Eisai Launches New Dual Orexin Receptor Antagonist DAYVIGO™ (lemborexant) in the U.S. for Adults with Insomnia

June 04, 2020 News /BioonBIOON/ -- Japanese pharmaceutical company Eisai recently announced the launch of its new insomnia medication, Dayvigo (lemborexant) CIV, in the US market. Available in two strengths (5 mg and 10 mg tablets), the drug is indicated for the treatment of adult insomnia, a sleep-wake disorder characterized by difficulty falling asleep and/or staying asleep despite adequate opportunity for sleep. It is estimated that approximately 30% of adults worldwide experience symptoms of insomnia, many of which persist for months to years.

Dayvigo is a drug discovered and developed internally by EisaiSmall-molecule compounds. In the United States, Dayvigo was approved in December 2019FDAApproved for the treatment of insomnia in adults. In April this year, the U.S. Drug Enforcement Administration (DEA) classified Dayvigo as a Schedule IV controlled substance. According to the definition of Schedule IV, patients with a history of abuse or addiction to alcohol or other drugs may have an increased risk of abuse and addiction to Dayvigo, and such patients should be carefully monitored.

The active pharmaceutical ingredient of Dayvigo is lemborexant, an orexin receptor antagonist that inhibits orexin signaling by competitively binding to orexin receptors (OX1R and OX2R). Orexin is a naturally occurring chemical produced in the hypothalamus and is involved in sleep and wakefulness.

The mechanism of action of lemborexant in the treatment of insomnia is believed to be through antagonism of orexin receptors. The orexin neuropeptide signaling system plays a role in wakefulness. Blocking the binding of the wake-promoting neuropeptides orexin A and orexin B to the orexin receptors OX1R and OX2R is thought to inhibit arousal drive signals. Lemborexant binds to the orexin receptors OX1R and OX2R, acting as a competitive antagonist (with IC50 values of 6.1 nM and 2.6 nM, respectively), and exhibits stronger inhibitory activity against OX2R.

It is estimated that insomnia affects one in three adults. However, because safety is a major concern with sleep medications, new therapies face a difficult path to gaining acceptance among physicians and patients. Earlier this year,FDABlack box warnings were issued for a class of insomnia medications, including Lunesta, Sonata, and Ambien, due to reports of injuries and fatalities resulting from hazardous activities such as sleepwalking and sleep-driving in patients taking these drugs.

Significant Unmet Medical Needs Remain in the Treatment of Insomnia Due to Efficacy and Safety ConcernsDayvigo is a medication that addresses both sleep onset and sleep maintenance issues. Its mechanism of action does not impair morning postural stability or cognitive function.The launch of Dayvigo will provide an important new treatment option for patients with insomnia.

Molecular structure of lemborexant (Image source: Wikipedia)

Dayvigo Receives U.S.FDAApproved, based on data from the clinical development program of lemborexant for insomnia, which included two pivotal Phase III clinical studies: SUNRISE-1 (Study 304) and SUNRISE-2 (Study 303), enrolling approximately 2,000 patients. The SUNRISE-1 study was conducted in 1,006 patients aged ≥55 years (45% of whom were aged ≥65 years) with difficulty initiating sleep, evaluating the efficacy and safety of lemborexant compared to placebo and the active control drug zolpidem tartrate extended-release. The data showed that the study met its primary and secondary endpoints, and the most commonly reported adverse events in the lemborexant treatment group were headache and somnolence. The SUNRISE-2 study was conducted in 949 adult patients (aged 18–88 years) with insomnia, evaluating the efficacy and safety of lemborexant compared to placebo. The data showed that this study also met its primary and key secondary endpoints. The most commonly reported adverse events in the lemborexant treatment group were somnolence, nasopharyngitis, headache, and influenza.

In addition to these pivotal trials, Eisai conducted several studies to further evaluate the safety of Dayvigo, including assessments of the impact of lemborexant on auditory arousal capacity, next-day postural stability and memory, and next-morning driving performance. The data showed that although there was no significant difference between lemborexant and placebo in terms of auditory arousal capacity, lemborexant was associated with dose-dependent impairments in attention and memory compared with placebo. Furthermore, no significant differences were observed between lemborexant and placebo regarding next-day postural stability or memory. Although neither the 5 mg nor the 10 mg dose of lemborexant caused statistically significant impairment in next-morning driving performance in adult or elderly subjects compared with placebo, driving performance was impaired in some subjects receiving the 10 mg dose of lemborexant. (Bioon.com)

Original Source: EISAI LAUNCHES NEW INSOMNIA DRUG DAYVIGO™ (LEMBOREXANT) CIV IN THE UNITED STATES AS A TREATMENT OPTION FOR ADULTS WITH INSOMNIA