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]

ATC Code

N05CM19: Suvorexant

N05CM: Other hypnotics and sedatives

N05C: HYPNOTICS AND SEDATIVES

N05: PSYCHOLEPTICS

N: NERVOUS SYSTEM

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)

Hydrogen Bond Donor Count (hbonddonor)

Hydrogen Bond Acceptor Count (hbondacc)

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: CHEMBL1083659
CAS Number: 1030377-33-3
UNII: 081L192FO9
DrugBank ID: DB09034
TTD ID: D00OVU
VARIDT ID: DR00487
INTEDE ID: DR1521
ACDINA ID: D00647

Drug-Molecule Activity Atlas (DMA)^NEW

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Drug Pharmacogenomic Perturbation (DPP)^NEW

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Drug ADMET Endpoint Profile (DAE)^NEW

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Combinatorial Drugs (CBD)

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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)

MIA Detail

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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]


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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


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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

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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.