CNS: A big market for sleep disorders, new domestic orexin drugs enter Phase 3 clinical trials

Insomnia (Insomnia), which is a sleep-wake disorder, is characterized by difficulty falling asleep and/or difficulty maintaining sleep despite adequate sleep opportunities
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It is estimated that about 30% of adults worldwide have symptoms of insomnia, many of which last for months to years

Insomnia (Insomnia), which is a sleep-wake disorder, is characterized by difficulty falling asleep and/or difficulty maintaining sleep despite adequate sleep opportunities

Orexin is a neuropeptide naturally produced by the hypothalamus and mainly acts on the central nervous system
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It has a wide range of effects in regulating food intake, energy metabolism balance, wake-up cycle, blood pressure and so on .

Orexin is a neuropeptide naturally produced by the hypothalamus and mainly acts on the central nervous system

Introduction to YZJ-1139

Introduction to YZJ-1139

YZJ-1139 is a highly effective antagonist of orexin type 1 and type 2 dual receptors (OX1R and OX2R), which can improve sleep by inhibiting orexin receptors, including speeding up sleep and prolonging sleep time
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At the same time, YZJ-1139 has the advantages of fast absorption and moderate half-life, which can achieve rapid onset and low residual effect on the next day.

It is the first orexin receptor antagonist to complete clinical phase II in China

Pharmacy Cloud Data,This product is currently undergoing Phase 3 clinical trials

This product is currently undergoing Phase 3 clinical trials

The primary and secondary endpoints of this clinical trial are: the change in subjective sleep efficiency (sSE) from baseline;

The change in sleep efficiency (SE) monitored by PSG from baseline
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The recent guidelines for the diagnosis and treatment of insomnia in China show that the drugs for the treatment of insomnia at this stage include benzodiazepines, melatonin drugs, orexins, antidepressants and other types
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In terms of pharmacological mechanism, it can improve patients' insomnia symptoms from different perspectives such as calming and hypnotic effects, regulating circadian rhythm, improving anxiety and depression

BZDAs: benzodiazepine receptor agonists; non-BZDs: non-benzodiazepine drugs insomnia treatment flow chart

New drug development area for sleep disorders: Merck’s Suvorexant has dual receptor antagonistic effects on orexin 1 and orexin 2 receptors, and is the first drug in this category to be approved for use; Eisai/Purdue Pharma Dayvigo (lemborexant) was approved in the United States in June 2020; other targets such as Jingxin Pharmaceutical’s EVT-201 Phase 3 clinical trial is in the final stage (EVT201 is a partial positive allosteric modulator of GABAA receptors)
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refer to:

refer to:

NMPA/CDE;

NMPA/CDE;

Yaorong Cloud Data,Cloud Data,FDA/EMA;

FDA/EMA;

Public disclosure by related companies;

Public disclosure by related companies;

Chinese Adult Insomnia Diagnosis and Treatment Guidelines (2017 Edition); Chinese Journal of Neurology, 2018,51(5): 324-335; Sleep Disorder Group, Chinese Medical Association Neurology Branch, Chinese Medical Association Neurology Branch; https://mp .
weixin.
qq.
com / s / jIdmihCta8G8s1UNRnc2Yw; and the like
.

Chinese Adult Insomnia Diagnosis and Treatment Guidelines (2017 Edition); Chinese Journal of Neurology, 2018,51(5): 324-335; Sleep Disorder Group, Chinese Medical Association Neurology Branch, Chinese Medical Association Neurology Branch; https://mp .
weixin.
qq.
com / s / jIdmihCta8G8s1UNRnc2Yw; and the like
.