The difference between Leboreson and Suvoreson

Differences in the mechanism of action between Leborexen and Suvorexan

There is a difference between Leborexen and Suvorexan. Leborexen acts on orexin 1 and 2 receptors and has a stronger inhibitory effect on the 2 receptors. By blocking the wake-promoting effect of orexin, it induces physiological sleep. It is a dual inhibitor of orexin receptors OX1 and OX2. Suvorexan promotes sleep by blocking orexin receptors, which can shorten the sleep latency, reduce the time to wake up after falling asleep, and increase the total sleep time. It is a highly selective orexin receptor antagonist. Research shows that Suvorexan can reduce sleep onset and post-sleep awakening latency without disrupting sleep structure. Which drug a patient wants to use needs to be chosen under the guidance of a doctor.

Differences in side effects of Leborexen and Suvorexan

The main side effects of leborexan are drowsiness and fatigue, while the side effects of suvorexan are mainly daytime sleepiness. In addition, complex sleep behaviors, suicidal ideation, sleep paralysis, hallucinations and cataplexy-like symptoms have also been reported, which is dose-dependent.

Therapeutic effects of Leborexan

A 12-month global, multicenter, randomized, double-blind, parallel-group Phase 3 study (NCT02952820), including a 6-month placebo-controlled period (reported here) and a 6-month active treatment-only period (reported separately). A total of 949 participants (age ≥18 years) with insomnia were randomized to receive oral doses of placebo or leborexan (LEM, 5 mg [LEM5] or 10 mg [LEM10]) and analyzed. Sleep onset and sleep maintenance endpoints were analyzed from daily electronic sleep diary data. Treatment-emergent adverse events (TEAEs) were monitored throughout the study.

Results: LEM5 and LEM10 patients reported decreases in (subjective) sleep onset latency and subjective arousal after sleep onset compared to baseline and increases in subjective sleep efficiency compared to placebo. Significant benefit compared with placebo was observed at the end of month 6 and assessed at most time points during the 6-month period, demonstrating long-term sustained efficacy of LEM (LEM).

The proportion of sleep onset responders and sleep maintenance responders was significantly higher in the LEM treatment group compared with placebo. Participants who received LEM reported significantly improved sleep quality after 6 months compared to placebo. Most TEAEs are mild or moderate. The incidence of serious TEAE was low and there were no deaths.

Conclusions: LEM5 and LEM10 had significant benefits compared with placebo on sleep initiation and sleep maintenance in patients with insomnia disorders and were well tolerated.

Leborexen usage and dosage

Leborexan is 5 mg and should be taken at least 7 hours before the planned awakening time and no more than once per night before bedtime. If taken with or shortly after a meal, the time to sleep may be delayed. The dose may be increased based on clinical response and tolerability to the maximum recommended dose of 10 mg.

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References

Kärppä M, Yardley J, Pinner K, Filippov G, Zammit G, Moline M, Perdomo C, Inoue Y, Ishikawa K, Kubota N. Long-term efficacy and tolerability of lemborexant compared with placebo in adults with insomnia disorder: results from the phase 3 randomized clinical trial SUNRISE 2. Sleep. 2020 Sep 14;43(9):zsaa123. doi: 10.1093/sleep/zsaa123. PMID: 32585700; PMCID: PMC7487867.