New medicine for insomnia! Dayvigo (lemborexant), a dual effect orexin receptor antagonist of Weicai, has been approved by the US FDA!

December 23, 2019 / BIOON / -- Japanese pharmaceutical company Eisai recently announced that the U.S Food and Drug Administration (FDA) has approved dayvigo (lemborexant), an orexin receptor antagonist found and developed in the interior of Eisai, which is used to treat adult insomnia, a sleep wake disorder characterized by difficulties in sleeping and / or maintaining sleep According to the plan of the United States regulatory (special) Drug Administration (DEA), dayvigo will be available in 5mg and 10mg tablets in the next three months It is estimated that insomnia affects one third of adults But because safety is a big problem of sleep drugs, the new therapy faces a difficult process in obtaining the approval of doctors and patients Earlier this year, the FDA issued a black box warning on a number of insomnia drugs, including lunesta, Sonata and Ambien, due to reports that dangerous activities such as sleepwalking and sleep driving among patients taking the drugs resulted in casualties Dayvigo suppresses orexin signals by competitively binding orexin receptors (ox1r and ox2r) Orexin is a chemical produced naturally in the hypothalamus, which is involved in sleep and arousal "There are still significant unmet medical needs in the treatment of insomnia due to efficacy and safety issues," said Tushar Patel, global head of wakefulness disorders at Weicai neuro business group Dayvigo is a product that can solve both sleeping problems and sleep maintenance problems Its mechanism of action will not damage the posture stability and cognitive ability in the morning " The mechanism of lemborexant in the treatment of insomnia is believed to be through the antagonism of orexin receptor The orexin neuropeptide signaling system plays a role in arousal Blocking arousal promotes the binding of orexin A and orexin B to orexin receptor ox1r and ox2r, which is believed to inhibit the arousal driving signal Lamborexant can bind orexin receptors ox1r and ox2r As a competitive antagonist, it has a stronger inhibitory effect on ox2r This approval was based on data from the clinical development program to evaluate the efficacy of lemborexant in the treatment of insomnia, including two key phase III clinical studies, sunrise-1 (study 304) and sunrise-2 (study 303), involving about 2000 patients The sunrise-1 study was conducted in 1006 patients aged ≥ 55 years (45% of patients aged ≥ 65 years) who had difficulty sleeping at night The efficacy and safety of lamborexant compared with placebo and the positive control drug zolpidem tartrate were evaluated The data showed that the study reached the primary and secondary end points The most common adverse event reported by the lamborexant treatment group was headache And lethargy The sunrise-2 study, conducted in 949 adults (18-88 years old) with insomnia, evaluated the efficacy and safety of lamborexant compared with placebo The data showed that the study also reached the primary and secondary endpoints The most common adverse events reported in the lamborexant treatment group were drowsiness, nasopharyngitis, headache and influenza In addition to these key tests, Weicai has conducted a number of studies to further assess the safety of dayvigo, including the effects of lemborexant on voice wake-up ability, posture stability or memory on the next day, and driving performance on the next morning The data showed that although there was no significant difference between lamborexant and placebo in the ability to wake up the voice, there was a dose-dependent deterioration of lamborexant compared with placebo in terms of attention and memory In addition, there was no significant difference between lamborexant and placebo in postural stability or memory on the second day Although 5mg and 10mg of lamborexant did not cause statistically significant damage to driving performance in adults or elderly subjects the next morning (compared to placebo), driving performance was impaired in some subjects taking 10mg of lamborexant Lamborexant molecular structure formula (picture source: Wikipedia) lamborexant is a dual inhibitor of orexin receptor OX1 and ox2, which was discovered and developed by Weicai The compound suppresses orexin by competitively binding orexin receptor (orexin receptor 1 and receptor 2) of 2-bell subtype In individuals with insomnia, the orexin system that regulates sleep and wakefulness may not function properly In the normal sleep cycle, the activity of orexin system is inhibited, which reveals that it may interfere orexin neurotransmission through lemborexant, and promote the initiation and maintenance of sleep purposefully Orexin signals are associated with other physiological functions, such as memory, mood, motivation, and attention Therefore, in addition to the awakening rhythm disorder (iswrd), Weicai is also testing the application of lemborexant in Alzheimer's disease (AD) Previously, the drug was jointly developed by Weicai and Purdue, but earlier this year, Weicai repurchased all rights to the drug Original source: U.S FDA approvals Eisai's dayvigo Gamma (LEMBOREXANT) FOR TREATMENT OF INSOMNIA IN ADULT PATIENTS