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Chemistry

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Also known as: 1369764-02-2, Dayvigo, E-2006, E2006, 0k5743g68x, (1r,2s)-2-[(2,4-dimethylpyrimidin-5-yl)oxymethyl]-2-(3-fluorophenyl)-n-(5-fluoropyridin-2-yl)cyclopropane-1-carboxamide
Molecular Formula
C22H20F2N4O2
Molecular Weight
410.4  g/mol
InChI Key
MUGXRYIUWFITCP-PGRDOPGGSA-N
FDA UNII
0K5743G68X

Lemborexant
Lemborexant is a novel dual orexin receptor antagonist used in the treatment of insomnia characterized by difficulties with sleep onset and/or sleep maintenance. Recent research in the field of sleep disorders has revealed that insomnia is likely driven not by the inability of the brain to "switch on" sleep-related circuits, but rather an inability to "switch-off" wake-promoting circuits. Whereas historically popular pharmacologic treatments for insomnia (e.g. [zopiclone], [zolpidem], benzodiazepines) focus on enhancing sleep drive via modulation of GABA and melatonin receptors, lemborexant and other orexin antagonists (e.g. [suvorexant]) act to counteract inappropriate wakefulness. This novel mechanism of action offers potential advantages over classic hypnotic agents, including a more favorable adverse effect profile and potentially greater efficacy, and may signal the beginning of a new wave of treatment options for patients suffering from insomnia.
Lemborexant is an Orexin Receptor Antagonist. The mechanism of action of lemborexant is as an Orexin Receptor Antagonist, and Cytochrome P450 2B6 Inducer.
1 2D Structure

Lemborexant

2 Identification
2.1 Computed Descriptors
2.1.1 IUPAC Name
(1R,2S)-2-[(2,4-dimethylpyrimidin-5-yl)oxymethyl]-2-(3-fluorophenyl)-N-(5-fluoropyridin-2-yl)cyclopropane-1-carboxamide
2.1.2 InChI
InChI=1S/C22H20F2N4O2/c1-13-19(11-25-14(2)27-13)30-12-22(15-4-3-5-16(23)8-15)9-18(22)21(29)28-20-7-6-17(24)10-26-20/h3-8,10-11,18H,9,12H2,1-2H3,(H,26,28,29)/t18-,22+/m0/s1
2.1.3 InChI Key
MUGXRYIUWFITCP-PGRDOPGGSA-N
2.1.4 Canonical SMILES
CC1=NC(=NC=C1OCC2(CC2C(=O)NC3=NC=C(C=C3)F)C4=CC(=CC=C4)F)C
2.1.5 Isomeric SMILES
CC1=NC(=NC=C1OC[C@]2(C[C@H]2C(=O)NC3=NC=C(C=C3)F)C4=CC(=CC=C4)F)C
2.2 Other Identifiers
2.2.1 UNII
0K5743G68X
2.3 Synonyms
2.3.1 MeSH Synonyms

1. (1r,2s)-2-(((2,4-dimethyl-5-pyrimidinyl)oxy)methyl)-2-(3-fluorophenyl)-n-(5-fluoro-2-pyridinyl)cyclopropanecarboxamide

2. Cyclopropanecarboxamide, 2-(((2,4-dimethyl-5-pyrimidinyl)oxy)methyl)-2-(3-fluorophenyl)-n-(5-fluoro-2-pyridinyl)-, (1r,2s)-

3. Dayvigo

2.3.2 Depositor-Supplied Synonyms

1. 1369764-02-2

2. Dayvigo

3. E-2006

4. E2006

5. 0k5743g68x

6. (1r,2s)-2-[(2,4-dimethylpyrimidin-5-yl)oxymethyl]-2-(3-fluorophenyl)-n-(5-fluoropyridin-2-yl)cyclopropane-1-carboxamide

7. (1r,2s)-2-(((2,4-dimethylpyrimidin-5-yl)oxy)methyl)-2-(3-fluorophenyl)-n-(5-fluoropyridin-2-yl)cyclopropanecarboxamide

8. Cyclopropanecarboxamide, 2-(((2,4-dimethyl-5-pyrimidinyl)oxy)methyl)-2-(3-fluorophenyl)-n-(5-fluoro-2-pyridinyl)-, (1r,2s)-

9. (1~{r},2~{s})-2-[(2,4-dimethylpyrimidin-5-yl)oxymethyl]-~{n}-(5-fluoranylpyridin-2-yl)-2-(3-fluorophenyl)cyclopropane-1-carboxamide

