Introduction to the instructions and listing status of lemborexant

1. Name:lemborexant, DAYVIGO, Leborexant, Daweimian

2. Indications:

Lemborexant is indicated for the treatment of adult patients with insomnia, which is characterized by difficulty initiating and/or maintaining sleep.

3. Usage and dosage:

1. Dosage information: The recommended dose of leborexan is 5 mg, taken no more than once per night, before bedtime, with at least 7 hours remaining before the planned awakening time. Based on clinical response and tolerability, the dose may be increased to the maximum recommended dose of 10 mg. If taken with or shortly after a meal, the time it takes to fall asleep may be delayed.

2. Dosage adjustment:

(1) Use concurrently with CYP3A inhibitors or CYP3A inducers:

1) Concomitant use with strong or moderateCYP3A inhibitors: Avoid coadministration of Leborexan with strong or moderate CYP3A inhibitors.

2) Coadministration with weakCYP3A inhibitors: When coadministered with weak CYP3A inhibitors, the maximum recommended dose of leborexan is 5 mg, not to exceed once per night.

3) Coadministration with Strong or Moderate CYP3A Inducers: Avoid coadministration of Leborexant with strong or moderate CYP3A inducers.

(2) Patients with liver function impairment

1) The maximum recommended dose of leborexan in patients with moderate hepatic impairment is 5 mg, not to exceed once per night.

2) Leborexan is not recommended for patients with severe liver damage.

4. Adverse reactions:

In clinical studies of leborexan, common adverse reactions include drowsiness or fatigue(drowsiness, drowsiness, fatigue and slow movement), headache and nightmares or abnormal dreams; less common adverse reactions include sleep paralysis and hypnotic hallucinations.

5. Supply and storage:

Leborexan tablets are available in 5 mg and 10 mg tablets and can be stored at 20°C to 25°C (68°F to 77°F), with a tolerance of 15°C to 30°C (59°F to 86°F).

6. Taboo:

Lebraxen is contraindicated in patients with narcolepsy.

7. Mechanism of action:

The mechanism of action of leborexan in treating insomnia is thought to be through antagonism of orexin receptors. The orexin neuropeptide signaling system plays a role in insomnia. Blocking the binding of the wake-promoting neuropeptides orexinA and orexin B to the receptors OX1R and OX2R is thought to inhibit arousal drive.

8. Overdose:

Clinical experience with leborexan overdose is limited. In clinical pharmacology studies, healthy patients treated with multiple doses of leborexan up to 75 mg (7.5 times the maximum recommended dose) experienced a dose-dependent increase in the frequency of somnolence. There is no specific antidote for leborexan overdose. In the event of an overdose, any standard medical practice for overdose management should be used. When managing overdose, provide supportive care, including close medical supervision and monitoring, and consider the possibility of multiple drugs being involved.

9. Listing situation:

In December 2019, Lebraxant was approved by the U.S. Food and Drug Administration (FDA) to be launched in the United States; in January 2020, Lebraxant was launched in Japan under the trade name DAYVIGO; in June 2021, it was launched in Hong Kong, China, under the trade name Daweimian. Currently, it has not been approved for marketing in the EU or China.

Reference materials:https://www.drugs.com/dayvigo.html