Details of the Drug

General Information of Drug (ID: DM0E6S3)

Drug Name
Suvorexant
Synonyms
Suvorexant; 1030377-33-3; MK-4305; BELSOMRA; MK 4305; MK4305; UNII-081L192FO9; Suvorexant (MK-4305); [(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; (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; CHEMBL1083659; CHEBI:82698; 081L192FO9; C23H23ClN6O2; ((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
Indication
Disease Entry ICD 11 Status REF
Insomnia 7A00-7A0Z Approved [1]
Drug Type
Small molecular drug
Structure
3D MOL 2D MOL
#Ro5 Violations (Lipinski): 0 Molecular Weight (mw) 450.9
Logarithm of the Partition Coefficient (xlogp) 4.9
Rotatable Bond Count (rotbonds) 3
Hydrogen Bond Donor Count (hbonddonor) 0
Hydrogen Bond Acceptor Count (hbondacc) 6
ADMET Property
Absorption Tmax
The time to maximum plasma concentration (Tmax) is 2 h []
Bioavailability
The bioavailability of drug is 82% []
Clearance
The drug present in the plasma can be removed from the body at the rate of 0.84 mL/min/kg [2]
Half-life
The concentration or amount of drug in body reduced by one-half in 12 hours [2]
Metabolism
The drug is metabolized via the cytochrome-P450 3A4 enzyme (CYP3A4) with a minor contribution from CYP2C19 []
Unbound Fraction
The unbound fraction of drug in plasma is 0.05% [2]
Vd
The volume of distribution (Vd) of drug is 49 L []
Chemical Identifiers
Formula
C23H23ClN6O2
IUPAC Name
[(7R)-4-(5-chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl]-[5-methyl-2-(triazol-2-yl)phenyl]methanone
Canonical SMILES
C[C@@H]1CCN(CCN1C(=O)C2=C(C=CC(=C2)C)N3N=CC=N3)C4=NC5=C(O4)C=CC(=C5)Cl
InChI
InChI=1S/C23H23ClN6O2/c1-15-3-5-20(30-25-8-9-26-30)18(13-15)22(31)29-12-11-28(10-7-16(29)2)23-27-19-14-17(24)4-6-21(19)32-23/h3-6,8-9,13-14,16H,7,10-12H2,1-2H3/t16-/m1/s1
InChIKey
JYTNQNCOQXFQPK-MRXNPFEDSA-N
Cross-matching ID
PubChem CID
24965990
ChEBI ID
CHEBI:82698
CAS Number
1030377-33-3
DrugBank ID
DB09034
TTD ID
D00OVU
VARIDT ID
DR00487
INTEDE ID
DR1521
ACDINA ID
D00647
Combinatorial Drugs (CBD) Click to Jump to the Detailed CBD Information of This Drug

Molecular Interaction Atlas of This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Orexin receptor type 2 (HCRTR2) TT9N02I OX2R_HUMAN Modulator [3]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 3A4 (CYP3A4)
Main DME 		DE4LYSA CP3A4_HUMAN Substrate [4]
Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This Drug