10. E 2006

11. Lemborexant [usan:inn]

12. Unii-0k5743g68x

13. (1r,2s)-2-(((2,4-dimethyl-5-pyrimidinyl)oxy)methyl)-2-(3-fluorophenyl)-n-(5-fluoro-2-pyridinyl)cyclopropanecarboxamide

14. (1r,2s)-2-((2,4-dimethylpyrimidin-5-yl)oxymethyl)-2-(3-fluorophenyl)-n-(5-fluoropyridin-2-yl)cyclopropane-1-carboxamide

15. (1r,2s)-2-[[(2,4-dimethyl-5-pyrimidinyl)oxy]methyl]-2-(3-fluorophenyl)-n-(5-fluoro-2-pyridinyl)cyclopropanecarboxamide

16. Cyclopropanecarboxamide, 2-[[(2,4-dimethyl-5-pyrimidinyl)oxy]methyl]-2-(3-fluorophenyl)-n-(5-fluoro-2-pyridinyl)-, (1r,2s)-

17. Dayvigo (tn)

18. Lemborexant [inn]

19. Lemborexant(e2006)

20. Lemborexant [mi]

21. Lemborexant; E-2006

22. Lemborexant [jan]

23. Lemborexant [usan]

24. Lemborexant [who-dd]

25. Lemborexant (jan/usan/inn)

26. Gtpl9302

27. Schembl2116558

28. Chembl3545367

29. Lemborexant [orange Book]

30. Dtxsid401027940

31. Amy27888

32. Ex-a2337

33. Bdbm50093793

34. Zinc118073503

35. Db11951

36. Compound 34 [pmid: 25953512]

37. Ncgc00488783-01

38. Ac-30918

39. Hy-16725

40. J3.610.985h

41. D11022

42. E-2006e-2006

43. A886588

44. Q20707990

45. (1r,2s)-2-{[(2,4-dimethylpyrimidin-5-yl)oxy]methyl}-2-(3-fluorophenyl)-n-(5-fluoropyridin-2-yl)cyclopropane-1-carboxamide

2.4 Create Date
2012-04-23
3 Chemical and Physical Properties
Molecular Weight 410.4 g/mol
Molecular Formula C22H20F2N4O2
XLogP33.2
Hydrogen Bond Donor Count1
Hydrogen Bond Acceptor Count7
Rotatable Bond Count6
Exact Mass410.15543222 g/mol
Monoisotopic Mass410.15543222 g/mol
Topological Polar Surface Area77 Ų
Heavy Atom Count30
Formal Charge0
Complexity612
Isotope Atom Count0
Defined Atom Stereocenter Count2
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

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


FDA Label


5 Pharmacology and Biochemistry
5.1 Pharmacology

Lemborexant promotes sleep by antagonizing the actions of wake-promoting chemicals in the brain. Episodes of complex sleep behaviors (e.g. eating food, having sex, making phone calls) have been reported in patients using lemborexant - these events may occur in hypnotic-naive and hyponotic-experienced patients, and patients are unlikely to remember these events. Patients exhibiting complex sleep behaviors should discontinue lemborexant immediately. Lemborexant may carry some risk of abuse, and should be used with caution in patients with a history of alcohol or drug addiction. Its controlled substance schedule is currently under review by the Drug Enforcement Administration.


5.2 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.)


5.3 FDA Pharmacological Classification
5.3.1 Active Moiety
LEMBOREXANT
5.3.2 FDA UNII
0K5743G68X
5.3.3 Pharmacological Classes
Orexin Receptor Antagonist [EPC]; Orexin Receptor Antagonists [MoA]; Cytochrome P450 2B6 Inducers [MoA]
5.4 ATC Code

N - Nervous system

N05 - Psycholeptics

N05C - Hypnotics and sedatives

N05CM - Other hypnotics and sedatives

N05CM21 - Lemborexant


5.5 Absorption, Distribution and Excretion

Absorption

Animal models of lemborexant disposition have demonstrated rapid absorption following oral administration. The Tmax of lemborexant is approximately 1-3 hours, or 3-5 hours following administration of a high-fat, high-calorie meal. Cmax and AUC0-24h increase at a rate slightly less than proportionate to the given dose. Following administration of a high-fat, high-calorie meal, Cmax is decreased by 23% and AUC0-inf is increased by 18%. AUC, Cmax, and terminal half-life are increased in the presence of moderate hepatic impairment, and AUC (but not half-life) is increased in the presence of mild hepatic impairment.


