Pitolisant: First Global Approval

@article{Syed2016PitolisantFG,
  title={Pitolisant: First Global Approval},
  author={Yahiya Y. Syed},
  journal={Drugs},
  year={2016},
  volume={76},
  pages={1313-1318}
}
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… 
The cost utility of pitolisant as narcolepsy treatment
TLDR
The objective in this study was to estimate the cost‐effectiveness of pitoliant as monotherapy, and pitolisant as an adjunctive treatment to modafinil, compared with standard treatment.
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
TLDR
Pitolisant demonstrated significantly lower potential for abuse compared with phentermine and an overall profile similar to placebo; this suggests a low risk of abuse for pitolisant.
Pitolisant to Treat Excessive Daytime Sleepiness and Cataplexy in Adults with Narcolepsy: Rationale and Clinical Utility
TLDR
Randomized and observational studies demonstrate pitolisant to be effective in treating both hypersomnolence and cataplexy while generally being well tolerated at prescribed doses.
Pharmacokinetics of pitolisant in children and adolescents with narcolepsy.
TLDR
After single-dose administration, the exposure parameters of pitolisant were significantly greater in the younger compared with older pediatric patients with narcolepsy.
Pitolisant for treating patients with narcolepsy
TLDR
Clinical studies showed that pitolisant significantly decreased excessive daytime sleepiness and cataplexy rate versus placebo, and was well tolerated, common adverse reactions were headache, insomnia, nausea, and anxiety.
Update on the treatment of narcolepsy: clinical efficacy of pitolisant
TLDR
These four trials show that pitolisant is an effective drug to treat EDS and cataplexy in narcolepsy.
Exploring occupancy of the histamine H3 receptor by pitolisant in humans using PET
TLDR
The objective of the study was to investigate in vivo occupancy of H3 receptors by BF2.649 using PET brain imaging with the H3 receptor antagonist radioligand [11C]GSK189254.
Profile of pitolisant in the management of narcolepsy: design, development, and place in therapy
TLDR
The review confirmed the effectiveness of pitolisant in treating major clinically relevant narcolepsy symptoms, including cataplexy, as compared to placebo and revealed a safe profile when compared with placebo and active comparators.
Histamine H3 receptor antagonists/inverse agonists: Where do they go?
TLDR
The potential role of H3 receptors in the pathophysiology of various central nervous system, metabolic and allergic diseases is discussed, and the current status for H3 receptor antagonists/inverse agonists in ongoing clinical trial studies is reviewed.
Pitolisant, a wake‐promoting agent devoid of psychostimulant properties: Preclinical comparison with amphetamine, modafinil, and solriamfetol
TLDR
Pitolisant is a differentiated therapeutic option, when compared with psychostimulants, for the treatment of EDS, as this agent does not show any amphetamine‐like properties within in vivo preclinical models.
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Pitolisant, a histamine H3 receptor inverse agonist/antagonist is currently under Phase III clinical trials for treatment of excessive daytime sleepiness namely in narcoleptic patients. Its drug
Effects of pitolisant, a histamine H3 inverse agonist, in drug-resistant idiopathic and symptomatic hypersomnia: a chart review.
TLDR
Pitolisant had a long-term favorable benefit/risk ratio in 23-38% of drug-resistant patients with IH and SH, suggesting that histamine neurons can be stimulated in severe idiopathic and symptomatic hypersomnia.
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TLDR
Pitolisant at doses up to 40 mg was efficacious on EDS compared with placebo and well tolerated compared with modafinil, and could offer a new treatment option for patients with narcolepsy.
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TLDR
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TLDR
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