Two Phase II randomized trials on the CRTh2 antagonist AZD1981 in adults with asthma

References

• Global Initiative for Asthma (GINA)GINA Report, Global Strategy for Asthma Management and Prevention2016 Available from: http://ginasthma.org/2016-gina-report-global-strategy-for-asthma-management-and-prevention/Accessed June 2016
   Google Scholar
• RabeKFAdachiMLaiCKWorldwide severity and control of asthma in children and adults: the global asthma insights and reality surveysJ Allergy Clin Immunol20041141404715241342
   PubMed Web of Science ®Google Scholar
• HiraiHTanakaKYoshieOProstaglandin D2 selectively induces chemotaxis in T helper type 2 cells, eosinophils, and basophils via seven-transmembrane receptor CRTH2J Exp Med2001193225526111208866
   PubMed Web of Science ®Google Scholar
• NagataKHiraiHTanakaKCRTH2, an orphan receptor of T-helper-2-cells, is expressed on basophils and eosinophils and responds to mast cell-derived factor(s)FEBS Lett1999459219519910518017
   PubMed Web of Science ®Google Scholar
• NagataKTanakaKOgawaKSelective expression of a novel surface molecule by human Th2 cells in vivoJ Immunol19991623127812869973380
   PubMed Web of Science ®Google Scholar
• O’ByrnePMNajiNGauvreauGMSevere asthma: future treatmentsClin Exp Allergy201242570671122515391
   PubMed Web of Science ®Google Scholar
• MurrayJJTonnelABBrashARRelease of prostaglandin D2 into human airways during acute antigen challengeN Engl J Med1986315138008043462506
   PubMed Web of Science ®Google Scholar
• FajtMLGelhausSLFreemanBProstaglandin D(2) pathway upregulation: relation to asthma severity, control, and TH2 inflammationJ Allergy Clin Immunol201313161504151223506843
   PubMed Web of Science ®Google Scholar
• GervaisFGCruzRPChateauneufASelective modulation of chemokinesis, degranulation, and apoptosis in eosinophils through the PGD2 receptors CRTH2 and DPJ Allergy Clin Immunol2001108698298811742277
   PubMed Web of Science ®Google Scholar
• HiraiHTanakaKTakanoSIchimasaMNakamuraMNagataKCutting edge: agonistic effect of indomethacin on a prostaglandin D2 receptor, CRTH2J Immunol2002168398198511801628
   PubMed Web of Science ®Google Scholar
• StubbsVESchratlPHartnellAIndomethacin causes prostaglandin D(2)-like and eotaxin-like selective responses in eosinophils and basophilsJ Biol Chem200227729260122602011980903
   PubMed Web of Science ®Google Scholar
• ShirasakiHKikuchiMKanaizumiEHimiTAccumulation of CRTH2-positive leukocytes in human allergic nasal mucosaAnn Allergy Asthma Immunol2009102211011519230460
   PubMed Web of Science ®Google Scholar
• GylesSLXueLTownsendERWetteyFPettipherRA dominant role for chemoattractant receptor-homologous molecule expressed on T helper type 2 (Th2) cells (CRTH2) in mediating chemotaxis of CRTH2+ CD4+ Th2 lymphocytes in response to mast cell supernatantsImmunology2006119336236817067313
   PubMed Web of Science ®Google Scholar
• SchuligoiRSturmELuschnigPCRTH2 and D-type prostanoid receptor antagonists as novel therapeutic agents for inflammatory diseasesPharmacology201085637238220559016
   PubMed Web of Science ®Google Scholar
• PettipherRHanselTTAntagonists of the prostaglandin D2 receptor CRTH2Drug News Perspect200821631732218836589
   PubMedGoogle Scholar
• XueLBarrowAPettipherRInteraction between prostaglandin D and chemoattractant receptor-homologous molecule expressed on Th2 cells mediates cytokine production by Th2 lymphocytes in response to activated mast cellsClin Exp Immunol2009156112613319220324
   PubMed Web of Science ®Google Scholar
• XueLGylesSLWetteyFRProstaglandin D2 causes preferential induction of proinflammatory Th2 cytokine production through an action on chemoattractant receptor-like molecule expressed on Th2 cellsJ Immunol2005175106531653616272307
   PubMed Web of Science ®Google Scholar
• HeinemannASchuligoiRSabroeIHartnellAPeskarBADelta 12-prostaglandin J2, a plasma metabolite of prostaglandin D2, causes eosinophil mobilization from the bone marrow and primes eosinophils for chemotaxisJ Immunol200317094752475812707356
   PubMed Web of Science ®Google Scholar
• XueLBarrowAPettipherRNovel function of CRTH2 in preventing apoptosis of human Th2 cells through activation of the phosphatidylinositol 3-kinase pathwayJ Immunol2009182127580758619494281
   PubMed Web of Science ®Google Scholar
• LukacsNWBerlinAAFranz-BaconKCRTH2 antagonism significantly ameliorates airway hyperreactivity and downregulates inflammation-induced genes in a mouse model of airway inflammationAm J Physiol Lung Cell Mol Physiol20082955L767L77918757520
   PubMed Web of Science ®Google Scholar
• StebbinsKJBroadheadARCorreaLDTherapeutic efficacy of AM156, a novel prostanoid DP2 receptor antagonist, in murine models of allergic rhinitis and house dust mite-induced pulmonary inflammationEur J Pharmacol20106381–314214920447387
   PubMed Web of Science ®Google Scholar
• UllerLMathiesenJMAlenmyrLAntagonism of the prostaglandin D2 receptor CRTH2 attenuates asthma pathology in mouse eosinophilic airway inflammationRespir Res200781617328802
   PubMed Web of Science ®Google Scholar
• DiamantZSidhartaPNSinghDSetipiprant, a selective CRTH2 antagonist, reduces allergen-induced airway responses in allergic asthmaticsClin Exp Allergy20144481044105224964348
   PubMed Web of Science ®Google Scholar
• SidhartaPNDiamantZDingemanseJSingle- and multiple-dose tolerability and pharmacokinetics of the CRTH2 antagonist setipiprant in healthy male subjectsFundam Clin Pharmacol201428669069924734908
   PubMed Web of Science ®Google Scholar
• HorakFZieglmayerPZieglmayerRThe CRTH2 antagonist OC000459 reduces nasal and ocular symptoms in allergic subjects exposed to grass pollen, a randomised, placebo-controlled, double-blind trialAllergy201267121572157923025511
   PubMed Web of Science ®Google Scholar
• LukerTBonnertRBroughSSubstituted indole-1-acetic acids as potent and selective CRTh2 antagonists-discovery of AZD1981Bioorg Med Chem Lett201121216288629221944852
   PubMed Web of Science ®Google Scholar
• SinghDCaddenPHunterMInhibition of the asthmatic allergen challenge response by the CRTH2 antagonist OC000459Eur Respir J2013411465222496329
   PubMed Web of Science ®Google Scholar
• BarnesNPavordIChuchalinAA randomized, double-blind, placebo-controlled study of the CRTH2 antagonist OC000459 in moderate persistent asthmaClin Exp Allergy2012421384821762224
   PubMed Web of Science ®Google Scholar
• SchröderRXueLKonyaVPGH1, the precursor for the anti-inflammatory prostaglandins of the 1-series, is a potent activator of the pro-inflammatory receptor CRTH2/DP2PLoS One201273e3332922442685
   PubMed Web of Science ®Google Scholar
• BusseWWWenzelSEMeltzerEOSafety and efficacy of the prostaglandin D2 receptor antagonist AMG 853 in asthmatic patientsJ Allergy Clin Immunol2013131233934523174659
   PubMed Web of Science ®Google Scholar
• Nishikawa-ShimonoRSekiguchiYKoamiTIsoquinoline derivatives as potent CRTH2 receptor antagonists: synthesis and SARBioorg Med Chem Lett20122293305331022469703
   PubMed Web of Science ®Google Scholar