Route of Elimination

Following oral administration, 57.4% of the dose is found in the feces and 29.1% in the urine. Less than 1% of the dose recovered in the urine exists as unchanged parent drug, suggesting extensive metabolism.


Volume of Distribution

The volume of distribution of lemborexant is 1970 L, indicating extensive tissue distribution.


5.6 Metabolism/Metabolites

Given that less than 1% of an administered dose is recovered unchanged in the urine, it is likely that lemborexant is extensively metabolized - this has been confirmed in rat and monkey models, but its metabolism in humans has not been fully characterized. Prescribing information states that it is predominantly metabolized by CYP3A4, with a smaller contribution by CYP3A5. The major circulating metabolite is lemborexant's M10 metabolite, which is pharmacologically active and binds to orexin receptors with a similar affinity to the parent drug. The M10 metabolite has the potential to induce CYP3A and CYP2B6 enzymes, weakly inhibit CYP3A enzymes, and is a substrate of P-gp transporters.


5.7 Biological Half-Life

The half-life for lemborexant at doses of 5mg and 10mg is 17 and 19 hours, respectively.


5.8 Mechanism of Action

The orexin neuropeptide signaling system is involved in many physiologic functions, including sleep/wake control. Orexin-A and orexin-B activate post-synaptic G-protein coupled orexin-1 receptors (OX1R) and orexin-2 receptors (OX2R), which are found on neurons in the hypothalamus that project to numerous wake-controlling nuclei. Each receptor carries slightly different activity - activation of OX1R appears to suppress the onset of rapid eye movement (REM) sleep, whereas activation of OX2R appears to suppress non-REM sleep. Lemborexant is an competitive antagonist of OX1R and OX2R. By blocking the binding of wake-promoting orexin-A and -B at these receptors, lemborexant suppresses the wake-drive, thereby promoting sleep.


Listed Suppliers

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Virtual BoothQingmu Pharma: Patients first, FDA/CEP/US-DMF/US-VMF/ASMF APIs for Humans & Vets in 100+ countries.

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Lemborexant

About the Company : Sichuan Qingmu Pharmaceutical Co., Ltd. is an innovation-driven pharmaceutical company focused on regulated markets. We specialize in the R&D and manufacturing of generic APIs and ...

Sichuan Qingmu Pharmaceutical Co., Ltd. is an innovation-driven pharmaceutical company focused on regulated markets. We specialize in the R&D and manufacturing of generic APIs and advanced intermediates, and also offer high-quality CDMO/CMO services for small-molecule drugs. Qingmu has been inspected and approved by global regulatory authorities such as the US FDA, Korea MFDS, and China NMPA, and has earned client approvals across the U.S., Europe, Japan, and China. With strong technical capabilities and a commitment to international quality standards, we support customers from early development through to commercial supply.
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Virtual BoothMoehs Group, a reference company in the production of pharmaceutical active ingredients.

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About the Company : Since 1962, MOEHS has produced high-quality Active Pharmaceutical Ingredients (APIs) for the global market. With decades of technical expertise, Moehs Group delivers pharmaceutical...

Since 1962, MOEHS has produced high-quality Active Pharmaceutical Ingredients (APIs) for the global market. With decades of technical expertise, Moehs Group delivers pharmaceutical, veterinary, agrochemical, nutraceutical, cosmetic, and fine chemical products. Our facilities meet the highest standards, including GMP, ICH, FDA, and TGA approvals, ensuring reliable and safe manufacturing. Note: None of the products will be supplied to countries in which this could be in conflict with existing patents. Further, any products under patent will be offered for R&D purposes only.
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Virtual BoothTAPI, a leading global supplier of APIs, provides over 350 products and customized CDMO solutions for every stage of development.

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Lemborexant

About the Company : Founded in 1935, TAPI Technology & API Services has a long-standing tradition of advancing health through innovation and dedication. Today, we proudly build upon this legacy, drivi...

Founded in 1935, TAPI Technology & API Services has a long-standing tradition of advancing health through innovation and dedication. Today, we proudly build upon this legacy, driving progress in the pharmaceutical industry. Leveraging our extensive experience and world-class expertise, we deliver one of the most comprehensive API portfolios in the industry with over 350 Products portfolio. Additionally, we provide tailored CDMO services, harnessing our proficiency in diverse technologies to meet our partners' unique needs, ensuring flexibility and excellence in every project.
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Lemborexant

About the Company : Bajaj Healthcare Ltd. is a company established in 1993, services various Pharmaceuticals, Nutraceutical and Food industries globally with a spirit of scrupulousness. Bajaj Healt...

