词条 | Fevipiprant |
释义 |
| IUPAC_name = {2-methyl-1-[4-(methylsulfonyl)-2-(trifluoromethyl)benzyl]-1H-pyrrolo[2,3-b]pyridin-3-yl}acetic acid | image = Fevipiprant.svg | tradename = | pregnancy_category = | legal_status = Investigational | routes_of_administration = Oral | bioavailability = Unaffected by food[1] | metabolism = Hepatic glucuronidation | elimination_half-life = ~20 hours | excretion = Renal (≤30%) | CAS_number = 872365-14-5 | ATC_prefix = none | ATC_suffix = | KEGG = D10631 | PubChem = 23582412 | ChemSpiderID = 23582412 | UNII = 2PEX5N7DQ4 | C=19 | H=17 | F=3 | N=2 | O=4 | S=1 | molecular_weight = 426.41 g/mol | smiles = CC1=C(C2=C(N1CC3=C(C=C(C=C3)S(=O)(=O)C)C(F)(F)F)N=CC=C2)CC(=O)O | StdInChI=1S/C19H17F3N2O4S/c1-11-15(9-17(25)26)14-4-3-7-23-18(14)24(11)10-12-5-6-13(29(2,27)28)8-16(12)19(20,21)22/h3-8H,9-10H2,1-2H3,(H,25,26) | StdInChIKey = GFPPXZDRVCSVNR-UHFFFAOYSA-N }}Fevipiprant (INN; code name QAW039) is a drug being developed by Novartis which acts as a selective, orally available antagonist of the prostaglandin D2 receptor 2 (DP2 or CRTh2).[1][2][3]{{As of|2016}}, it is in phase III[4] clinical trials for the treatment of asthma.[5] See also
References1. ^1 {{cite journal|vauthors=Erpenbeck VJ, Vets E, Gheyle L, Osuntokun W, Larbig M, Neelakantham S, etal | title=Pharmacokinetics, Safety, and Tolerability of Fevipiprant (QAW039), a Novel CRTh2 Receptor Antagonist: Results From 2 Randomized, Phase 1, Placebo-Controlled Studies in Healthy Volunteers | journal=Clin Pharmacol Drug Dev | year= 2016 | volume= 5 | issue= 4 | pages= 306-13 | pmid=27310331 | doi=10.1002/cpdd.244 | pmc=5071756}} {{Asthma and copd rx}}{{Prostanoidergics}}{{respiratory-system-drug-stub}}2. ^Sykes DA, Bradley ME, Riddy DM, Willard E, Reilly J, Miah A, Bauer C, Watson SJ, Sandham DA, Dubois G, Charlton SJ. Fevipiprant (QAW039), a Slowly Dissociating CRTh2 Antagonist with the Potential for Improved Clinical Efficacy. Mol Pharmacol. 2016 May;89(5):593-605. doi: 10.1124/mol.115.101832 {{PMID|26916831}} 3. ^{{cite journal|vauthors=Erpenbeck VJ, Popov TA, Miller D, Weinstein SF, Spector S, Magnusson B, etal | title=The oral CRTh2 antagonist QAW039 (fevipiprant): A phase II study in uncontrolled allergic asthma | journal=Pulm Pharmacol Ther | year= 2016 | volume= 39 | issue= | pages= 54–63 | pmid=27354118 | doi=10.1016/j.pupt.2016.06.005}} 4. ^https://clinicaltrials.gov/ct2/show/NCT02555683 5. ^{{cite journal|vauthors=Gonem S, Berair R, Singapuri A, Hartley R, Laurencin M, Bacher G, etal | title=Fevipiprant, a prostaglandin D2 receptor 2 antagonist, in patients with persistent eosinophilic asthma: a single-centre, randomised, double-blind, parallel-group, placebo-controlled trial | journal=Lancet Respir Med | year=2016 | volume= 4| issue= | pages= 699–707| pmid= | doi=10.1016/S2213-2600(16)30179-5}} 5 : Antiasthmatic drugs|Receptor antagonists|Sulfones|Carboxylic acids|Trifluoromethyl compounds |
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