Suvorexant (MK-4305) CAS No. 1030377-33-3

Product Description

Suvorexant (Belsomra®) is the first-in-class dual orexin receptor antagonist approved for insomnia, introduced in the United States in August 2014 and subsequently in Japan. By selectively blocking orexin-1 and orexin-2 receptors, it dampens the orexin-mediated wake-promoting system, thereby facilitating both sleep initiation and maintenance. Across four randomized, placebo-controlled trials that enrolled more than 3,000 adults with primary insomnia, nightly doses of 10–20 mg (5–20 mg in the U.S.; 15–20 mg in Japan) significantly shortened subjective sleep-onset latency, lengthened total sleep time, and improved sleep quality at 1- and 3-month assessments. Objective polysomnography corroborates these benefits, showing dose-related increases in sleep efficiency and reductions in wake after sleep onset. The drug is generally well-tolerated, but somnolence, fatigue, abnormal dreams, and next-day residual drowsiness are common; higher doses also raise concerns about complex sleep behaviors and, rarely, suicidal ideation. Although the FDA initially debated the balance between efficacy and safety—approving 5–20 mg rather than the sponsor-proposed 15–40 mg—suvorexant nonetheless represents a mechanistically novel alternative to benzodiazepines, “Z-drugs,” melatonin receptor agonists, and sedating antidepressants for the short- to medium-term management of insomnia.

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Product Use & Characteristics

1. Identity

• Name: Suvorexant

• Brand: Belsomra®

• Formula: C₂₃H₂₃ClN₆O₂

• MW: 450.9 g/mol

• IUPAC: [(7R)-4-(5-chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl]-[5-methyl-2-(triazol-2-yl)phenyl]methanone

• Class: First-in-class Dual Orexin Receptor Antagonist (DORA)

2. Mechanism

• Targets: Orexin-1 (OX₁R) & Orexin-2 (OX₂R) receptors

• Action: Blocks orexin-A/B → suppresses wakefulness → promotes natural sleep

3. Pharmacokinetics

• Absorption: Oral, Tₘₐₓ ~2 h, 82 % bioavailability

• Half-life: 12 h

• Metabolism: CYP3A4 (major), CYP2C19 (minor)

• Excretion: 66 % feces, 23 % urine

4. Uses

• Primary: Insomnia (sleep onset & maintenance)

• Investigational: Delirium, Alzheimer’s, PTSD, Parkinson’s, stroke-related insomnia

5. Dosing

• Adults: 5–20 mg nightly (US: 5–20 mg; Japan: 15–20 mg)

• Elderly: Start 5 mg; max 15 mg

6. Adverse Effects

• Common: Somnolence, dizziness, headache, abnormal dreams

• Serious: Complex sleep behaviors, suicidal ideation (rare)

7. Contraindications / Interactions

• Avoid: Narcolepsy, severe OSA, strong CYP3A4 inhibitors

• Reduce dose with moderate CYP3A4 inhibitors (e.g., diltiazem)

• Caution: Pregnancy, breastfeeding, depression history

8. Advantages vs. Traditional Hypnotics

• Preserves REM sleep

• Minimal cognitive impairment

• No tolerance/withdrawal

• Lower abuse potential

9. Synthesis Methods

• Route: HTS-derived diazepane amide → metabolic soft-spot elimination → MK-4305 (suvorexant)

10. Market Status

• Approval: FDA (Aug 2014), Japan (Sep 2014)

• Forms: 5, 10, 15, 20 mg tablets

• Usage: ~2/3 of US prescriptions are 10 mg

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