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ACT-129968
ACT-129968 is a selective orexin 2 receptor antagonist that promotes sleep by blocking wake-promoting signals in the brain.
ACT-129968 is a selective orexin 2 receptor antagonist that promotes sleep by blocking wake-promoting signals in the brain. Used for Insomnia disorder.
At a glance
| Generic name | ACT-129968 |
|---|---|
| Also known as | Setipiprant |
| Sponsor | Idorsia Pharmaceuticals Ltd. |
| Drug class | Orexin 2 receptor antagonist |
| Target | OX2R (Orexin 2 receptor) |
| Modality | Small molecule |
| Therapeutic area | Neurology / Sleep Medicine |
| Phase | Phase 3 |
Mechanism of action
The drug selectively antagonizes the orexin 2 receptor, which is involved in regulating the sleep-wake cycle. By blocking orexin signaling, ACT-129968 reduces wakefulness and facilitates sleep onset and maintenance. This mechanism is distinct from traditional sedative-hypnotics and targets the underlying neurobiological drivers of insomnia.
Approved indications
- Insomnia disorder
Common side effects
- Somnolence
- Headache
- Dizziness
- Fatigue
Key clinical trials
- Study of ACT-129968 in Adult Patients With Seasonal Allergic Rhinitis (PHASE2)
- Efficacy, Safety, and Tolerability Study of ACT-129968 in Patients With Seasonal Allergic Rhinitis (PHASE3)
- A Study to Assess the Tolerability, Safety, Pharmacodynamics, and Pharmacokinetics of Ascending Single Doses (Including Food Interaction) and Ascending Multiple Doses of ACT-453859, and Multiple Doses of Setipiprant (ACT-129968) (PHASE1)
- Clinical Study to Assess the Pharmacokinetics, Safety, and Tolerability of ACT-129968 in Healthy Subjects (PHASE1)
- Clinical Study to Explore the Efficacy of ACT-129968 in Patients With Partly Controlled Asthma (PHASE2)
Primary sources
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| Source | Used for |
|---|---|
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |