Stem definition | Drug id | CAS RN |
---|---|---|
4881 | 1030377-33-3 |
None
Property | Value | Reference |
---|---|---|
Vd (Volume of distribution) | 0.69 L/kg | Lombardo F, Berellini G, Obach RS |
CL (Clearance) | 0.84 mL/min/kg | Lombardo F, Berellini G, Obach RS |
fu (Fraction unbound in plasma) | 0.05 % | Lombardo F, Berellini G, Obach RS |
t_half (Half-life) | 10.37 hours | Lombardo F, Berellini G, Obach RS |
Date | Agency | Company | Orphan |
---|---|---|---|
Aug. 13, 2014 | FDA | MERCK SHARP DOHME |
MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
---|---|---|---|---|---|---|
Drug ineffective | 526.62 | 21.60 | 513 | 4576 | 818820 | 49781215 |
Nightmare | 173.39 | 21.60 | 64 | 5025 | 16022 | 50584013 |
Abnormal dreams | 145.75 | 21.60 | 49 | 5040 | 9328 | 50590707 |
Somnolence | 121.42 | 21.60 | 110 | 4979 | 154875 | 50445160 |
Sleep paralysis | 116.57 | 21.60 | 23 | 5066 | 509 | 50599526 |
Poor quality sleep | 91.96 | 21.60 | 41 | 5048 | 16605 | 50583430 |
Wrong technique in product usage process | 88.36 | 21.60 | 60 | 5029 | 55450 | 50544585 |
No adverse event | 85.65 | 21.60 | 49 | 5040 | 33529 | 50566506 |
Feeling abnormal | 75.29 | 21.60 | 77 | 5012 | 125415 | 50474620 |
Product dose omission issue | 74.66 | 21.60 | 92 | 4997 | 183746 | 50416289 |
Product packaging quantity issue | 64.02 | 21.60 | 16 | 5073 | 1064 | 50598971 |
Initial insomnia | 53.76 | 21.60 | 20 | 5069 | 5095 | 50594940 |
Hallucination | 50.54 | 21.60 | 40 | 5049 | 46617 | 50553418 |
Product blister packaging issue | 48.02 | 21.60 | 9 | 5080 | 150 | 50599885 |
Middle insomnia | 47.10 | 21.60 | 22 | 5067 | 9899 | 50590136 |
Sleep terror | 39.32 | 21.60 | 10 | 5079 | 713 | 50599322 |
Altered state of consciousness | 37.98 | 21.60 | 25 | 5064 | 21885 | 50578150 |
Therapeutic product effect incomplete | 37.36 | 21.60 | 46 | 5043 | 91469 | 50508566 |
Inappropriate schedule of product administration | 32.41 | 21.60 | 38 | 5051 | 71793 | 50528242 |
Sleep disorder | 30.43 | 21.60 | 33 | 5056 | 57250 | 50542785 |
Product quality issue | 28.24 | 21.60 | 24 | 5065 | 30834 | 50569201 |
Suicidal ideation | 26.14 | 21.60 | 30 | 5059 | 55355 | 50544680 |
Headache | 25.97 | 21.60 | 110 | 4979 | 506425 | 50093610 |
Circumstance or information capable of leading to medication error | 24.73 | 21.60 | 10 | 5079 | 3178 | 50596857 |
Anxiety | 23.74 | 21.60 | 54 | 5035 | 177552 | 50422483 |
Poor quality product administered | 22.41 | 21.60 | 9 | 5080 | 2810 | 50597225 |
MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
---|---|---|---|---|---|---|
Drug ineffective | 394.82 | 22.89 | 315 | 2858 | 362855 | 29208499 |
Nightmare | 140.79 | 22.89 | 51 | 3122 | 11366 | 29559988 |
Abnormal dreams | 89.33 | 22.89 | 32 | 3141 | 6888 | 29564466 |
Somnolence | 82.24 | 22.89 | 73 | 3100 | 93882 | 29477472 |