Bajaj Healthcare Ltd. is a company established in 1993, services various Pharmaceuticals, Nutraceutical and Food industries globally with a spirit of scrupulousness. Bajaj Healthcare Ltd. have metamorphosed into specialty company and focused on development, manufacturing and supply of Amino Acids, Nutritional Supplements and Active Pharmaceutical Ingredients (API) for Pharmaceutical, Nutraceuticals and Food industries. Bajaj healthcare Ltd. in its shot life span has gained loyalty from national and international customers and our products enjoy good fame in the overseas market.
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Lemborexant

About the Company : Beijing Sjar Technology Development Co., Ltd. founded in 2014, it is a high-tech enterprise which specialized in the research and development of active pharmaceutical ingredients a...

Beijing Sjar Technology Development Co., Ltd. founded in 2014, it is a high-tech enterprise which specialized in the research and development of active pharmaceutical ingredients and their intermediates, electronic chemical materials and intermediates, large-scale production, sales and services, and provide customized synthetic services according to customer requirements. Sjar-Tech locates in Beijing Economic and Technological Development Zone, has its own R&D and development laboratory. Sjar-Tech has set up a R&D team with rich experience and strong technical strength, most of the practitioners have more than ten years' experience.
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Lemborexant

About the Company : Bulat Pharmaceutical is a fast growing pharmaceutical company, founded in the year 2017, Bulat Pharmaceutical is engaged in the manufacturing and sales of high quality APIs and Int...

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Drugs in Development

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  • Development Update

Details:

Lemborexant is a Controlled Substance drug candidate, which is currently being evaluated in phase IV clinical studies for the treatment of Sleep Disorders, Circadian Rhythm.


Lead Product(s): Lemborexant,Inapplicable

Therapeutic Area: Sleep Brand Name: Undisclosed

Study Phase: Phase IVProduct Type: Controlled Substance

Sponsor: Eisai | Stanford University

Deal Size: Inapplicable Upfront Cash: Inapplicable

Deal Type: Inapplicable March 13, 2025

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University of California, San Francisco

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University of California, San Francisco

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Lead Product(s) : Lemborexant,Inapplicable

Therapeutic Area : Sleep

Highest Development Status : Phase IV

Partner/Sponsor/Collaborator : Eisai | Stanford University

Deal Size : Inapplicable

Deal Type : Inapplicable

Details : Lemborexant is a Controlled Substance drug candidate, which is currently being evaluated in phase IV clinical studies for the treatment of Sleep Disorders, Circadian Rhythm.

Product Name : Undisclosed

Product Type : Controlled Substance

Upfront Cash : Inapplicable

March 13, 2025

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  • Development Update

Details:

Lemborexant is a Controlled Substance drug candidate, which is currently being evaluated in phase II clinical studies for the treatment of Depressive Disorder, Major.


Lead Product(s): Lemborexant,Inapplicable

Therapeutic Area: Psychiatry/Psychology Brand Name: Undisclosed

Study Phase: Phase IIProduct Type: Controlled Substance

Sponsor: University of Toronto | Centre for Addiction and Mental Health | Toronto Metropolitan University

Deal Size: Inapplicable Upfront Cash: Inapplicable

Deal Type: Inapplicable February 24, 2025

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Unity Health Toronto

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Unity Health Toronto

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Lead Product(s) : Lemborexant,Inapplicable

Therapeutic Area : Psychiatry/Psychology

Highest Development Status : Phase II

Partner/Sponsor/Collaborator : University of Toronto | Centre for Addiction and Mental Health | Toronto Metropolitan University

Deal Size : Inapplicable

Deal Type : Inapplicable

Details : Lemborexant is a Controlled Substance drug candidate, which is currently being evaluated in phase II clinical studies for the treatment of Depressive Disorder, Major.

Product Name : Undisclosed

Product Type : Controlled Substance

Upfront Cash : Inapplicable

February 24, 2025

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  • Development Update

Details:

Lemborexant is a Controlled Substance drug candidate, which is currently being evaluated in clinical studies for the treatment of Sleep Initiation and Maintenance Disorders.


