Lemborexant

Generic Name: Lemborexant

Brand Names: Dayvigo

Drug Type: Small Molecule

Chemical Formula: C_₂₂H_₂₀F_₂N_₄O_₂

CAS Number: 1369764-02-2

Unique Ingredient Identifier: 0K5743G68X

Background: 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.

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

Associated Conditions: Insomnia

Clinical Trials

Study to Evaluate the Pharmacokinetics of Lemborexant (E2006) and Its Metabolites in Subjects With Mild and Moderate Hepatic Impairment Compared to Healthy Subjects

Phase 1

Completed

Conditions: Hepatic Impairment

Interventions: Drug: Lemborexant

First Posted Date: 2018-02-22

Last Posted Date: 2020-03-20

Lead Sponsor: Eisai Inc.

Target Recruit Count: 24

Registration Number: NCT03440424

Locations: 🇺🇸
Orlando Clinical Research Center, Orlando, Florida, United States
🇺🇸
Clinical Pharmacology of Miami, LLC, Miami, Florida, United States

Study to Evaluate the Pharmacokinetics of Lemborexant (E2006) and Its Metabolites in Subjects With Normal Renal Function or With Severe Renal Impairment

Phase 1

Completed

Conditions: Renal Impairment

Interventions: Drug: Lemborexant

First Posted Date: 2018-02-22

Last Posted Date: 2020-03-12

Lead Sponsor: Eisai Inc.

Target Recruit Count: 16

Registration Number: NCT03443063

Locations: 🇺🇸
Clinical Pharmacology of Miami, LLC, Miami, Florida, United States
🇺🇸
Orlando Clinical Research Center, Orlando, Florida, United States

A Study to Determine the Abuse Potential of Single Oral Doses of Lemborexant Compared to Zolpidem, Suvorexant and Placebo in Healthy, Non-Dependent, Recreational Sedative Users

Phase 1

Completed

Conditions: Insomnia Disorders

Interventions: Drug: Zolpidem tablets
Drug: Suvorexant tablets, over-encapsulated
Drug: Lemborexant tablets
Drug: Placebo lemborexant
Drug: Placebo zolpidem
Drug: Placebo suvorexant

First Posted Date: 2017-05-17

Last Posted Date: 2020-06-29

Lead Sponsor: Eisai Inc.

Target Recruit Count: 39

Registration Number: NCT03158025

Locations: 🇨🇦
INC Research Toronto, Inc., Toronto, Canada

Crossover Study to Evaluate the Effect of Lemborexant Versus Placebo and Zolpidem on Postural Stability, Auditory Awakening Threshold, and Cognitive Performance in Healthy Subjects 55 Years and Older

Phase 1

Completed

Conditions: Healthy Subjects

Interventions: Drug: LEM5
Drug: LEM10
Drug: ZOL
Drug: PBO

First Posted Date: 2017-01-02

Last Posted Date: 2019-08-01

Lead Sponsor: Eisai Inc.

Target Recruit Count: 60

Registration Number: NCT03008447

Locations: 🇺🇸
Clinilabs, Inc, New York, New York, United States
🇺🇸
NeuroTrials Research, Inc, Atlanta, Georgia, United States
🇺🇸
Wake Research Assoicates, LLC, Raleigh, North Carolina, United States

and more 1 locations

Study of Lemborexant for Irregular Sleep-Wake Rhythm Disorder and Mild to Moderate Alzheimer's Disease Dementia

Phase 2

Completed

Conditions: Irregular Sleep-Wake Rhythm Disorder

Interventions: Drug: Lemborexant 2.5 mg
Drug: Lemborexant 10 mg
Drug: Lemborexant 5 mg
Drug: Lemborexant 15 mg
Drug: Lemborexant-matched placebo

First Posted Date: 2016-12-23

Last Posted Date: 2021-05-17

Lead Sponsor: Eisai Inc.

Target Recruit Count: 63

Registration Number: NCT03001557

Locations: 🇺🇸
Facility #1, Columbia, South Carolina, United States
🇺🇸
Nevada Senior Services (NSS) Adult Day Care Center, Henderson, Nevada, United States
🇯🇵
Eisai Trial Site #1, Tachikawa-shi, Tokyo, Japan

and more 4 locations

Long-term Study of Lemborexant in Insomnia Disorder (SUNRISE 2)

Phase 3

Completed

Conditions: Insomnia Disorder

Interventions: Drug: lemborexant
Drug: Placebo

First Posted Date: 2016-11-02

Last Posted Date: 2020-02-06

Lead Sponsor: Eisai Inc.

Target Recruit Count: 971

Registration Number: NCT02952820

Locations: 🇵🇱
Facility # 2, Warszawa, Poland
🇯🇵
Eisai Trial Site 3, Yokohama, Kanagawa, Japan
🇯🇵
Eisai Trial Site 2, Yokohama, Kanagawa, Japan

and more 8 locations

Study of the Efficacy and Safety of Lemborexant in Subjects 55 Years and Older With Insomnia Disorder (SUNRISE 1)

Phase 3

Completed

Conditions: Insomnia

Interventions: Drug: Lemborexant
Drug: Lemborexant-matched placebo
Drug: Zolpidem-matched placebo
Drug: Zolpidem tartrate

First Posted Date: 2016-05-26

Last Posted Date: 2024-11-12

Lead Sponsor: Eisai Inc.

Target Recruit Count: 1006

Registration Number: NCT02783729

Locations: 🇺🇸
Saint Francis Sleep Allergy and Lung Institute, Clearwater, Florida, United States
🇨🇦
Toronto Sleep Institute, Toronto, Ontario, Canada
🇺🇸
University of Pennsylvania, Philadelphia, Pennsylvania, United States

and more 92 locations