Poor quality sleep | 80.55 | 22.89 | 30 | 3143 | 7203 | 29564151 |
Wrong technique in product usage process | 65.02 | 22.89 | 41 | 3132 | 31387 | 29539967 |
Sleep paralysis | 53.04 | 22.89 | 10 | 3163 | 161 | 29571193 |
Hepatic function abnormal | 52.20 | 22.89 | 39 | 3134 | 39220 | 29532134 |
No adverse event | 46.99 | 22.89 | 27 | 3146 | 17451 | 29553903 |
Delirium | 43.36 | 22.89 | 35 | 3138 | 39362 | 29531992 |
Therapeutic product effect incomplete | 37.19 | 22.89 | 32 | 3141 | 39273 | 29532081 |
Middle insomnia | 36.86 | 22.89 | 16 | 3157 | 5692 | 29565662 |
Sleep disorder | 36.41 | 22.89 | 26 | 3147 | 24360 | 29546994 |
Hangover | 35.70 | 22.89 | 10 | 3163 | 967 | 29570387 |
Interstitial lung disease | 31.94 | 22.89 | 35 | 3138 | 57683 | 29513671 |
Oesophageal dilatation | 29.75 | 22.89 | 6 | 3167 | 139 | 29571215 |
Product packaging quantity issue | 28.73 | 22.89 | 8 | 3165 | 757 | 29570597 |
Feeling abnormal | 28.38 | 22.89 | 32 | 3141 | 54413 | 29516941 |
Initial insomnia | 25.45 | 22.89 | 10 | 3163 | 2765 | 29568589 |
MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
---|---|---|---|---|---|---|
Drug ineffective | 687.39 | 20.28 | 632 | 6581 | 839615 | 63651904 |
Nightmare | 274.43 | 20.28 | 99 | 7114 | 20894 | 64470625 |
Abnormal dreams | 178.25 | 20.28 | 60 | 7153 | 10296 | 64481223 |
Somnolence | 168.20 | 20.28 | 156 | 7057 | 203489 | 64288030 |
Sleep paralysis | 143.10 | 20.28 | 28 | 7185 | 530 | 64490989 |
Poor quality sleep | 139.60 | 20.28 | 59 | 7154 | 18892 | 64472627 |
Wrong technique in product usage process | 107.66 | 20.28 | 75 | 7138 | 64899 | 64426620 |
Feeling abnormal | 81.58 | 20.28 | 87 | 7126 | 133515 | 64358004 |
Initial insomnia | 70.64 | 20.28 | 26 | 7187 | 5778 | 64485741 |
Middle insomnia | 68.74 | 20.28 | 32 | 7181 | 12845 | 64478674 |
Hallucination | 60.30 | 20.28 | 56 | 7157 | 72732 | 64418787 |
Delirium | 58.80 | 20.28 | 54 | 7159 | 69140 | 64422379 |
Altered state of consciousness | 56.38 | 20.28 | 41 | 7172 | 37861 | 64453658 |
Sleep disorder | 55.46 | 20.28 | 49 | 7164 | 59660 | 64431859 |
Hepatic function abnormal | 54.27 | 20.28 | 50 | 7163 | 64263 | 64427256 |
Therapeutic product effect incomplete | 50.48 | 20.28 | 60 | 7153 | 103422 | 64388097 |
Hangover | 44.85 | 20.28 | 14 | 7199 | 1887 | 64489632 |
Inappropriate schedule of product administration | 40.92 | 20.28 | 51 | 7162 | 92235 | 64399284 |
Interstitial lung disease | 40.16 | 20.28 | 52 | 7161 | 97680 | 64393839 |
Product packaging quantity issue | 39.97 | 20.28 | 11 | 7202 | 955 | 64490564 |
Therapeutic product effect delayed | 36.91 | 20.28 | 13 | 7200 | 2546 | 64488973 |
Suicidal ideation | 33.11 | 20.28 | 39 | 7174 | 66503 | 64425016 |
Product dose omission issue | 25.82 | 20.28 | 63 | 7150 | 194684 | 64296835 |
Somnambulism | 25.05 | 20.28 | 12 | 7201 | 5129 | 64486390 |
