Pitolisant
Structural formula | ||||||||||||||||
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General | ||||||||||||||||
Non-proprietary name | Pitolisant | |||||||||||||||
other names | ||||||||||||||||
Molecular formula | C 17 H 26 ClNO | |||||||||||||||
Brief description |
white solid |
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Drug information | ||||||||||||||||
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Drug class | ||||||||||||||||
Mechanism of action |
Histamine H 3 receptor antagonist |
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properties | ||||||||||||||||
Molar mass | 295.9 g · mol -1 | |||||||||||||||
solubility |
soluble in water |
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As far as possible and customary, SI units are used. Unless otherwise noted, the data given apply to standard conditions . |
Pitolisant is a drug selected from the group of H 3 - antihistamines . It was developed by Walter Schunack and Jean-Charles Schwartz in collaboration with the French pharmaceutical company Bioprojet .
application areas
Pitolisant has been granted orphan drug status for possible use in the treatment of excessive daytime sleepiness (EDS) in narcolepsy . In this indication, it was approved in the EU in March 2016 under the finished drug name Wakix . Further potential areas of application for this drug are currently being tested in phases II and III of clinical research. These include a. the improvement of cognitive abilities in schizophrenia patients, the treatment of excessive daytime sleepiness in sleep apnea syndrome and Parkinson's disease . and photosensitivity in genetic (idiopathic) epilepsies.
Mechanism of action
Pitolisant mediates its effect as an H 3 antihistamine via an inverse agonism at the histamine H 3 receptor . Its affinity for this receptor is in the low nanomolar range.
literature
- Holger Stark: New generations of antihistamines . In: Pharmaceutical newspaper . No. 32, 2011.
- Jean-Charles Schwartz: The histamine H3 receptor: from discovery to clinical trials with pitolisant . In: Br. J. Pharmacol. . 163, No. 4, 2011, pp. 713-721. PMID 21615387 .
Web links
- Public Assessment Report (EPAR) of the European Medicines Agency (EMA) for: Pitolisant
Individual evidence
- ↑ a b c d Tocris: MSDS BF 2649 hydrochloride , accessed December 27, 2019.
- ↑ Study to Demonstrate Cognitive Enhancing Effects of BF2.649 . Retrieved October 11, 2012.
- ↑ BF2.649 in Patients With OSA, Still Complaining of EDS and Refusing to be Treated by CPAP. (HAROSA2) . Retrieved October 11, 2012.
- ↑ BF2.649 in Patients With OSA and Treated by CPAP But Still Complaining of EDS (HAROSA1) . Retrieved October 11, 2012.
- ↑ Efficacy and Safety of BF2.649 in Excessive Daytime Sleepiness (EDS) in Parkinson's Disease (HARPS1) . Retrieved October 11, 2012.
- ↑ Efficacy and Safety of BF2.649 in Excessive Daytime Sleepiness (EDS) in Parkinson's Disease (HARPS2) . Retrieved October 11, 2012.
- ↑ Kasteleijn-Nolst Trenité D, Parain D, Genton P, et al. Efficacy of the histamine 3 receptor (H3R) antagonist pitolisant (formerly known as tiprolisant; BF2.649) in epilepsy: Dose-dependent effects in the human photosensitivity model. Epilepsy Behav 2013; 28: 66-70.
- ↑ Jean-Charles Schwartz: The histamine H3 receptor: from discovery to clinical trials with pitolisant . In: Br. J. Pharmacol. . 163, No. 4, 2011, pp. 713-721. PMID 21615387 .