Lead Product(s): Lemborexant,Inapplicable

Therapeutic Area: Sleep Brand Name: Undisclosed

Study Phase: UndisclosedProduct Type: Controlled Substance

Sponsor: Toronto Metropolitan University | The Royal Ottawa Mental Health Centre

Deal Size: Inapplicable Upfront Cash: Inapplicable

Deal Type: Inapplicable January 16, 2025

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Laval University

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Laval University

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Lead Product(s) : Lemborexant,Inapplicable

Therapeutic Area : Sleep

Highest Development Status : Undisclosed

Partner/Sponsor/Collaborator : Toronto Metropolitan University | The Royal Ottawa Mental Health Centre

Deal Size : Inapplicable

Deal Type : Inapplicable

Details : Lemborexant is a Controlled Substance drug candidate, which is currently being evaluated in clinical studies for the treatment of Sleep Initiation and Maintenance Disorders.

Product Name : Undisclosed

Product Type : Controlled Substance

Upfront Cash : Inapplicable

January 16, 2025

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  • Development Update

Details:

Lemborexant is a Controlled Substance drug candidate, which is currently being evaluated in phase II clinical studies for the treatment of Delirium.


Lead Product(s): Lemborexant,Inapplicable

Therapeutic Area: Neurology Brand Name: Undisclosed

Study Phase: Phase IIProduct Type: Controlled Substance

Sponsor: Eisai Inc | Providence Healthcare | St. Paul's Hospital, Vancouver

Deal Size: Inapplicable Upfront Cash: Inapplicable

Deal Type: Inapplicable October 18, 2024

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University of British Columbia

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University of British Columbia

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Lead Product(s) : Lemborexant,Inapplicable

Therapeutic Area : Neurology

Highest Development Status : Phase II

Partner/Sponsor/Collaborator : Eisai Inc | Providence Healthcare | St. Paul's Hospital, Vancouver

Deal Size : Inapplicable

Deal Type : Inapplicable

Details : Lemborexant is a Controlled Substance drug candidate, which is currently being evaluated in phase II clinical studies for the treatment of Delirium.

Product Name : Undisclosed

Product Type : Controlled Substance

Upfront Cash : Inapplicable

October 18, 2024

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Details:

Lemborexant is a Controlled Substance drug candidate, which is currently being evaluated in phase II clinical studies for the treatment of Alzheimer Disease.


Lead Product(s): Lemborexant,Inapplicable

Therapeutic Area: Neurology Brand Name: Undisclosed

Study Phase: Phase IIProduct Type: Controlled Substance

Sponsor: National Institutes of Health | Eisai Inc | National Institute on Aging

Deal Size: Inapplicable Upfront Cash: Inapplicable

Deal Type: Inapplicable February 23, 2024

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Lead Product(s) : Lemborexant,Inapplicable

Therapeutic Area : Neurology

Highest Development Status : Phase II

Partner/Sponsor/Collaborator : National Institutes of Health | Eisai Inc | National Institute on Aging

Deal Size : Inapplicable

Deal Type : Inapplicable

Details : Lemborexant is a Controlled Substance drug candidate, which is currently being evaluated in phase II clinical studies for the treatment of Alzheimer Disease.

Product Name : Undisclosed

Product Type : Controlled Substance

Upfront Cash : Inapplicable

February 23, 2024

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Details:

Lemborexant is a Controlled Substance drug candidate, which is currently being evaluated in phase IV clinical studies for the treatment of Sleep Initiation and Maintenance Disorders.


Lead Product(s): Lemborexant,Inapplicable

Therapeutic Area: Sleep Brand Name: Undisclosed

Study Phase: Phase IVProduct Type: Controlled Substance

Sponsor: Undisclosed

Deal Size: Inapplicable Upfront Cash: Inapplicable

Deal Type: Inapplicable October 23, 2023

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06

CTAD25
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CTAD25
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Lead Product(s) : Lemborexant,Inapplicable

Therapeutic Area : Sleep

Highest Development Status : Phase IV

Partner/Sponsor/Collaborator : Undisclosed

Deal Size : Inapplicable

Deal Type : Inapplicable

Details : Lemborexant is a Controlled Substance drug candidate, which is currently being evaluated in phase IV clinical studies for the treatment of Sleep Initiation and Maintenance Disorders.

Product Name : Undisclosed

Product Type : Controlled Substance

Upfront Cash : Inapplicable

October 23, 2023

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Details:

Lemborexant is a Controlled Substance drug candidate, which is currently being evaluated in phase II clinical studies for the treatment of Alzheimer Disease.


Lead Product(s): Lemborexant,Inapplicable

Therapeutic Area: Neurology Brand Name: Undisclosed

Study Phase: Phase IIProduct Type: Controlled Substance

Sponsor: Brendan Lucey

Deal Size: Inapplicable Upfront Cash: Inapplicable

Deal Type: Inapplicable February 15, 2023

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Eisai Inc

U.S.A
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Eisai Inc

U.S.A
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CTAD25
Not Confirmed

Details : Lemborexant is a Controlled Substance drug candidate, which is currently being evaluated in phase II clinical studies for the treatment of Alzheimer Disease.

