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Chemistry

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Also known as: 1030377-33-3, Mk-4305, Belsomra, Mk4305, 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
Molecular Formula
C23H23ClN6O2
Molecular Weight
450.9  g/mol
InChI Key
JYTNQNCOQXFQPK-MRXNPFEDSA-N
FDA UNII
081L192FO9

Suvorexant
Suvorexant is a selective dual antagonist of orexin receptors OX1R and OX2R that promotes sleep by reducing wakefulness and arousal. It has been approved for the treatment of insomnia.
Suvorexant is an Orexin Receptor Antagonist. The mechanism of action of suvorexant is as an Orexin Receptor Antagonist, and P-Glycoprotein Inhibitor, and Cytochrome P450 3A Inhibitor.
1 2D Structure

Suvorexant

2 Identification
2.1 Computed Descriptors
2.1.1 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
2.1.2 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
2.1.3 InChI Key
JYTNQNCOQXFQPK-MRXNPFEDSA-N
2.1.4 Canonical SMILES
CC1CCN(CCN1C(=O)C2=C(C=CC(=C2)C)N3N=CC=N3)C4=NC5=C(O4)C=CC(=C5)Cl
2.1.5 Isomeric SMILES
C[C@@H]1CCN(CCN1C(=O)C2=C(C=CC(=C2)C)N3N=CC=N3)C4=NC5=C(O4)C=CC(=C5)Cl
2.2 Other Identifiers
2.2.1 UNII
081L192FO9
2.3 Synonyms
2.3.1 MeSH Synonyms

1. (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

2. Belsomra

3. 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)-

4. Mk 4305

5. Mk-4305

6. Mk4305

2.3.2 Depositor-Supplied Synonyms

1. 1030377-33-3

2. Mk-4305

3. Belsomra

4. Mk4305

5. Mk 4305

6. [(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

7. Suvorexant (mk-4305)

8. 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

9. Chembl1083659

10. Chebi:82698

11. 081l192fo9

12. ((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

13. 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)-

14. (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.

15. [(7r)-4-(5-chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl]-[5-methyl-2-(triazol-2-yl)phenyl]methanone

16. Suvorexant [usan:inn]

17. Dora-analogue

18. Unii-081l192fo9

19. Belsomra (tn)

20. Suv

21. Suvorexant [mi]

22. Suvorexant [inn]

23. Suvorexant [jan]

24. Suvorexant (jan/usan)

25. Suvorexant [usan]

26. Suvorexant; Mk 4305

27. Suvorexant [vandf]

28. Suvorexant [who-dd]

29. Amy337

30. Gtpl2890

31. Schembl1586289

32. Suvorexant [orange Book]

33. Dtxsid90145616

34. Ex-a211

35. Belsomra Component Suvorexant

36. Bdbm50318701

37. Mfcd22377755

38. Zinc49036447

39. Akos022185167

40. Cs-0614

41. Db09034

42. Suvorexant Component Of Belsomra

43. (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

44. Ac-30276

45. As-74879

46. Hy-10807

47. Bcp0726000197

48. Ft-0697203

49. Sw219649-1

50. D10082

51. J-690010

52. Q7650517

53. Cas:1030377-33-3;mk-4305

54. 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 Mk 4305

2.4 Create Date
2008-10-20
3 Chemical and Physical Properties
Molecular Weight 450.9 g/mol
Molecular Formula C23H23ClN6O2
XLogP34.9
Hydrogen Bond Donor Count0
Hydrogen Bond Acceptor Count6
Rotatable Bond Count3
Exact Mass450.1571017 g/mol
Monoisotopic Mass450.1571017 g/mol
Topological Polar Surface Area80.3 Ų
Heavy Atom Count32
Formal Charge0
Complexity664
Isotope Atom Count0
Defined Atom Stereocenter Count1
Undefined Atom Stereocenter Count0
Defined Bond Stereocenter Count0
Undefined Bond Stereocenter Count0
Covalently Bonded Unit Count1
4 Drug and Medication Information
4.1 Drug Indication

Suvorexant is indicated for the treatment of insomnia characterized by difficulties with sleep onset and/or sleep maintenance.


