Pitolisant

Structural formula
General
Non-proprietary name	Pitolisant
other names	1- (3- (3- (4-chlorophenyl) propoxy) propyl) piperidine ( IUPAC ) ; Tiprolisant ( USAN ) ; BF 2649;
Molecular formula	C 17 H 26 ClNO
Brief description	white solid
External identifiers / databases
PubChem	9948102
ChemSpider	8123714
DrugBank	DB11642
Wikidata	Q426044
Drug information
ATC code	N07 XX11
Drug class	Antihistamine
Mechanism of action	Histamine H 3 receptor antagonist
properties
Molar mass	295.9 g · mol -1
solubility	soluble in water
safety instructions
	Please note the exemption from the labeling requirement for drugs, medical devices, cosmetics, food and animal feed
GHS labeling of hazardous substances Hydrochloride	no GHS pictograms
	no GHS pictograms
H and P phrases	H: no H-phrases
	P: no P-phrases
	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 .

[tocris-1] Tocris: MSDS BF 2649 hydrochloride , accessed December 27, 2019.

[2] Study to Demonstrate Cognitive Enhancing Effects of BF2.649 . Retrieved October 11, 2012.

[3] BF2.649 in Patients With OSA, Still Complaining of EDS and Refusing to be Treated by CPAP. (HAROSA2) . Retrieved October 11, 2012.

[4] BF2.649 in Patients With OSA and Treated by CPAP But Still Complaining of EDS (HAROSA1) . Retrieved October 11, 2012.

[5] Efficacy and Safety of BF2.649 in Excessive Daytime Sleepiness (EDS) in Parkinson's Disease (HARPS1) . Retrieved October 11, 2012.

[6] Efficacy and Safety of BF2.649 in Excessive Daytime Sleepiness (EDS) in Parkinson's Disease (HARPS2) . Retrieved October 11, 2012.

[7] 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.

[8] 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 .