Product Name : Undisclosed

Product Type : Controlled Substance

Upfront Cash : Inapplicable

February 15, 2023

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Details:

Lemborexant is a Controlled Substance drug candidate, which is currently being evaluated in phase II clinical studies for the treatment of Sleep Initiation and Maintenance Disorders.


Lead Product(s): Lemborexant,Inapplicable

Therapeutic Area: Sleep Brand Name: Undisclosed

Study Phase: Phase IIProduct Type: Controlled Substance

Sponsor: Undisclosed

Deal Size: Inapplicable Upfront Cash: Inapplicable

Deal Type: Inapplicable October 26, 2022

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Eisai

Japan
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Eisai

Japan
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CTAD25
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Lead Product(s) : Lemborexant,Inapplicable

Therapeutic Area : Sleep

Highest Development Status : Phase II

Partner/Sponsor/Collaborator : Undisclosed

Deal Size : Inapplicable

Deal Type : Inapplicable

Details : Lemborexant is a Controlled Substance drug candidate, which is currently being evaluated in phase II clinical studies for the treatment of Sleep Initiation and Maintenance Disorders.

Product Name : Undisclosed

Product Type : Controlled Substance

Upfront Cash : Inapplicable

October 26, 2022

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Details:

DAYVIGO (Lemborexant), an orexin receptor antagonist, is Eisai’s in-house discovered and developed small molecule that inhibits orexin neurotransmission by binding competitively to the two subtypes of orexin receptors (orexin receptor 1 and 2).


Lead Product(s): Lemborexant,Inapplicable

Therapeutic Area: Sleep Brand Name: Dayvigo

Study Phase: Approved FDFProduct Type: Controlled Substance

Sponsor: Undisclosed

Deal Size: Inapplicable Upfront Cash: Inapplicable

Deal Type: Inapplicable June 02, 2022

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09

Eisai

Japan
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CTAD25
Not Confirmed

Eisai

Japan
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CTAD25
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Details : DAYVIGO (Lemborexant), an orexin receptor antagonist, is Eisai’s in-house discovered and developed small molecule that inhibits orexin neurotransmission by binding competitively to the two subtypes of orexin receptors (orexin receptor 1 and 2).

Product Name : Dayvigo

Product Type : Controlled Substance

Upfront Cash : Inapplicable

June 02, 2022

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Details:

DAYVIGO (lemborexant) is a small-molecule compound, discovered and developed by Eisai in-house scientists, that inhibits orexin signaling by binding competitively to both orexin receptor subtypes (orexin receptor 1 and 2).


Lead Product(s): Lemborexant,Inapplicable

Therapeutic Area: Sleep Brand Name: Dayvigo

Study Phase: Approved FDFProduct Type: Controlled Substance

Sponsor: Undisclosed

Deal Size: Inapplicable Upfront Cash: Inapplicable

Deal Type: Inapplicable June 09, 2021

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10

Eisai

Japan
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CTAD25
Not Confirmed

Eisai

Japan
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CTAD25
Not Confirmed

Details : DAYVIGO (lemborexant) is a small-molecule compound, discovered and developed by Eisai in-house scientists, that inhibits orexin signaling by binding competitively to both orexin receptor subtypes (orexin receptor 1 and 2).

Product Name : Dayvigo

Product Type : Controlled Substance

Upfront Cash : Inapplicable

June 09, 2021

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INTERMEDIATE SUPPLIERS

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Virtual BoothQingmu Pharma: Patients first, FDA/CEP/US-DMF/US-VMF/ASMF APIs for Humans & Vets in 100+ countries.

CAS Number : 1369768-29-5

End Use API : Lemborexant

About The Company : Sichuan Qingmu Pharmaceutical Co., Ltd. is an innovation-driven pharmaceutical company focused on regulated markets. We specialize in the R&D and manufacturing ...

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  • WHO-GMP

Virtual BoothQingmu Pharma: Patients first, FDA/CEP/US-DMF/US-VMF/ASMF APIs for Humans & Vets in 100+ countries.

CAS Number : 412003-95-3

End Use API : Lemborexant

About The Company : Sichuan Qingmu Pharmaceutical Co., Ltd. is an innovation-driven pharmaceutical company focused on regulated markets. We specialize in the R&D and manufacturing ...