FDA Label


5 Pharmacology and Biochemistry
5.1 MeSH Pharmacological Classification

Orexin Receptor Antagonists

Substances that bind to and inhibit the action of OREXIN RECEPTORS. Drugs in this class have been used as SLEEP AIDS, PHARMACEUTICAL. (See all compounds classified as Orexin Receptor Antagonists.)


Sleep Aids, Pharmaceutical

Drugs used to induce SLEEP, prevent SLEEPLESSNESS, or treat SLEEP INITIATION AND MAINTENANCE DISORDERS. (See all compounds classified as Sleep Aids, Pharmaceutical.)


5.2 FDA Pharmacological Classification
5.2.1 Active Moiety
SUVOREXANT
5.2.2 FDA UNII
081L192FO9
5.2.3 Pharmacological Classes
Orexin Receptor Antagonist [EPC]; Orexin Receptor Antagonists [MoA]; P-Glycoprotein Inhibitors [MoA]; Cytochrome P450 3A Inhibitors [MoA]
5.3 ATC Code

N - Nervous system

N05 - Psycholeptics

N05C - Hypnotics and sedatives

N05CM - Other hypnotics and sedatives

N05CM19 - Suvorexant


5.4 Absorption, Distribution and Excretion

Absorption

Peak concentrations occur at a median Tmax of 2 hours under fasted conditions. Ingestion of suvorexant with a high-fat meal has no effect on AUC or Cmax, but may delay Tmax by approximately 1.5 hours. Mean absolute bioavailability of 10 mg is 82%.


Route of Elimination

Approximately 66% is eliminated in feces and 23% is eliminated in urine.


Volume of Distribution

Mean volume of distribution is approximately 49 litres.


5.5 Metabolism/Metabolites

Suvorexant is primarily metabolized by cytochrome-P450 3A4 enzyme (CYP3A4) with a minor contribution from CYP2C19. Major circulating metabolites are suvorexant and a hydroxy-suvorexant metabolite, which is not expected to be pharmacologically active. There is potential for drug-drug interactions with drugs that inhibit or induce CYP3A4 activity.


5.6 Biological Half-Life

Mean half life is approximately 12 hours.


5.7 Mechanism of Action

Suvorexant is a dual antagonist of orexin receptors OX1R and OX2R. It exerts its pharmacological effect by inhibiting binding of neuropeptides orexin A and B, also known as hypocretin 1 and 2, that are produced by neurons in the lateral hypothalamus. These neurons control the wake-promoting centers of the brain and are active during wakefulness, especially during motor activities, and stop firing during sleep. By inhibiting the reinforcement of arousal systems, suvorexant use causes a decrease in arousal and wakefulness, rather than having a direct sleep-promoting effect.


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01

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Company : Merck Sharp & D

Suvorexant

Drug Cost (USD) : 161,202,978

Year : 2023

Prescribers : 86387

Prescriptions : 329090

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02

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Company : Merck Sharp & D

Suvorexant

Drug Cost (USD) : 130,017,868

Year : 2022

Prescribers : 70601

Prescriptions : 280812

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03

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Company : Merck Sharp & D

Suvorexant

Drug Cost (USD) : 114,695,562

Year : 2021

Prescribers : 63614

Prescriptions : 262719

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04

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Company : Merck Sharp & D

Suvorexant

Drug Cost (USD) : 104,140,127

Year : 2020

Prescribers : 61153

Prescriptions : 253504

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05

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Biotech Showcase
Not Confirmed
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Biotech Showcase
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Company : Merck Sharp & D

