 | Completed | ||
| Examining the Role of the Orexin System in Sleep and Stress in Persons With Opioid Use Disorder [NCT04287062] | Phase 2 | 200 participants (Anticipated) | Interventional | 2020-11-20 | Recruiting | ||
| A Double-blind, Randomized, Placebo-controlled Trial of Adjunctive Suvorexant for Treatment-resistant Insomnia in Patients With Bipolar Disorder [NCT02527564] | Phase 4 | 61 participants (Actual) | Interventional | 2015-09-30 | Completed | ||
| A Multi-center, Double-blind, Randomized, Parallel Design Study to Compare the Effectiveness of Suvorexant Versus Placebo on Sleep Pressure and Circadian Rhythm in Hypertensives With Insomnia: The Super 1 Study [NCT02849184] | Phase 4 | 82 participants (Actual) | Interventional | 2017-01-17 | Completed | ||
| Orexin Receptor Antagonists as Modulators of Threat Sensitivity in Individuals With Alcohol Use Disorder [NCT05656534] | Early Phase 1 | 80 participants (Anticipated) | Interventional | 2022-11-29 | Recruiting | ||
| Medication Development for Protracted Abstinence in Alcoholism: Suvorexant Versus Placebo [NCT04229095] | Phase 2 | 26 participants (Actual) | Interventional | 2021-11-17 | Completed | ||
| Efficacy of Suvorexant to Improve Postoperative Sleep and Reduce Delirium Severity in Older Surgical Patients: A Double-blinded, Randomized, Placebo-controlled Trial [NCT05733286] | Phase 2 | 130 participants (Anticipated) | Interventional | 2023-06-28 | Recruiting | ||
| Treating Insomnia and Improving Glycemic Control in Midlife Women With Insomnia and Pre-diabetes [NCT05593653] | Phase 4 | 61 participants (Anticipated) | Interventional | 2023-01-06 | Recruiting | ||
| Influence of Orexin Antagonism on Motivation for Cocaine [NCT03937986] | Early Phase 1 | 8 participants (Actual) | Interventional | 2019-07-11 | Completed | ||
| [NCT02491788] | Phase 4 | 19 participants (Actual) | Interventional | 2016-02-01 | Completed | ||
| Suvorexant as an Adjunct to Buprenorphine Induction and Maintenance in Persons Who Use Fentanyl [NCT05145764] | Phase 2 | 120 participants (Anticipated) | Interventional | 2022-03-30 | Recruiting | ||
| A Comparison of the Physiological and Behavioral Effects of Suvorexant and Zolpidem in Healthy Volunteers: A Randomized, Double-blind, Placebo Controlled Study [NCT04273776] | Early Phase 1 | 90 participants (Anticipated) | Interventional | 2019-12-01 | Enrolling by invitation | ||
| Treatment of Disturbed Sleep in Progressive Supranuclear Palsy (PSP) [NCT04014387] | Phase 4 | 60 participants (Anticipated) | Interventional | 2019-06-02 | Recruiting | ||
| Can Blocking the Orexin System Enhance Sleep's Benefits to Therapeutic Exposure for PTSD? [NCT02849548] | Phase 4 | 27 participants (Actual) | Interventional | 2017-01-03 | Completed | ||
| An Open-Label, Single-Dose Study to Investigate the Pharmacokinetics of MK-4305 in Patients With Impaired Renal Function [NCT01059851] | Phase 1 | 16 participants (Actual) | Interventional | 2010-05-24 | Completed | ||
| Double-blind Randomized Controlled Trial Comparing Suvorexant 20 mg to Placebo for Treatment of Insomnia in Cancer Survivors [NCT06162663] | Phase 4 | 44 participants (Anticipated) | Interventional | 2024-01-31 | Not yet recruiting | ||
| Effect of Suvorexant on Sleep Disturbance in Patients With Chronic Insomnia and Suboptimally Controlled Type 2 Diabetes: A Randomized 3-month Clinical Trial Using a Sequential Parallel Comparison Design [NCT03818581] | Phase 4 | 108 participants (Actual) | Interventional | 2019-03-15 | Completed | ||
| A Randomized, Double-Blind, Placebo-Controlled Pilot Study of Suvorexant for Insomnia in Parkinson Disease [NCT02729714] | Phase 4 | 20 participants (Actual) | Interventional | 2016-04-30 | Completed | ||
| Role of the Orexin Receptor System in Stress, Sleep and Cocaine Use [NCT02785406] | Phase 2 | 20 participants (Actual) | Interventional | 2016-05-31 | Completed | ||
| A Phase IV 3-Way Double-blind, Randomized, Crossover Study to Compare the Awakening Threshold Effects (Responsivity) of Belsomra 10 mg and 20 mg to Placebo in Non-elderly Insomniacs [NCT03312517] | Phase 4 | 12 participants (Actual) | Interventional | 2018-04-15 | Completed | ||
| The Role of Orexin in Human Panic Disorder [NCT02593682] | Phase 4 | 3 participants (Actual) | Interventional | 2016-05-31 | Completed | ||
| A Double-blind, Crossover, Placebo-controlled Study to Compare the Effects of Nighttime Administration of Suvorexant in Patients With Multiple Sclerosis Fatigue and Insomnia [NCT03110315] | Phase 4 | 34 participants (Actual) | Interventional | 2017-03-28 | Completed | ||
| Medical Management of Sleep Disturbance During Opioid Tapering [NCT03789214] | Phase 2 | 90 participants (Actual) | Interventional | 2019-07-01 | Completed | ||
| A Randomized, Double-Blind, 6-Way Crossover Study to Determine the Abuse Potential of Single Oral Doses of Lemborexant Compared to Zolpidem, Suvorexant and Placebo in Healthy, Non-Dependent, Recreational Sedative Users [NCT03158025] | Phase 1 | 39 participants (Actual) | Interventional | 2017-04-19 | Completed | ||
| A Single Dose Study to Investigate the Pharmacokinetics of MK-4305 in Patients With Hepatic Insufficiency [NCT01043926] | Phase 1 | 16 participants (Actual) | Interventional | 2010-02-22 | Completed | ||
| Improvement of Restorative Sleep and Post-surgical Insomnia Following Suvorexant Administration [NCT05823844] | Phase 4 | 92 participants (Anticipated) | Interventional | 2023-05-31 | Not yet recruiting | ||
| [information is prepared from clinicaltrials.gov, extracted Sep-2024] | |||||||