| 词条 | Tradipitant |
| 释义 |
| drug_name = | IUPAC_name = (2-(1-(3,5-Bis(trifluoromethyl)benzyl)-5-(pyridin-4-yl)-1H-1,2,3-triazol-4-yl)pyridin-3-yl)(2-chlorophenyl)methanone | image = LY686017.svg | alt = | caption = | pronounce = | tradename = | Drugs.com = | MedlinePlus = | pregnancy_AU = | pregnancy_AU_comment = | pregnancy_US = | pregnancy_category= | legal_AU = | legal_AU_comment = | legal_CA = | legal_DE = | legal_NZ = | legal_UK = | legal_US = | legal_UN = | legal_status = Investigational | routes_of_administration = | bioavailability = | protein_bound = | metabolism = | metabolites = | onset = | elimination_half-life = | duration_of_action = | excretion = | CAS_number = 622370-35-8 | ATCvet = | ATC_prefix = | ATC_suffix = | PubChem = 9916461 | DrugBank = | ChemSpiderID = 8092108 | chemical_formula = | C=28 | H=16 | Cl=1 | F=6 | N=5 | O=1 | molecular_weight = 587.90 g/mol | StdInChI = 1S/C28H16ClF6N5O/c29-22-6-2-1-4-20(22)26(41)21-5-3-9-37-23(21)24-25(17-7-10-36-11-8-17)40(39-38-24)15-16-12-18(27(30,31)32)14-19(13-16)28(33,34)35/h1-14H,15H2 | StdInChIKey = CAVRKWRKTNINFF-UHFFFAOYSA-N | smiles = Clc1ccccc1C(=O)c2c(nccc2)c3nnn(c3c4ccncc4)Cc5cc(cc(c5)C(F)(F)F)C(F)(F)F }}Tradipitant (VLY-686 or LY686017) is an experimental drug that is a neurokinin 1 antagonist. It works by blocking substance P, a small signaling molecule. Originally, this compound was owned by Eli Lilly and named LY686017. VLY-686 was purchased by Vanda Pharmaceuticals from Eli Lilly and Company in 2012.[1] Vanda Pharmaceuticals is a U.S. pharmaceutical company that as of November 2015 only has 3 drugs in their product pipeline: tasimelteon, VLY-686, and iloperidone.[2] IndicationsPruritusIt is being investigated by Vanda Pharmaceuticals for chronic pruritus (itchiness) in atopic dermatitis. In March 2015, Vanda announced positive results from a Phase II proof of concept study.[3] A proof of concept study is done in early stage clinical trials after there have been promising preclinical results. It provides preliminary evidence that the drug is active in humans and has some efficacy.[4] AlcoholismVLY-686 reduced alcohol craving in recently detoxified alcoholic patients as measured by the Alcohol Urge Questionnaire.[5] In a placebo controlled clinical trial of recently detoxified alcoholic patients, VLY-686 significantly reduced alcohol craving as measured by the Alcohol Urge Questionnaire. It also reduced the cortisol increase seen after a stress test compared to placebo. The dose given was 50 mg per day. Social anxiety disorderIn a 12-week randomized trial of LY68017 in 189 patients with social anxiety disorder, 50 mg of LY68017 did not provide any statistically significant improvement over placebo.[6] References1. ^{{cite web|title=Company Overview of Eli Lilly & Co., Worldwide License to Develop and Commercialize VLY-686|url=https://www.bloomberg.com/research/stocks/private/snapshot.asp?privcapId=195909200|website=Bloomberg Business|accessdate=16 November 2015}} {{Neurokinin receptor modulators}}2. ^ 3. ^{{cite news|title=Vanda Pharmaceuticals Announces Tradipitant Phase II Proof of Concept Study Results for Chronic Pruritus in Atopic Dermatitis|url=http://www.prnewswire.com/news-releases/vanda-pharmaceuticals-announces-tradipitant-phase-ii-proof-of-concept-study-results-for-chronic-pruritus-in-atopic-dermatitis-300045700.html|accessdate=16 November 2015|publisher=PR Newswire}} 4. ^{{cite journal|last1=Schmidt|first1=B|title=Proof of principle studies|journal=Epilepsy Res|date=2006|volume=68|issue=1|pages=48–52|pmid=16377153|doi=10.1016/j.eplepsyres.2005.09.019}} 5. ^{{cite journal|last1=George|first1=DT|last2=Gilman|first2=J|last3=Hersh|first3=J|title=Neurokinin 1 receptor antagonism as a possible therapy for alcoholism. |journal=Science|date=2008|pages=1536–1539|pmc=4567173|display-authors=etal|pmid=26379454|doi=10.2147/SAR.S70350|volume=6}} 6. ^{{cite journal|last1=Tauscher|first1=J|last2=Kielbasa|first2=W|last3=Iyengar|first3=S|title=Development of the 2nd generation neurokinin-1 receptor antagonist LY686017 for social anxiety disorder|journal=European Neuropsychopharmacology|volume=20|issue=2|pages=80–87|display-authors=etal|pmid=20018493|doi=10.1016/j.euroneuro.2009.10.005|year=2010}} 4 : NK1 receptor antagonists|Triazoles|Trifluoromethyl compounds|Pyridines |
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