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BF2.649 (pitolisant)
Pitolisant is a selective histamine H3 receptor antagonist that increases histamine release in the brain to promote wakefulness.
Pitolisant is a selective histamine H3 receptor antagonist that increases histamine release in the brain to promote wakefulness. Used for Narcolepsy type 1 and type 2, Idiopathic hypersomnia.
At a glance
| Generic name | BF2.649 (pitolisant) |
|---|---|
| Also known as | Pitolisant |
| Sponsor | Bioprojet |
| Drug class | Histamine H3 receptor antagonist |
| Target | H3 receptor |
| Modality | Small molecule |
| Therapeutic area | Neurology |
| Phase | Phase 3 |
Mechanism of action
By blocking H3 autoreceptors on histaminergic neurons in the hypothalamus, pitolisant removes negative feedback inhibition and enhances histamine neurotransmission. This increased histaminergic signaling promotes arousal and wakefulness, making it effective for narcolepsy and other hypersomnias. The drug crosses the blood-brain barrier and acts centrally without significant peripheral effects.
Approved indications
- Narcolepsy type 1 and type 2
- Idiopathic hypersomnia
Common side effects
- Insomnia
- Headache
- Anxiety
- Nausea
- Irritability
Key clinical trials
- Proof of Concept Study on Pitolisant Effect on Autism Spectrum Disorders in Children and Adolescents (PHASE2)
- Efficacy and Safety of Pitolisant in Pediatric Narcoleptic Patients With or Without Cataplexy, Double-blind Study Followed by a Prolonged Open-label Period (PHASE3)
- Pitolisant (BF2.649) in the Treatment of EDS in Patients With OSA (PHASE3)
- Study to Demonstrate Cognitive Enhancing Effects of BF2.649 (PHASE2)
- Pitolisant (BF2.649) in the Treatment of Excessive Daytime Sleepiness in Patients With Obstructive Sleep Apnoea Syndrome, Treated or Not by Nasal Continuous Positive Airway Pressure, But Still Complaining of Excessive Daytime Sleepiness (PHASE3)
- Determination the Abuse Potential of Pitolisant in Healthy, Non-Dependent Recreational Stimulant Users (PHASE1)
- Effects of BF2.649 in the Treatment of Excessive Daytime Sleepiness in Narcolepsy. (PHASE3)
- Long Term Open Label Study in Narcolepsy With BF2.649 (Pitolisant) (PHASE3)
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- BF2.649 (pitolisant) CI brief — competitive landscape report
- BF2.649 (pitolisant) updates RSS · CI watch RSS
- Bioprojet portfolio CI