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 | 516.49 | 22.37 | 526 | 4918 | 918463 | 55368160 |
Nightmare | 172.99 | 22.37 | 64 | 5380 | 16762 | 56269861 |
Abnormal dreams | 150.22 | 22.37 | 50 | 5394 | 9599 | 56277024 |
Insomnia | 140.83 | 22.37 | 129 | 5315 | 191731 | 56094892 |
Somnolence | 127.96 | 22.37 | 114 | 5330 | 163299 | 56123324 |
Sleep paralysis | 121.90 | 22.37 | 24 | 5420 | 547 | 56286076 |
Poor quality sleep | 90.95 | 22.37 | 41 | 5403 | 17714 | 56268909 |
Wrong technique in product usage process | 90.31 | 22.37 | 61 | 5383 | 58107 | 56228516 |
No adverse event | 83.78 | 22.37 | 49 | 5395 | 36325 | 56250298 |
Feeling abnormal | 73.74 | 22.37 | 77 | 5367 | 133525 | 56153098 |
Product dose omission issue | 71.15 | 22.37 | 93 | 5351 | 204660 | 56081963 |
Initial insomnia | 63.89 | 22.37 | 23 | 5421 | 5556 | 56281067 |
Product packaging quantity issue | 62.78 | 22.37 | 16 | 5428 | 1198 | 56285425 |
Hallucination | 54.39 | 22.37 | 42 | 5402 | 49107 | 56237516 |
Product blister packaging issue | 47.46 | 22.37 | 9 | 5435 | 167 | 56286456 |
Middle insomnia | 45.84 | 22.37 | 22 | 5422 | 10928 | 56275695 |
Altered state of consciousness | 40.18 | 22.37 | 26 | 5418 | 22995 | 56263628 |
Sleep terror | 39.27 | 22.37 | 10 | 5434 | 746 | 56285877 |
Therapeutic product effect incomplete | 34.93 | 22.37 | 47 | 5397 | 105984 | 56180639 |
Inappropriate schedule of product administration | 33.84 | 22.37 | 41 | 5403 | 83346 | 56203277 |
Sleep disorder | 32.00 | 22.37 | 36 | 5408 | 67627 | 56218996 |
Product quality issue | 30.55 | 22.37 | 25 | 5419 | 31711 | 56254912 |
Suicidal ideation | 27.78 | 22.37 | 31 | 5413 | 57711 | 56228912 |
Anxiety | 26.53 | 22.37 | 58 | 5386 | 193114 | 56093509 |
Delirium | 26.11 | 22.37 | 26 | 5418 | 42491 | 56244132 |
Circumstance or information capable of leading to medication error | 24.35 | 22.37 | 10 | 5434 | 3438 | 56283185 |
Headache | 23.21 | 22.37 | 111 | 5333 | 558933 | 55727690 |
Poor quality product administered | 22.51 | 22.37 | 9 | 5435 | 2890 | 56283733 |
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 | 384.85 | 22.95 | 323 | 3103 | 395250 | 31298668 |
Nightmare | 144.74 | 22.95 | 53 | 3373 | 12084 | 31681834 |
Abnormal dreams | 88.25 | 22.95 | 32 | 3394 | 7076 | 31686842 |
Somnolence | 86.01 | 22.95 | 77 | 3349 | 99368 | 31594550 |
Poor quality sleep | 78.59 | 22.95 | 30 | 3396 | 7648 | 31686270 |
Insomnia | 63.90 | 22.95 | 64 | 3362 | 94772 | 31599146 |
Wrong technique in product usage process | 62.50 | 22.95 | 41 | 3385 | 33302 | 31660616 |
Sleep paralysis | 52.29 | 22.95 | 10 | 3416 | 173 | 31693745 |
Hepatic function abnormal | 50.24 | 22.95 | 39 | 3387 | 41183 | 31652735 |
No adverse event | 49.07 | 22.95 | 29 | 3397 | 19596 | 31674322 |
Delirium | 43.67 | 22.95 | 36 | 3390 | 41385 | 31652533 |
Therapeutic product effect incomplete | 37.96 | 22.95 | 34 | 3392 | 43662 | 31650256 |
Sleep disorder | 36.66 | 22.95 | 27 | 3399 | 26321 | 31667597 |