Sleep terror | 24.86 | 20.28 | 8 | 7205 | 1189 | 64490330 |
Oesophageal dilatation | 24.37 | 20.28 | 6 | 7207 | 336 | 64491183 |
Headache | 23.53 | 20.28 | 119 | 7094 | 529348 | 63962171 |
Circumstance or information capable of leading to medication error | 23.25 | 20.28 | 10 | 7203 | 3330 | 64488189 |
Restlessness | 20.92 | 20.28 | 24 | 7189 | 39761 | 64451758 |
None
Source | Code | Description |
---|---|---|
ATC | N05CM19 | NERVOUS SYSTEM PSYCHOLEPTICS HYPNOTICS AND SEDATIVES Other hypnotics and sedatives |
MeSH PA | D002491 | Central Nervous System Agents |
MeSH PA | D002492 | Central Nervous System Depressants |
MeSH PA | D006993 | Hypnotics and Sedatives |
MeSH PA | D018377 | Neurotransmitter Agents |
MeSH PA | D000068796 | Orexin Receptor Antagonists |
MeSH PA | D000068776 | Sleep Aids, Pharmaceutical |
FDA MoA | N0000185503 | P-Glycoprotein Inhibitors |
FDA MoA | N0000190114 | Cytochrome P450 3A Inhibitors |
FDA MoA | N0000190998 | Orexin Receptor Antagonists |
FDA EPC | N0000191000 | Orexin Receptor Antagonist |
CHEBI has role | CHEBI:35488 | central nervous system depressants |
CHEBI has role | CHEBI:83296 | orexin receptor antagonists |
Disease | Relation | SNOMED_ID | DOID |
---|---|---|---|
Insomnia | indication | 193462001 | |
Narcolepsy | contraindication | 60380001 | DOID:8986 |
None
None
Dissociation level | Dissociation constant | Type (acidic/basic) |
---|---|---|
pKa1 | 0.96 | Basic |
Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent use |
---|---|---|---|---|---|---|---|---|---|---|
10MG | BELSOMRA | MERCK SHARP DOHME | N204569 | Aug. 13, 2014 | RX | TABLET | ORAL | 7951797 | Nov. 20, 2029 | TREATMENT OF INSOMNIA |
15MG | BELSOMRA | MERCK SHARP DOHME | N204569 | Aug. 13, 2014 | RX | TABLET | ORAL | 7951797 | Nov. 20, 2029 | TREATMENT OF INSOMNIA |
20MG | BELSOMRA | MERCK SHARP DOHME | N204569 | Aug. 13, 2014 | RX | TABLET | ORAL | 7951797 | Nov. 20, 2029 | TREATMENT OF INSOMNIA |
5MG | BELSOMRA | MERCK SHARP DOHME | N204569 | Aug. 13, 2014 | RX | TABLET | ORAL | 7951797 | Nov. 20, 2029 | TREATMENT OF INSOMNIA |
Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
---|---|---|---|---|---|---|---|---|---|
10MG | BELSOMRA | MERCK SHARP DOHME | N204569 | Aug. 13, 2014 | RX | TABLET | ORAL | Jan. 29, 2023 | INFORMATION ADDED TO THE LABELING TO DESCRIBE STUDY P061, A RANDOMIZED, PLACEBO-CONTROLLED, PARALLEL GROUP, MULTI-SITE, DOUBLE-BLIND STUDY TO EVALUATE SAFETY AND EFFICACY OF SUVOREXANT FOR THE TREATMENT OF INSOMNIA IN SUBJECTS WITH ALZHEIMERS DISEASE |
15MG | BELSOMRA | MERCK SHARP DOHME | N204569 | Aug. 13, 2014 | RX | TABLET | ORAL | Jan. 29, 2023 | INFORMATION ADDED TO THE LABELING TO DESCRIBE STUDY P061, A RANDOMIZED, PLACEBO-CONTROLLED, PARALLEL GROUP, MULTI-SITE, DOUBLE-BLIND STUDY TO EVALUATE SAFETY AND EFFICACY OF SUVOREXANT FOR THE TREATMENT OF INSOMNIA IN SUBJECTS WITH ALZHEIMERS DISEASE |