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03

  • fda
  • EDQM
  • WHO-GMP

Virtual BoothQingmu Pharma: Patients first, FDA/CEP/US-DMF/US-VMF/ASMF APIs for Humans & Vets in 100+ countries.

CAS Number : 1369767-20-3

End Use API : Lemborexant

About The Company : Sichuan Qingmu Pharmaceutical Co., Ltd. is an innovation-driven pharmaceutical company focused on regulated markets. We specialize in the R&D and manufacturing ...

Company Banner

04

  • fda
  • EDQM
  • WHO-GMP

Virtual BoothQingmu Pharma: Patients first, FDA/CEP/US-DMF/US-VMF/ASMF APIs for Humans & Vets in 100+ countries.

CAS Number : 1450904-92-3

End Use API : Lemborexant

About The Company : Sichuan Qingmu Pharmaceutical Co., Ltd. is an innovation-driven pharmaceutical company focused on regulated markets. We specialize in the R&D and manufacturing ...

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05

CTAD25
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CTAD25
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CAS Number : 412003-95-3

End Use API : Lemborexant

About The Company : Bulat Pharmaceutical is a fast growing pharmaceutical company, founded in the year 2017, Bulat Pharmaceutical is engaged in the manufacturing and sales of high ...

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LinkChem

China
CTAD25
Not Confirmed
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LinkChem

China
CTAD25
Not Confirmed
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CAS Number : 1369768-29-5

End Use API : Lemborexant

About The Company : LinkChem is a leading China headquartered CMO | CRO provider within the pharmaceutical industry. Our core focus includes: custom synthesis, process development,...

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LinkChem

China
CTAD25
Not Confirmed
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LinkChem

China
CTAD25
Not Confirmed
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CAS Number : 412003-95-3

End Use API : Lemborexant

About The Company : LinkChem is a leading China headquartered CMO | CRO provider within the pharmaceutical industry. Our core focus includes: custom synthesis, process development,...

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APIs

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Patents & EXCLUSIVITIES

Check the patents & exclusivity for this product

US Patents

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01

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Cosmoprof India
Not Confirmed

EISAI INC

U.S.A
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Cosmoprof India
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LEMBOREXANT

US Patent Number : 10188652

Drug Substance Claim :

Drug Product Claim : Y

Application Number : 212028

Patent Use Code : U-2791

Delist Requested :

Patent Use Description :

Patent Expiration Date : 2035-10-21

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02

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Cosmoprof India
Not Confirmed

EISAI INC

U.S.A
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Cosmoprof India
Not Confirmed

LEMBOREXANT

US Patent Number : 8268848

Drug Substance Claim : Y

Drug Product Claim : Y

Application Number : 212028

Patent Use Code : U-2791

Delist Requested :

Patent Use Description :

Patent Expiration Date : 2031-09-20

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03

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Cosmoprof India
Not Confirmed

EISAI INC

U.S.A
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Cosmoprof India
Not Confirmed

LEMBOREXANT

US Patent Number : 10702529

Drug Substance Claim :

Drug Product Claim : Y

Application Number : 212028

Patent Use Code :

Delist Requested :

Patent Use Description :

Patent Expiration Date : 2035-10-21

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04

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Cosmoprof India
Not Confirmed

EISAI INC

U.S.A
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Cosmoprof India
Not Confirmed

LEMBOREXANT

US Patent Number : 11026944

Drug Substance Claim :

Drug Product Claim : Y

Application Number : 212028

Patent Use Code :

Delist Requested :

Patent Use Description :

Patent Expiration Date : 2035-10-21

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05

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Cosmoprof India
Not Confirmed

EISAI INC

U.S.A
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Cosmoprof India
Not Confirmed

LEMBOREXANT

US Patent Number : 10702529

Drug Substance Claim :

Drug Product Claim : Y

Application Number : 212028

Patent Use Code :

Delist Requested :

Patent Use Description :

Patent Expiration Date : 2035-10-21

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06

arrow
Cosmoprof India
Not Confirmed

EISAI INC

U.S.A
arrow
Cosmoprof India
Not Confirmed

LEMBOREXANT

US Patent Number : 11026944

Drug Substance Claim :

Drug Product Claim : Y

Application Number : 212028

Patent Use Code :

Delist Requested :

Patent Use Description :

