Modafinil

E2086 Showed Potential to Improve Wakefulness in People Living with Narcolepsy Type 1 TOKYO, Sept. 8, 2025 /PRNewswire/ -- Eisai Co., Ltd. (Headquarters: Tokyo, CEO: Haruo Naito, "Eisai") announced today that the results from a Phase Ib clinical trial (NCT06462404) of its in-house developed novel selective orexin 2 receptor agonist E2086 have been presented at the World Sleep 2025 congress, held in Singapore from September 5 to 10. These data demonstrate that once-daily dosing of E2086 has the potential to improve daytime wakefulness in individuals with narcolepsy type 1 (NT1). Continue Reading Clinical Trial Design This randomized, double-blind, single-dose, multiple crossover, Phase Ib clinical trial was conducted in the United States and Canada to evaluate the efficacy, safety, and tolerability of E2086 in people meeting criteria for NT1, compared with placebo and an existing treatment (modafinil). There were a total of 21 patients in the clinical trial (21 patients received the study medication, 19 patients completed the trial). Participants received a single dose of one of five treatments (E2086 5 mg, 10 mg, 25 mg, placebo, or modafinil) shortly after waking, efficacy assessments were conducted for each treatment. Efficacy was assessed using the objective Maintenance of Wakefulness Test (MWT)*1 to evaluate excessive daytime sleepiness (EDS), and subjective sleepiness was measured using the Karolinska Sleepiness Scale (KSS)*2 at the end of each MWT session. Clinical Trial Results As evaluated by MWT, all doses of E2086 demonstrated statistically significant longer sleep latencies*3 – a measure of the ability to stay awake – compared with placebo (P<0.0001 for all doses) and modafinil (E2086 5 mg: P=0.0009; E2086 10 mg and 25 mg: P<0.0001) (See the figure below). For the KSS, all doses of E2086 showed statistically significant higher alertness compared with placebo (P<0.0001), while E2086 10 mg and 25 mg demonstrated statistically significantly higher alertness compared with modafinil (P<0.0001). These outcomes confirmed the Proof of Mechanism for E2086. Treatment-emergent adverse events (TEAEs), based on the 21 patients who received the study medication in the clinical trial, exhibited a dose-dependent trend. The four most frequently observed TEAEs with E2086 included increased urinary frequency (E2086 5 mg: 14.3%, 10 mg: 23.8%, 25 mg: 52.4%), nausea (14.3%, 19.0%, 47.6%), dizziness (4.8%, 23.8%, 38.1%), and urinary urgency (9.5%, 19.0%, 38.1%). No participants discontinued due to TEAEs, and most TEAEs were mild to moderate in severity. No serious TEAEs were reported. Katsutoshi Ido, Ph.D., Chief Scientific Officer at Eisai, commented: "At World Sleep 2025, we presented data supporting the potential of E2086 to improve daytime wakefulness in people diagnosed with narcolepsy type 1. Narcolepsy is a condition with high unmet medical needs, characterized not only by excessive daytime sleepiness but also by symptoms such as cataplexy, hypnagogic/hynopompic hallucinations, and sleep paralysis, all of which significantly impair the quality of life of those affected. The efficacy and safety findings from this trial warrant further investigation in the narcolepsy patient population." Orexin is a neurotransmitter that plays a central role in regulating sleep and wakefulness. Inhibiting orexinergic neurons is believed to promote a natural transition from wakefulness to sleep. Conversely, activating orexinergic neurons is believed to help maintain a more stable state of wakefulness. From the perspective of inhibiting orexinergic neuron activity, Eisai has developed the insomnia treatment DAYVIGO ® (generic name: lemborexant) an orexin receptor antagonist that is available in more than 25 countries worldwide. Furthermore, leveraging the orexin platform established through the development of DAYVIGO, Eisai has created E2086, an orexin receptor agonist that activates orexinergic neurons. In addition to DAYVIGO, Eisai aims to contribute to people living with sleep disorders through the development of E2086. *1 Maintenance of Wakefulness Test (MWT): An objective test that evaluates the ability to stay awake in a sleep-conducive environment. The test is conducted in a quiet examination room with the lights turned off, consisting of four 40-minute sessions carried out at two-hour intervals throughout the day, during which the time taken to fall asleep (sleep latency) is measured using electroencephalography. *2 Karolinska Sleepiness Scale (KSS): A simple subjective scale used to assess the current intensity of sleepiness on a 9-point scale, ranging from "1 - Very clearly awake" to "9 - Very sleepy, struggling against sleepiness". *3 Sleep latency: The amount of time it takes to fall asleep. MEDIA CONTACTS: Eisai Co., Ltd. Public Relations Department, TEL: +81-(0)3-3817-5120 Eisai Europe, Ltd. EMEA Communications Department + 44 (0) 797 487 9419 Eisai Inc. (U.S.) Libby Holman + 1-201-753-1945 [Notes to editors] 1. About E2086 E2086 is Eisai's in house discovered novel selective orexin 2 receptor agonist. Nonclinical studies have demonstrated statistically significant increases in time spent awake and significant reductions in rates of cataplexy. Individuals with a deficiency of orexin demonstrate excessive daytime sleepiness (EDS), as exemplified by patients with narcolepsy Type 1, demonstrate a loss of orexinergic neurons, and low cerebrospinal fluid (CSF) orexin levels. E2086 has the potential to improve patients' symptoms by enhancing orexin receptor activity. 2. About narcolepsy Narcolepsy is a chronic sleep disorder that is characterized by EDS. Narcolepsy is classified into two subtypes, type 1 (narcolepsy with cataplexy) and type 2 (narcolepsy without cataplexy). Due to problems with fatigue, cognition, and persistence of residual symptoms despite treatment, disease burden for narcolepsy is high.1 References 1. Maski. K, et.al. Listening to the Patient Voice in Narcolepsy: Diagnostic Delay, Disease Burden, and Treatment Efficacy. J. Clinical Sleep Medicine. 2017, 13 (3) p419-, SOURCE Eisai Inc. WANT YOUR COMPANY'S NEWS FEATURED ON PRNEWSWIRE.COM? 440k+ Newsrooms & Influencers 9k+ Digital Media Outlets 270k+ Journalists Opted In GET STARTED