20MG | BELSOMRA | MERCK SHARP DOHME | N204569 | Aug. 13, 2014 | RX | TABLET | ORAL | Jan. 29, 2023 | INFORMATION ADDED TO THE LABELING TO DESCRIBE STUDY P061, A RANDOMIZED, PLACEBO-CONTROLLED, PARALLEL GROUP, MULTI-SITE, DOUBLE-BLIND STUDY TO EVALUATE SAFETY AND EFFICACY OF SUVOREXANT FOR THE TREATMENT OF INSOMNIA IN SUBJECTS WITH ALZHEIMERS DISEASE |
5MG | BELSOMRA | MERCK SHARP DOHME | N204569 | Aug. 13, 2014 | RX | TABLET | ORAL | Jan. 29, 2023 | INFORMATION ADDED TO THE LABELING TO DESCRIBE STUDY P061, A RANDOMIZED, PLACEBO-CONTROLLED, PARALLEL GROUP, MULTI-SITE, DOUBLE-BLIND STUDY TO EVALUATE SAFETY AND EFFICACY OF SUVOREXANT FOR THE TREATMENT OF INSOMNIA IN SUBJECTS WITH ALZHEIMERS DISEASE |
Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
---|---|---|---|---|---|---|---|---|---|
Orexin receptor type 1 | GPCR | ANTAGONIST | Ki | 9.26 | SCIENTIFIC LITERATURE | SCIENTIFIC LITERATURE | |||
Orexin receptor type 2 | GPCR | ANTAGONIST | Ki | 9.46 | SCIENTIFIC LITERATURE | SCIENTIFIC LITERATURE | |||
Orexin receptor type 2 | GPCR | Ki | 8.06 | CHEMBL | |||||
Orexin receptor type 1 | GPCR | Ki | 8.77 | CHEMBL |
ID | Source |
---|---|
081L192FO9 | UNII |
D10082 | KEGG_DRUG |
4033910 | VUID |
N0000191283 | NUI |
4033910 | VANDF |
C3179535 | UMLSCUI |
CHEBI:82698 | CHEBI |
SUV | PDB_CHEM_ID |
CHEMBL1083659 | ChEMBL_ID |
24965990 | PUBCHEM_CID |
DB09034 | DRUGBANK_ID |
9435 | INN_ID |
C551624 | MESH_SUPPLEMENTAL_RECORD_UI |
2890 | IUPHAR_LIGAND_ID |
1547099 | RXNORM |
227824 | MMSL |
30487 | MMSL |
d08281 | MMSL |
015650 | NDDF |
708714001 | SNOMEDCT_US |
715609002 | SNOMEDCT_US |
Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
---|---|---|---|---|---|---|---|---|
BELSOMRA | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0006-0005 | TABLET, FILM COATED | 5 mg | ORAL | NDA | 36 sections |
BELSOMRA | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0006-0005 | TABLET, FILM COATED | 5 mg | ORAL | NDA | 36 sections |
BELSOMRA | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0006-0033 | TABLET, FILM COATED | 10 mg | ORAL | NDA | 36 sections |
BELSOMRA | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0006-0033 | TABLET, FILM COATED | 10 mg | ORAL | NDA | 36 sections |
BELSOMRA | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0006-0325 | TABLET, FILM COATED | 15 mg | ORAL | NDA | 36 sections |
BELSOMRA | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0006-0325 | TABLET, FILM COATED | 15 mg | ORAL | NDA | 36 sections |
BELSOMRA | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0006-0335 | TABLET, FILM COATED | 20 mg | ORAL | NDA | 36 sections |
BELSOMRA | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0006-0335 | TABLET, FILM COATED | 20 mg | ORAL | NDA | 36 sections |