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Disease Different from Suvorexant (Comorbidity)
DDI Drug Name DDI Drug ID Severity Mechanism Comorbidity REF
Metreleptin DM1NOEK Moderate Increased metabolism of Suvorexant caused by Metreleptin mediated induction of CYP450 enzyme. Acute diabete complication [5A2Y] [5]
Ivosidenib DM8S6T7 Moderate Increased metabolism of Suvorexant caused by Ivosidenib mediated induction of CYP450 enzyme. Acute myeloid leukaemia [2A60] [5]
Arn-509 DMT81LZ Major Increased metabolism of Suvorexant caused by Arn-509 mediated induction of CYP450 enzyme. Acute myeloid leukaemia [2A60] [5]
Gilteritinib DMTI0ZO Moderate Decreased clearance of Suvorexant due to the transporter inhibition by Gilteritinib. Acute myeloid leukaemia [2A60] [6]
Oliceridine DM6MDCF Major Additive CNS depression effects by the combination of Suvorexant and Oliceridine. Acute pain [MG31] [7]
Ivabradine DM0L594 Moderate Decreased metabolism of Suvorexant caused by Ivabradine mediated inhibition of CYP450 enzyme. Angina pectoris [BA40] [6]
Troleandomycin DMUZNIG Major Decreased metabolism of Suvorexant caused by Troleandomycin mediated inhibition of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [8]
Erdafitinib DMI782S Moderate Increased metabolism of Suvorexant caused by Erdafitinib mediated induction of CYP450 enzyme. Bladder cancer [2C94] [9]
Talazoparib DM1KS78 Moderate Decreased clearance of Suvorexant due to the transporter inhibition by Talazoparib. Breast cancer [2C60-2C6Y] [10]
Tucatinib DMBESUA Major Decreased metabolism of Suvorexant caused by Tucatinib mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [8]
Palbociclib DMD7L94 Moderate Decreased metabolism of Suvorexant caused by Palbociclib mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [8]
PF-04449913 DMSB068 Moderate Decreased metabolism of Suvorexant caused by PF-04449913 mediated inhibition of CYP450 enzyme. Chronic myelomonocytic leukaemia [2A40] [11]
Osilodrostat DMIJC9X Moderate Decreased metabolism of Suvorexant caused by Osilodrostat mediated inhibition of CYP450 enzyme. Cushing syndrome [5A70] [8]
Lumacaftor DMCLWDJ Major Increased metabolism of Suvorexant caused by Lumacaftor mediated induction of CYP450 enzyme. Cystic fibrosis [CA25] [12]
MK-8228 DMOB58Q Major Decreased metabolism of Suvorexant caused by MK-8228 mediated inhibition of CYP450 enzyme. Cytomegaloviral disease [1D82] [5]
Esketamine DMVU687 Moderate Additive CNS depression effects by the combination of Suvorexant and Esketamine. Depression [6A70-6A7Z] [8]
Polatuzumab vedotin DMF6Y0L Moderate Decreased metabolism of Suvorexant caused by Polatuzumab vedotin mediated inhibition of CYP450 enzyme. Diffuse large B-cell lymphoma [2A81] [13]
Eslicarbazepine DMZREFQ Moderate Increased metabolism of Suvorexant caused by Eslicarbazepine mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [5]
Tazemetostat DMWP1BH Moderate Decreased metabolism of Suvorexant caused by Tazemetostat mediated inhibition of CYP450 enzyme. Follicular lymphoma [2A80] [14]
Ripretinib DM958QB Moderate Decreased metabolism of Suvorexant caused by Ripretinib mediated inhibition of CYP450 enzyme. Gastrointestinal stromal tumour [2B5B] [8]
Avapritinib DMK2GZX Moderate Decreased metabolism of Suvorexant caused by Avapritinib mediated inhibition of CYP450 enzyme. Gastrointestinal stromal tumour [2B5B] [6]
MK-1439 DM215WE Minor Decreased metabolism of Suvorexant caused by MK-1439 mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [15]
Cobicistat DM6L4H2 Major Decreased metabolism of Suvorexant caused by Cobicistat mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [8]
Berotralstat DMWA2DZ Major Decreased metabolism of Suvorexant caused by Berotralstat mediated inhibition of CYP450 enzyme. Innate/adaptive immunodeficiency [4A00] [5]
Naloxegol DML0B41 Minor Decreased clearance of Suvorexant due to the transporter inhibition by Naloxegol. Large intestine motility disorder [DB32] [16]
Pemigatinib DM819JF Moderate Decreased metabolism of Suvorexant caused by Pemigatinib mediated inhibition of CYP450 enzyme. Liver cancer [2C12] [6]
Brigatinib DM7W94S Moderate Decreased metabolism of Suvorexant caused by Brigatinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [8]
Ceritinib DMB920Z Major Decreased metabolism of Suvorexant caused by Ceritinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [8]
Lurbinectedin DMEFRTZ Moderate Decreased metabolism of Suvorexant caused by Lurbinectedin mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [17]