Drug developers from around the world rang in a new era of sleep medicine Monday, as data from a series of clinical trials show narcolepsy can be effectively treated by amplifying a specific brain protein.That protein, called orexin-2, helps regulate important body functions like appetite, arousal and wakefulness, which has in turn made it a promising target for drug companies. Johnson & Johnson, for instance, hopes that by blocking orexin-2, its experimental medicine seltorexant can be used to combat insomnia in patients with major depression.More commonly, though, developers are looking to boost this protein to keep people with narcolepsy awake longer. The furthest along in this pursuit is Takeda Pharmaceutical with its drug oveporexton, which recently met the main and secondary goals of two late-stage clinical trials that focused on the most common, Type 1 form of narcolepsy.On Monday, at a medical conference focused on sleep therapies, Takeda presented more detailed results from these studies. In each, researchers evaluated whether oveporexton was any better than a placebo at keeping participants awake by using what Sarah Sheikh, Takedas head of global development, describes as the most boring test of all time.This Maintenance of Wakefulness Test places participants in a dark, quiet, peaceful room and measures how long it takes them to fall asleep. The exam has several rounds, with each lasting roughly 40 minutes. According to Takeda, at the start of its studies, most participants were asleep within five minutes. But 12 weeks in, those who were taking 2 mg doses of oveporexton twice daily were staying awake about 20 minutes to 25 minutes a clinically meaningful improvement.One hallmark of Type 1 narcolepsy is a loss of muscle control known as cataplexy. Takeda additionally said the median weekly rates of cataplexy decreased more than 80% for oveporexton-treated patients during its studies. The median number of days per week that patients experienced no cataplexy had also grown, from 0 to between 4 and 5.This is the first time any drug in this field has ever shown this magnitude of effect, Sheikh said in an interview ahead of the presentation.Takeda highlighted other findings as well, like that drug-treated patients reported significant improvements in their quality of life. Oveporexton was generally well tolerated, too, as researchers did not observe serious adverse events related to treatment. There were no liver toxicity issues, nor were there any signs of patients experiencing visual disturbances a potential safety concern with orexin drugs that analysts have homed in on.The most common adverse events, Takeda said, were insomnia and frequent urination, and a majority were transient.With these results in hand, the company plans to submit its drug for approval by the end of March. Jefferies analyst Stephen Barker wrote in a note to clients how the fresh data make his team increasingly confident oveporexton will dominate a market that Takeda estimates having as many as 120,000 patients in the U.S. alone.Takeda is currently well ahead of its closest competitor, and its drug, if ultimately approved, could achieve annual sales of $1 billion, according to Barker.While Takeda may have the lead, companies like Alkermes, Eisai and Centessa Pharmaceuticals are working to make up ground.At the medical conference, Alkermes gave a more in-depth look into a mid-stage study where three different doses of its once-daily drug alixorexton each beat a placebo on that Maintenance of Wakefulness Test. After six weeks, the drug-treated groups were able to stay awake for 24 to 28 minutes and were showing meaningful improvements on sleepiness and cataplexy, Alkermes said. And, as with Takedas studies, most treatment-emergent adverse events were mild or moderate.The most common adverse events were frequent or abnormal urination, insomia, excessive saliva secretion and blurred vision, though Alkermes noted how there were no clinically meaningful changes in vital signs, eye exams, or liver or kidney function.Overall, the data was good and about as expected, wrote Marc Goodman, an analyst at Leerink Partners. Goodman added that the once-daily and flexible dosing of alixorexton should be an advantage for Alkermes, as the #2 player.Eisai also presented data from an early-stage study with 21 participants, who either received a placebo, an existing medication known as modafinil, or one of three doses of the companys drug E2086. Eisai said all doses appeared to keep patients awake significantly longer in that wakefulness test. The most common treatment-emergent adverse events were dizziness, nausea, and frequent or urgent urination. None were classified as serious.Katsutoshi Ido, Eisais chief scientific officer, said in a satement the results warrant further investigation of E2086 as a potential treatment for narcolepsy.Takedas stock price had slipped 1% in U.S. trading by Monday afternoon. Eisai shares, meanwhile, rose nearly 4% on the Tokyo stock exchange, while Alkermes were down more than 6% on the Nasdaq.The Food and Drug Administration has approved a few orexin-blocking agents for insomnia. They include Merck & Co.s Belsomra, Idorsias Quviviq and Eisais Dayvigo. '