Suvorexant

Drug Cost (USD) : 94,327,905

Year : 2019

Prescribers : 60260

Prescriptions : 243900

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06

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Company : Merck Sharp & D

Suvorexant

Drug Cost (USD) : 79,276,233

Year : 2018

Prescribers : 56312

Prescriptions : 220206

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07

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Company : Merck Sharp & D

Suvorexant

Drug Cost (USD) : 60,805,250

Year : 2017

Prescribers : 53169

Prescriptions : 190070

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08

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Company : Merck Sharp & D

Suvorexant

Drug Cost (USD) : 43,689,850

Year : 2016

Prescribers : 47836

Prescriptions : 150302

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Annual Reports

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01

Brand Name : Belsomra

Suvorexant

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Brand Name : Belsomra

U.S.A
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Suvorexant

Main Therapeutic Indication : CNS & Anesthesia

Currency : USD

2020 Revenue in Millions : 328

2019 Revenue in Millions : 306

Growth (%) : 7

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02

Brand Name : Belsomra

Suvorexant

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Brand Name : Belsomra

U.S.A
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Suvorexant

Main Therapeutic Indication : Sleep

Currency : USD

2021 Revenue in Millions : 318

2020 Revenue in Millions : 328

Growth (%) : -3

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03

Brand Name : Belsomra

Suvorexant

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Brand Name : Belsomra

U.S.A
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Not Confirmed

Suvorexant

Main Therapeutic Indication : Sleep

Currency : USD

2022 Revenue in Millions : 258

2021 Revenue in Millions : 318

Growth (%) : -19

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04

Brand Name : Belsomra

Suvorexant

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Brand Name : Belsomra

U.S.A
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Suvorexant

Main Therapeutic Indication : Sleep

Currency : USD

2023 Revenue in Millions : 231

2022 Revenue in Millions : 258

Growth (%) : -10

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05

Brand Name : Belsomra

Suvorexant

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Brand Name : Belsomra

U.S.A
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Suvorexant

Main Therapeutic Indication : Sleep

Currency : USD

2024 Revenue in Millions : 222

2023 Revenue in Millions : 231

Growth (%) : -4

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06

Brand Name : Belsomra

Suvorexant

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Brand Name : Belsomra

U.S.A
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Suvorexant

Main Therapeutic Indication : CNS & Anesthesia

Currency : USD

2019 Revenue in Millions : 306

2018 Revenue in Millions : 260

Growth (%) : 18

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Patents & EXCLUSIVITIES

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ABOUT THIS PAGE

Looking for 1030377-33-3 / Suvorexant API manufacturers, exporters & distributors?

Suvorexant manufacturers, exporters & distributors 1

23

PharmaCompass offers a list of Suvorexant API manufacturers, exporters & distributors, which can be sorted by GMP, USDMF, JDMF, KDMF, CEP (COS), WC, Price,and more, enabling you to easily find the right Suvorexant manufacturer or Suvorexant supplier for your needs.

Send us enquiries for free, and we will assist you in establishing a direct connection with your preferred Suvorexant manufacturer or Suvorexant supplier.

PharmaCompass also assists you with knowing the Suvorexant API Price utilized in the formulation of products. Suvorexant API Price is not always fixed or binding as the Suvorexant Price is obtained through a variety of data sources. The Suvorexant Price can also vary due to multiple factors, including market conditions, regulatory modifications, or negotiated pricing deals.

API | Excipient name

Suvorexant

Synonyms

1030377-33-3, Mk-4305, Belsomra, Mk4305, 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

Cas Number

1030377-33-3

Unique Ingredient Identifier (UNII)

081L192FO9

About Suvorexant

Suvorexant is a selective dual antagonist of orexin receptors OX1R and OX2R that promotes sleep by reducing wakefulness and arousal. It has been approved for the treatment of insomnia.

SUVOREXANT (2) Manufacturers

A SUVOREXANT (2) manufacturer is defined as any person or entity involved in the manufacture, preparation, processing, compounding or propagation of SUVOREXANT (2), including repackagers and relabelers. The FDA regulates SUVOREXANT (2) manufacturers to ensure that their products comply with relevant laws and regulations and are safe and effective to use. SUVOREXANT (2) API Manufacturers are required to adhere to Good Manufacturing Practices (GMP) to ensure that their products are consistently manufactured to meet established quality criteria.

click here to find a list of SUVOREXANT (2) manufacturers with USDMF, JDMF, KDMF, CEP, GMP, COA and API Price related information on PhamaCompass.

SUVOREXANT (2) Suppliers

A SUVOREXANT (2) supplier is an individual or a company that provides SUVOREXANT (2) active pharmaceutical ingredient (API) or SUVOREXANT (2) finished formulations upon request. The SUVOREXANT (2) suppliers may include SUVOREXANT (2) API manufacturers, exporters, distributors and traders.

click here to find a list of SUVOREXANT (2) suppliers with USDMF, JDMF, KDMF, CEP, GMP, COA and API Price related information on PharmaCompass.