Patent Expiration Date : 2035-10-21

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07

arrow
Cosmoprof India
Not Confirmed

EISAI INC

U.S.A
arrow
Cosmoprof India
Not Confirmed

LEMBOREXANT

US Patent Number : 8268848

Drug Substance Claim : Y

Drug Product Claim : Y

Application Number : 212028

Patent Use Code : U-2791

Delist Requested :

Patent Use Description :

Patent Expiration Date : 2031-09-20

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08

arrow
Cosmoprof India
Not Confirmed

EISAI INC

U.S.A
arrow
Cosmoprof India
Not Confirmed

LEMBOREXANT

US Patent Number : 10188652

Drug Substance Claim :

Drug Product Claim : Y

Application Number : 212028

Patent Use Code : U-2791

Delist Requested :

Patent Use Description :

Patent Expiration Date : 2035-10-21

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US Exclusivities

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01

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Cosmoprof India
Not Confirmed

EISAI INC

U.S.A
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Cosmoprof India
Not Confirmed

LEMBOREXANT

Exclusivity Code : M-293

Exclusivity Expiration Date : 2026-04-20

Application Number : 212028

Product Number : 1

Exclusivity Details :

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02

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Cosmoprof India
Not Confirmed

EISAI INC

U.S.A
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Cosmoprof India
Not Confirmed

LEMBOREXANT

Exclusivity Code : NCE

Exclusivity Expiration Date : 2025-04-07

Application Number : 212028

Product Number : 1

Exclusivity Details :

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03

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Cosmoprof India
Not Confirmed

EISAI INC

U.S.A
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Cosmoprof India
Not Confirmed

LEMBOREXANT

Exclusivity Code : M-293

Exclusivity Expiration Date : 2026-04-20

Application Number : 212028

Product Number : 2

Exclusivity Details :

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04

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Cosmoprof India
Not Confirmed

EISAI INC

U.S.A
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Cosmoprof India
Not Confirmed

LEMBOREXANT

Exclusivity Code : NCE

Exclusivity Expiration Date : 2025-04-07

Application Number : 212028

Product Number : 2

Exclusivity Details :

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ABOUT THIS PAGE

Looking for 1369764-02-2 / Lemborexant API manufacturers, exporters & distributors?

Lemborexant manufacturers, exporters & distributors 1

25

PharmaCompass offers a list of Lemborexant 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 Lemborexant manufacturer or Lemborexant supplier for your needs.

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

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

API | Excipient name

Lemborexant

Synonyms

1369764-02-2, Dayvigo, E-2006, E2006, 0k5743g68x, (1r,2s)-2-[(2,4-dimethylpyrimidin-5-yl)oxymethyl]-2-(3-fluorophenyl)-n-(5-fluoropyridin-2-yl)cyclopropane-1-carboxamide

Cas Number

1369764-02-2

Unique Ingredient Identifier (UNII)

0K5743G68X

About Lemborexant

Lemborexant is a novel dual orexin receptor antagonist used in the treatment of insomnia characterized by difficulties with sleep onset and/or sleep maintenance. Recent research in the field of sleep disorders has revealed that insomnia is likely driven not by the inability of the brain to "switch on" sleep-related circuits, but rather an inability to "switch-off" wake-promoting circuits. Whereas historically popular pharmacologic treatments for insomnia (e.g. [zopiclone], [zolpidem], benzodiazepines) focus on enhancing sleep drive via modulation of GABA and melatonin receptors, lemborexant and other orexin antagonists (e.g. [suvorexant]) act to counteract inappropriate wakefulness. This novel mechanism of action offers potential advantages over classic hypnotic agents, including a more favorable adverse effect profile and potentially greater efficacy, and may signal the beginning of a new wave of treatment options for patients suffering from insomnia.

Lemborexant Manufacturers

A Lemborexant manufacturer is defined as any person or entity involved in the manufacture, preparation, processing, compounding or propagation of Lemborexant, including repackagers and relabelers. The FDA regulates Lemborexant manufacturers to ensure that their products comply with relevant laws and regulations and are safe and effective to use. Lemborexant 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 Lemborexant manufacturers with USDMF, JDMF, KDMF, CEP, GMP, COA and API Price related information on PhamaCompass.

Lemborexant Suppliers

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

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

Lemborexant USDMF

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

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

click here to find a list of Lemborexant suppliers with USDMF on PharmaCompass.

Lemborexant GMP

Lemborexant 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 Lemborexant 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 Lemborexant GMP manufacturer or Lemborexant GMP API supplier for your needs.

Lemborexant CoA

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

Lemborexant CoA mostly includes findings from lab analyses of a specific batch. For each Lemborexant 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.

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