PF-06463922 DMKM7EW Moderate Increased metabolism of Suvorexant caused by PF-06463922 mediated induction of CYP450 enzyme. Lung cancer [2C25] [5]
Osimertinib DMRJLAT Moderate Decreased metabolism of Suvorexant caused by Osimertinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [18]
Pralsetinib DMWU0I2 Moderate Decreased metabolism of Suvorexant caused by Pralsetinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [19]
Selpercatinib DMZR15V Moderate Decreased metabolism of Suvorexant caused by Selpercatinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [8]
Idelalisib DM602WT Major Decreased metabolism of Suvorexant caused by Idelalisib mediated inhibition of CYP450 enzyme. Mature B-cell leukaemia [2A82] [8]
GDC-0199 DMH0QKA Major Decreased clearance of Suvorexant due to the transporter inhibition by GDC-0199. Mature B-cell leukaemia [2A82] [8]
IPI-145 DMWA24P Major Decreased metabolism of Suvorexant caused by IPI-145 mediated inhibition of CYP450 enzyme. Mature B-cell leukaemia [2A82] [5]
Acalabrutinib DM7GCVW Moderate Decreased metabolism of Suvorexant caused by Acalabrutinib mediated inhibition of CYP450 enzyme. Mature B-cell lymphoma [2A85] [20]
Arry-162 DM1P6FR Moderate Decreased clearance of Suvorexant due to the transporter inhibition by Arry-162. Melanoma [2C30] [8]
Selumetinib DMC7W6R Moderate Decreased metabolism of Suvorexant caused by Selumetinib mediated inhibition of CYP450 enzyme. Melanoma [2C30] [21]
Allopregnanolone DMNLHAC Moderate Additive CNS depression effects by the combination of Suvorexant and Allopregnanolone. Mental/behavioural/neurodevelopmental disorder [6E20-6E8Z] [22]
Ubrogepant DM749I3 Moderate Decreased metabolism of Suvorexant caused by Ubrogepant mediated inhibition of CYP450 enzyme. Migraine [8A80] [23]
Lasmiditan DMXLVDT Moderate Additive CNS depression effects by the combination of Suvorexant and Lasmiditan. Migraine [8A80] [24]
Fedratinib DM4ZBK6 Major Decreased metabolism of Suvorexant caused by Fedratinib mediated inhibition of CYP450 enzyme. Myeloproliferative neoplasm [2A20] [5]
Netupitant DMEKAYI Major Decreased metabolism of Suvorexant caused by Netupitant mediated inhibition of CYP450 enzyme. Nausea/vomiting [MD90] [25]
Entrectinib DMMPTLH Moderate Decreased metabolism of Suvorexant caused by Entrectinib mediated inhibition of CYP450 enzyme. Non-small cell lung cancer [2C25] [26]
S-297995 DM26IH8 Moderate Decreased clearance of Suvorexant due to the transporter inhibition by S-297995. Opioid use disorder [6C43] [6]
Olaparib DM8QB1D Moderate Decreased metabolism of Suvorexant caused by Olaparib mediated inhibition of CYP450 enzyme. Ovarian cancer [2C73] [27]
Rucaparib DM9PVX8 Moderate Decreased metabolism of Suvorexant caused by Rucaparib mediated inhibition of CYP450 enzyme. Ovarian cancer [2C73] [8]
Abametapir DM2RX0I Moderate Decreased metabolism of Suvorexant caused by Abametapir mediated inhibition of CYP450 enzyme. Pediculosis [1G00] [28]
Lefamulin DME6G97 Moderate Decreased metabolism of Suvorexant caused by Lefamulin mediated inhibition of CYP450 enzyme. Pneumonia [CA40] [29]
Relugolix DMK7IWL Major Decreased clearance of Suvorexant due to the transporter inhibition by Relugolix. Prostate cancer [2C82] [30]
Voxelotor DMCS6M5 Moderate Decreased metabolism of Suvorexant caused by Voxelotor mediated inhibition of CYP450 enzyme. Sickle-cell disorder [3A51] [8]
LDE225 DMM9F25 Moderate Decreased metabolism of Suvorexant caused by LDE225 mediated inhibition of CYP450 enzyme. Skin cancer [2C30-2C37] [31]
Telotristat ethyl DMDIYFZ Moderate Increased metabolism of Suvorexant caused by Telotristat ethyl mediated induction of CYP450 enzyme. Small intestine developmental anomaly [DA90] [6]
Larotrectinib DM26CQR Moderate Decreased metabolism of Suvorexant caused by Larotrectinib mediated inhibition of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [8]
LEE011 DMMX75K Major Decreased metabolism of Suvorexant caused by LEE011 mediated inhibition of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [5]
Fostamatinib DM6AUHV Moderate Decreased metabolism of Suvorexant caused by Fostamatinib mediated inhibition of CYP450 enzyme. Thrombocytopenia [3B64] [32]
Lusutrombopag DMH6IKO Moderate Decreased clearance of Suvorexant due to the transporter inhibition by Lusutrombopag. Thrombocytopenia [3B64] [33]
Elagolix DMB2C0E Moderate Increased metabolism of Suvorexant caused by Elagolix mediated induction of CYP450 enzyme. Uterine fibroid [2E86] [5]
Betrixaban DM2C4RF Moderate Decreased clearance of Suvorexant due to the transporter inhibition by Betrixaban. Venous thromboembolism [BD72] [34]
⏷ Show the Full List of 60 DDI Information of This Drug

Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug

DIG
DIG Name DIG ID PubChem CID Functional Classification
FD&C blue no. 1 E00263 19700 Colorant
Carmellose sodium E00625 Not Available Disintegrant
Ferric hydroxide oxide yellow E00539 23320441 Colorant
Ferrosoferric oxide E00231 14789 Colorant
Lactose monohydrate E00393 104938 Binding agent; Diluent; Dry powder inhaler carrier; Lyophilization aid
Magnesium stearate E00208 11177 lubricant
Titanium dioxide E00322 26042 Coating agent; Colorant; Opacifying agent
Triacetin E00080 5541 Humectant; Plasticizing agent; Solvent
⏷ Show the Full List of 8 Pharmaceutical Excipients of This Drug
Pharmaceutical Formulation
Formulation Name Drug Dosage Dosage Form Route
Suvorexant 10 mg tablet 10 mg Oral Tablet Oral
Suvorexant 5 mg tablet 5 mg Oral Tablet Oral
Suvorexant 15 mg tablet 15 mg Oral Tablet Oral
Suvorexant 20 mg tablet 20 mg Oral Tablet Oral
Jump to Detail Pharmaceutical Formulation Page of This Drug

References

1 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2890).
2 Trend Analysis of a Database of Intravenous Pharmacokinetic Parameters in Humans for 1352 Drug Compounds
3 2014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81.
4 Suvorexant: a promising, novel treatment for insomnia. Neuropsychiatr Dis Treat. 2016 Feb 25;12:491-5.
5 Product Information. Belsomra (suvorexant). Merck & Company Inc, Whitehouse Station, NJ.
6 Cerner Multum, Inc. "UK Summary of Product Characteristics.".
7 US Food and Drug Administration "FDA warns about serious risks and death when combining opioid pain or cough medicines with benzodiazepines requires its strongest warning.".
8 Cerner Multum, Inc. "Australian Product Information.".
9 Product Information. Balversa (erdafitinib). Janssen Products, LP, Horsham, PA.
10 Product Information. Talzenna (talazoparib). Pfizer U.S. Pharmaceuticals Group, New York, NY.
11 Product Information. Daurismo (glasdegib). Pfizer U.S. Pharmaceuticals Group, New York, NY.
12 Patel S, Robinson R, Burk M "Hypertensive crisis associated with St. John's Wort." Am J Med 112 (2002): 507-8. [PMID: 11959071]
13 Product Information. Polivy (polatuzumab vedotin). Genentech, South San Francisco, CA.
14 Product Information. Tazverik (tazemetostat). Epizyme, Inc, Cambridge, MA.
15 Product Information. Pifeltro (doravirine). Merck & Company Inc, Whitehouse Station, NJ.
16 Product Information. Movantik (naloxegol). Astra-Zeneca Pharmaceuticals, Wilmington, DE.
17 Product Information. Zepzelca (lurbinectedin). Jazz Pharmaceuticals, Palo Alto, CA.
18 Product Information. Tagrisso (osimertinib). Astra-Zeneca Pharmaceuticals, Wilmington, DE.
19 Product Information. Gavreto (pralsetinib). Blueprint Medicines Corporation, Cambridge, MA.
20 Product Information. Calquence (acalabrutinib). Astra-Zeneca Pharmaceuticals, Wilmington, DE.
21 Product Information. Koselugo (selumetinib). Astra-Zeneca Pharmaceuticals, Wilmington, DE.
22 Product Information. Zulresso (brexanolone). Sage Therapeutics, Inc., Cambridge, MA.
23 Product Information. Ubrelvy (ubrogepant). Allergan Inc, Irvine, CA.
24 Product Information. Reyvow (lasmiditan). Lilly, Eli and Company, Indianapolis, IN.
25 Product Information. Belsomra (suvorexant). Merck &amp Company Inc, Whitehouse Station, NJ.
26 Product Information. Rozlytrek (entrectinib). Genentech, South San Francisco, CA.
27 Product Information. Lynparza (olaparib). Astra-Zeneca Pharmaceuticals, Wilmington, DE.
28 Product Information. Xeglyze (abametapir topical). Dr. Reddy's Laboratories Inc, Upper Saddle River, NJ.
29 Product Information. Xenleta (lefamulin). Nabriva Therapeutics US, Inc., King of Prussia, PA.
30 Product Information. Orgovyx (relugolix). Myovant Sciences, Inc., Brisbane, CA.
31 Product Information. Odomzo (sonidegib). Novartis Pharmaceuticals, East Hanover, NJ.
32 Product Information. Tavalisse (fostamatinib). Rigel Pharmaceuticals, South San Francisco, CA.
33 EMA. European Medicines Agency. European Union "EMA - List of medicines under additional monitoring.".
34 Product Information. Bevyxxa (betrixaban). Portola Pharmaceuticals, South San Francisco, CA.