Pitolisant: First Global Approval
2005/01/01 by Yahiya Y. Syed, Storrs L. Olson · 26 citations
Environmental Science · #Avian ecology and behavior
paper · doi:10.1007/s40265-016-0620-1
Abstract
Pitolisant (Wakix™) is an inverse agonist of the histamine H3 receptor that is being developed by Bioproject. Oral pitolisant is approved in the EU for the treatment of narcolepsy with or without cataplexy in adults. Pitolisant has received a Temporary Authorization of Use in France for this indication in case of treatment failure, intolerance or contraindication to currently available treatment. Pitolisant has orphan drug designation in the EU and the USA. In the pivotal HARMONY I trial, pitolisant significantly decreased excessive daytime sleepiness versus placebo in adults with narcolepsy with or without cataplexy (primary endpoint). Pitolisant also significantly decreased cataplexy rate versus placebo in these patients. This article summarizes the milestones in the development of pitolisant leading to this first approval for narcolepsy.
Cited by
- Pitolisant [wikipedia]
- Histamine H3 Receptor Antagonist Prevents Memory Deficits and Synaptic Plasticity Disruption Following Isoflurane Exposure. [europepmc]
- QSAR Modeling of Histamine H3R Antagonists/inverse Agonists as Future Drugs for Neurodegenerative Diseases. [europepmc]
- Pharmacological Characterization of 5-Substituted 1-[(2,3-dihydro-1-benzofuran-2-yl)methyl]piperazines: Novel Antagonists for the Histamine H 3 and H 4 Receptors with Anti-inflammatory Potential. [europepmc]
- Histamine N -Methyltransferase in the Brain. [europepmc]
- Application of the SwissDrugDesign Online Resources in Virtual Screening. [europepmc]
- Evaluation of the abuse potential of pitolisant, a selective H3-receptor antagonist/inverse agonist, for the treatment of adult patients with narcolepsy with or without cataplexy. [europepmc]
- Computational design of syntheses leading to compound libraries or isotopically labelled targets. [europepmc]
- Exploring occupancy of the histamine H 3 receptor by pitolisant in humans using PET. [europepmc]
- Development of a Conformational Histamine H 3 Receptor Biosensor for the Synchronous Screening of Agonists and Inverse Agonists. [europepmc]
- Perspectives for New and More Efficient Multifunctional Ligands for Alzheimer's Disease Therapy. [europepmc]
- Living with Narcolepsy: Current Management Strategies, Future Prospects, and Overlooked Real-Life Concerns. [europepmc]
- Pitolisant to Treat Excessive Daytime Sleepiness and Cataplexy in Adults with Narcolepsy: Rationale and Clinical Utility. [europepmc]
- Pharmacogenomic Biomarkers and Their Applications in Psychiatry. [europepmc]
- A practical guide to the pharmacological and behavioral therapy of Narcolepsy. [europepmc]
- Analysis of Missense Variants in the Human Histamine Receptor Family Reveals Increased Constitutive Activity of E410 6.30×30 K Variant in the Histamine H 1 Receptor. [europepmc]
- Discovery of Potential, Dual-Active Histamine H 3 Receptor Ligands with Combined Antioxidant Properties. [europepmc]
- Pitolisant in an Adolescent with Prader-Willi Syndrome. [europepmc]
- Pitolisant, a wake-promoting agent devoid of psychostimulant properties: Preclinical comparison with amphetamine, modafinil, and solriamfetol. [europepmc]
- Sleep disturbances in autism spectrum disorder: Animal models, neural mechanisms, and therapeutics. [europepmc]
- Pharmacological interventions for the treatment of obstructive sleep apnea syndrome. [europepmc]
- Histamine H 3 Receptor Isoforms: Insights from Alternative Splicing to Functional Complexity. [europepmc]
- Pharmacological inhibition of histamine N-methyltransferase extends wakefulness and suppresses cataplexy in a mouse model of narcolepsy. [europepmc]
- Exploring the Literature on Narcolepsy: Insights into the Sleep Disorder That Strikes during the Day. [europepmc]
- Evaluation of pitolisant, sodium oxybate, solriamfetol, and modafinil for the management of narcolepsy: a retrospective analysis of the FAERS database. [europepmc]
- Modular synthesis of CF 2 -containing compounds with PhSO 2 CF 2 H reagent through difluoromethylene radical anion synthon strategy. [europepmc]
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