Middle insomnia | 35.72 | 22.95 | 16 | 3410 | 6083 | 31687835 |
Hangover | 35.55 | 22.95 | 10 | 3416 | 975 | 31692943 |
Interstitial lung disease | 35.09 | 22.95 | 38 | 3388 | 61365 | 31632553 |
Product packaging quantity issue | 32.70 | 22.95 | 9 | 3417 | 810 | 31693108 |
Oesophageal dilatation | 29.67 | 22.95 | 6 | 3420 | 140 | 31693778 |
Initial insomnia | 28.44 | 22.95 | 11 | 3415 | 2898 | 31691020 |
Feeling abnormal | 26.98 | 22.95 | 32 | 3394 | 56970 | 31636948 |
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 | 666.33 | 20.33 | 646 | 7080 | 939106 | 69981612 |
Nightmare | 271.72 | 20.33 | 99 | 7627 | 22057 | 70898661 |
Abnormal dreams | 178.40 | 20.33 | 60 | 7666 | 10543 | 70910175 |
Somnolence | 169.78 | 20.33 | 159 | 7567 | 215447 | 70705271 |
Insomnia | 145.83 | 20.33 | 147 | 7579 | 217659 | 70703059 |
Sleep paralysis | 141.29 | 20.33 | 28 | 7698 | 583 | 70920135 |
Poor quality sleep | 137.04 | 20.33 | 59 | 7667 | 20290 | 70900428 |
Wrong technique in product usage process | 105.64 | 20.33 | 75 | 7651 | 68623 | 70852095 |
Feeling abnormal | 78.90 | 20.33 | 87 | 7639 | 142232 | 70778486 |
Initial insomnia | 76.54 | 20.33 | 28 | 7698 | 6281 | 70914437 |
Middle insomnia | 66.87 | 20.33 | 32 | 7694 | 14021 | 70906697 |
Delirium | 66.25 | 20.33 | 59 | 7667 | 74555 | 70846163 |
Hallucination | 65.14 | 20.33 | 59 | 7667 | 76201 | 70844517 |
Altered state of consciousness | 57.60 | 20.33 | 42 | 7684 | 39980 | 70880738 |
Sleep disorder | 53.75 | 20.33 | 51 | 7675 | 69821 | 70850897 |
Hepatic function abnormal | 53.01 | 20.33 | 50 | 7676 | 67946 | 70852772 |
Therapeutic product effect incomplete | 47.79 | 20.33 | 62 | 7664 | 119820 | 70800898 |
Hangover | 44.98 | 20.33 | 14 | 7712 | 1919 | 70918799 |
Interstitial lung disease | 43.07 | 20.33 | 55 | 7671 | 104630 | 70816088 |
Product packaging quantity issue | 42.96 | 20.33 | 12 | 7714 | 1130 | 70919588 |
Inappropriate schedule of product administration | 40.35 | 20.33 | 54 | 7672 | 107501 | 70813217 |
Therapeutic product effect delayed | 36.25 | 20.33 | 13 | 7713 | 2754 | 70917964 |
Suicidal ideation | 32.52 | 20.33 | 39 | 7687 | 69557 | 70851161 |
Somnambulism | 28.17 | 20.33 | 13 | 7713 | 5247 | 70915471 |
Sleep terror | 24.95 | 20.33 | 8 | 7718 | 1207 | 70919511 |
Product dose omission issue | 24.41 | 20.33 | 65 | 7661 | 217403 | 70703315 |
Oesophageal dilatation | 24.26 | 20.33 | 6 | 7720 | 352 | 70920366 |
Stoma site hypergranulation | 23.46 | 20.33 | 6 | 7720 | 403 | 70920315 |
Circumstance or information capable of leading to medication error | 22.81 | 20.33 | 10 | 7716 | 3580 | 70917138 |
Radiation pneumonitis | 22.54 | 20.33 | 10 | 7716 | 3683 | 70917035 |
Restlessness | 22.00 | 20.33 | 25 | 7701 | 42103 | 70878615 |
Anxiety | 21.90 | 20.33 | 63 | 7663 | 220267 | 70700451 |
Headache | 20.33 | 20.33 | 120 | 7606 | 580285 | 70340433 |
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 |