Evonik Evonik

X

Find Suvorexant manufacturers, exporters & distributors on PharmaCompass

PharmaCompass
API SUPPLIERS
API Suppliers

API Suppliers

US DMFs Filed

US DMFs Filed

0

CEP/COS Certifications

CEP/COS Certifications

0

JDMFs Filed

JDMFs Filed

0

Other Certificates

Other Certificates

0

Other Suppliers

Other Suppliers

API REF. PRICE (USD / KG)
INTERMEDIATES
DOSSIERS // FDF
USA (Orange Book)

USA (Orange Book)

Europe

Europe

0

Canada

Canada

0

Australia

Australia

0

South Africa

South Africa

0

Uploaded Dossiers

Uploaded Dossiers

0

GLOBAL SALES (USD Million)

U.S. Medicaid

Annual Reports

0

EXCIPIENTS
PATENTS & EXCLUSIVITIES

USFDA Orange Book Patents

USFDA Exclusivities

0

DIGITAL CONTENT

Blog #PharmaFlow

News

REF STANDARD

EDQM

0

USP

0

JP

0

Other Listed Suppliers

0

SERVICES

0

Suvorexant
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 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.


Ask Us for Pharmaceutical Supplier and Partner
Ask Us, Find A Supplier / Partner
No Commissions, No Strings Attached, Get Connected for FREE

What are you looking for?

How can we help you?

The request can't be empty

Please read our Privacy Policy carefully

You must agree to the privacy policy

The name can't be empty
The company can't be empty.
The email can't be empty Please enter a valid email.
The mobile can't be empty
Post Enquiry
POST ENQUIRY