SUVOREXANT (2) USDMF

A SUVOREXANT (2) DMF (Drug Master File) is a document detailing the whole manufacturing process of SUVOREXANT (2) active pharmaceutical ingredient (API) in detail. Different forms of SUVOREXANT (2) DMFs exist exist since differing nations have different regulations, such as SUVOREXANT (2) USDMF, ASMF (EDMF), JDMF, CDMF, etc.

A SUVOREXANT (2) DMF submitted to regulatory agencies in the US is known as a USDMF. SUVOREXANT (2) USDMF includes data on SUVOREXANT (2)'s chemical properties, information on the facilities and procedures used, and details about packaging and storage. The SUVOREXANT (2) USDMF is kept confidential to protect the manufacturer’s intellectual property.

click here to find a list of SUVOREXANT (2) suppliers with USDMF on PharmaCompass.

SUVOREXANT (2) NDC

National Drug Code is a comprehensive database maintained by the FDA that contains information on all drugs marketed in the US. This directory includes information about finished drug products, unfinished drug products, and compounded drug products, including those containing SUVOREXANT (2) as an active pharmaceutical ingredient (API).

Finished drug products

The FDA updates the NDC directory daily. The NDC numbers for SUVOREXANT (2) API and other APIs are published in this directory by the FDA.

Unfinished drugs

The NDC unfinished drugs database includes product listing information submitted for all unfinished drugs, such as active pharmaceutical ingredients (APIs), drugs intended for further processing and bulk drug substances for compounding.

Pharmaceutical companies that manufacture SUVOREXANT (2) as an active pharmaceutical ingredient (API) must furnish the FDA with an updated record of all drugs that they produce, prepare, propagate, compound, or process for commercial distribution in the US at their facilities.

Compounded drug products

The NDC directory also contains data on finished compounded human drug products that contain SUVOREXANT (2) and are produced by outsourcing facilities. While these outsourcing facilities are not mandated to assign a SUVOREXANT (2) NDC to their finished compounded human drug products, they may choose to do so.

click here to find a list of SUVOREXANT (2) suppliers with NDC on PharmaCompass.

SUVOREXANT (2) GMP

SUVOREXANT (2) Active pharmaceutical ingredient (API) is produced in GMP-certified manufacturing facility.

GMP stands for Good Manufacturing Practices, which is a system used in the pharmaceutical industry to make sure that goods are regularly produced and monitored in accordance with quality standards. The FDA’s current Good Manufacturing Practices requirements are referred to as cGMP or current GMP which indicates that the company follows the most recent GMP specifications. The World Health Organization (WHO) has its own set of GMP guidelines, called the WHO GMP. Different countries can also set their own guidelines for GMP like China (Chinese GMP) or the EU (EU GMP).

PharmaCompass offers a list of SUVOREXANT (2) GMP manufacturers, exporters & distributors, which can be sorted by USDMF, JDMF, KDMF, CEP (COS), WC, API price, and more, enabling you to easily find the right SUVOREXANT (2) GMP manufacturer or SUVOREXANT (2) GMP API supplier for your needs.

SUVOREXANT (2) CoA

A SUVOREXANT (2) CoA (Certificate of Analysis) is a formal document that attests to SUVOREXANT (2)'s compliance with SUVOREXANT (2) specifications and serves as a tool for batch-level quality control.

SUVOREXANT (2) CoA mostly includes findings from lab analyses of a specific batch. For each SUVOREXANT (2) CoA document that a company creates, the USFDA specifies specific requirements, such as supplier information, material identification, transportation data, evidence of conformity and signature data.

SUVOREXANT (2) may be tested according to a variety of international standards, such as European Pharmacopoeia (SUVOREXANT (2) EP), SUVOREXANT (2) JP (Japanese Pharmacopeia) and the US Pharmacopoeia (SUVOREXANT (2) USP).

Inform the supplier about your product requirements, specifying if you need a product with particular monograph like EP (Ph. Eur.), USP, JP, BP, or any other quality. In addition, clarify whether you need hydrochloride (HCl), anhydricum, base, micronisatum or a specific level of purity. To find reputable suppliers, utilize the filters and select those certified by GMP, FDA, or any other certification as per your requirement.
For your convenience, we have listed synonyms and CAS numbers to help you find the best supplier. The use of synonyms and CAS numbers can be helpful in identifying potential suppliers, but it is crucial to note that they might not always indicate the exact same product. It is important to confirm the product details with the supplier before making a purchase to ensure that it meets your requirements.
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