Traditional

Structural formula
General
Non-proprietary name	Traditional
other names	LY686017; VLY-686; {2- [1 - {[3,5-bis (trifluoromethyl) phenyl] methyl} -5- (4-pyridinyl) -1 H -1,2,3-triazol-4-yl] -3-pyridinyl} ( 2-chlorophenyl) methanone;
Molecular formula	C 28 H 16 ClF 6 N 5 O
External identifiers / databases
PubChem	9916461
ChemSpider	8092108
DrugBank	DB12580
Wikidata	Q1798493
Drug information
Mechanism of action	NK 1 - antagonist
properties
Molar mass	587.9 g · mol -1
safety instructions
GHS hazard labeling ; no classification available
GHS hazard labeling ; no classification available
	As far as possible and customary, SI units are used. Unless otherwise noted, the data given apply to standard conditions .

Tradipitant is a potential drug in clinical development . It was initially clinically tested by the US pharmaceutical company Eli Lilly and Company for the treatment of addiction to alcohol withdrawal . In 2012, Vanda Pharmaceuticals Inc. acquired a license from Eli Lilly for development in other areas of application, such as the relief of chronic itching (pruritus).

Mechanism of action

People who suffer from alcohol addiction have elevated levels of stress-inducing neurotransmitters . Tradipitant inhibits the stress-inducing effect of substance P in the central nervous system (CNS) by blocking the neurokinin -1 receptor .

At a daily dose of 50 mg, tradipitant blocks over 90% of the neurokinin-1 receptors in the CNS.

literature

David T. George, Jodi Gilman, Jacqueline Hersh, Annika Thorsell, David Herion, Christopher Geyer, Xiaomei Peng, William Kielbasa, Robert Rawlings, John E. Brandt, Donald R. Gehlert, Johannes T. Tauscher, Stephen P. Hunt, Daniel Hommer, Markus Heilig: Neurokinin 1 Receptor Antagonism as a Possible Therapy for Alcoholism . In: Science . 319, No. 5869, March 2008, pp. 1536-1539. doi : 10.1126 / science.1153813 . PMID 18276852 .
David T. George, Jodi Gilman, Annika Thorsell, Donald R. Gehlert, Johannes T. Tauscher, Stephen P. Hunt, Daniel Hommer, Markus Heilig: Neurokinin 1 (NK1) receptor blockade: a novel anti-stress based mechanism for treatment of alcoholism . In: Alcoholism: Clinical and Experimental Research . 32, No. s1, June 2008, p. 342A. doi : 10.1111 / j.1530-0277.2008.00684.x-i1 .
Greg Miller: Tackling Alcoholism With Drugs . In: Science . 320, No. 5873, April 2008, pp. 168-170. doi : 10.1126 / science.320.5873.168 .

Individual evidence

↑ This substance has either not yet been classified with regard to its hazardousness or a reliable and citable source has not yet been found.
↑ Clinical study (phase II): Effect of LY686017 on Alcohol Craving at Clinicaltrials.gov of the NIH .
^ Vanda Pharma acquires world-wide license from Eli Lilly to develop & commercialize NK-1 receptor antagonist .
↑ Vanda Pharmaceuticals Announces Tradipitant Phase II Proof of Concept Study Results for Chronic Pruritus in Atopic Dermatitis , PM Vanda Pharmaceuticals, March 4, 2015, accessed May 4, 2015.

[NV-1] This substance has either not yet been classified with regard to its hazardousness or a reliable and citable source has not yet been found.

[2] Clinical study (phase II): Effect of LY686017 on Alcohol Craving at Clinicaltrials.gov of the NIH .

[3] Vanda Pharma acquires world-wide license from Eli Lilly to develop & commercialize NK-1 receptor antagonist .

[4] Vanda Pharmaceuticals Announces Tradipitant Phase II Proof of Concept Study Results for Chronic Pruritus in Atopic Dermatitis , PM Vanda Pharmaceuticals, March 4, 2015, accessed May 4, 2015.