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Volumn 352, Issue 3, 2015, Pages 559-567

CHF6001 I: A novel highly potent and selective phosphodiesterase 4 inhibitor with robust anti-inflammatory activity and suitable for topical pulmonary administration

Author keywords

[No Author keywords available]

Indexed keywords

3,5 DICHLORO 4 [2 [3 (CYCLOPROPYLMETHOXY) 4 (DIFLUOROMETHOXY)PHENYL] 2 [3 (CYCLOPROPYLMETHOXY) 4 (METHYLSULFONAMIDO)BENZOYLOXY]ETHYL]PYRIDINE 1 OXIDE; BACTERIUM LIPOPOLYSACCHARIDE; BUDESONIDE; CILOMILAST; ESCHERICHIA COLI LIPOPOLYSACCHARIDE; GAMMA INTERFERON; GSK 256066; PHOSPHODIESTERASE IV; PHOSPHODIESTERASE IV INHIBITOR; ROFLUMILAST; TUMOR NECROSIS FACTOR ALPHA; UNCLASSIFIED DRUG; [2 (3,4 DIFLUOROPHENOXY) 5 FLUORO N 4 (2 HYDROXY 5 METHYLBENZAMIDO)CYCLOHEXYL]NICOTINAMIDE; ANTIINFLAMMATORY AGENT;

EID: 84922031641     PISSN: 00223565     EISSN: 15210103     Source Type: Journal    
DOI: 10.1124/jpet.114.220541     Document Type: Article
Times cited : (60)

References (39)
  • 2
    • 10344242415 scopus 로고    scopus 로고
    • Nonredundant function of phosphodiesterases 4D and 4B in neutrophil recruitment to the site of inflammation
    • Ariga M, Neitzert B, Nakae S, Mottin G, Bertrand C, Pruniaux MP, Jin SL, and Conti M (2004) Nonredundant function of phosphodiesterases 4D and 4B in neutrophil recruitment to the site of inflammation. J Immunol 173:7531-7538.
    • (2004) J Immunol , vol.173 , pp. 7531-7538
    • Ariga, M.1    Neitzert, B.2    Nakae, S.3    Mottin, G.4    Bertrand, C.5    Pruniaux, M.P.6    Jin, S.L.7    Conti, M.8
  • 3
    • 84894049174 scopus 로고    scopus 로고
    • Novel class of benzoic acid ester derivatives as potent PDE4 inhibitors for inhaled administration in the treatment of respiratory diseases
    • Armani E, Amari G, Rizzi A, De Fanti R, Ghidini E, Capaldi C, Carzaniga L, Caruso P, Guala M, Peretto I, et al. (2014) Novel class of benzoic acid ester derivatives as potent PDE4 inhibitors for inhaled administration in the treatment of respiratory diseases. J Med Chem 57:793-816.
    • (2014) J Med Chem , vol.57 , pp. 793-816
    • Armani, E.1    Amari, G.2    Rizzi, A.3    De Fanti, R.4    Ghidini, E.5    Capaldi, C.6    Carzaniga, L.7    Caruso, P.8    Guala, M.9    Peretto, I.10
  • 4
    • 0018595710 scopus 로고
    • Isolation and characterization of cGMP phosphodiesterase from bovine rod outer segments
    • Baehr W, Devlin MJ, and Applebury ML (1979) Isolation and characterization of cGMP phosphodiesterase from bovine rod outer segments. J Biol Chem 254:11669-11677.
    • (1979) J Biol Chem , vol.254 , pp. 11669-11677
    • Baehr, W.1    Devlin, M.J.2    Applebury, M.L.3
  • 5
    • 0029939872 scopus 로고    scopus 로고
    • Association of the anti-inflammatory activity of phosphodiesterase 4 (PDE4) inhibitors with either inhibition of PDE4 catalytic activity or competition for [3H]rolipram binding
    • Barnette MS, Bartus JO, Burman M, Christensen SB, Cieslinski LB, Esser KM, Prabhakar US, Rush JA, and Torphy TJ (1996) Association of the anti-inflammatory activity of phosphodiesterase 4 (PDE4) inhibitors with either inhibition of PDE4 catalytic activity or competition for [3H]rolipram binding. Biochem Pharmacol 51: 949-956.
    • (1996) Biochem Pharmacol , vol.51 , pp. 949-956
    • Barnette, M.S.1    Bartus, J.O.2    Burman, M.3    Christensen, S.B.4    Cieslinski, L.B.5    Esser, K.M.6    Prabhakar, U.S.7    Rush, J.A.8    Torphy, T.J.9
  • 7
    • 33748686575 scopus 로고    scopus 로고
    • Cyclic nucleotide phosphodiesterases: Molecular regulation to clinical use
    • Bender AT and Beavo JA (2006) Cyclic nucleotide phosphodiesterases: molecular regulation to clinical use. Pharmacol Rev 58:488-520.
    • (2006) Pharmacol Rev , vol.58 , pp. 488-520
    • Bender, A.T.1    Beavo, J.A.2
  • 8
    • 69149103642 scopus 로고    scopus 로고
    • Roflumilast in symptomatic chronic obstructive pulmonary disease: Two randomised clinical trials
    • Calverley PM, Rabe KF, Goehring UM, Kristiansen S, Fabbri LM, and Martinez FJ; M2-124 and M2-125 Study Groups (2009) Roflumilast in symptomatic chronic obstructive pulmonary disease: two randomised clinical trials. Lancet 374:685-694.
    • (2009) Lancet , vol.374 , pp. 685-694
    • Calverley, P.M.1    Rabe, K.F.2    Goehring, U.M.3    Kristiansen, S.4    Fabbri, L.M.5    Martinez, F.J.6
  • 9
    • 77649267205 scopus 로고    scopus 로고
    • The identification of markers of macrophage differentiation in PMA-stimulated THP-1 cells and monocyte-derived macrophages
    • Daigneault M, Preston JA, Marriott HM, Whyte MK, and Dockrell DH (2010) The identification of markers of macrophage differentiation in PMA-stimulated THP-1 cells and monocyte-derived macrophages. PLoS ONE 5:e8668.
    • (2010) PLoS ONE , vol.5 , pp. e8668
    • Daigneault, M.1    Preston, J.A.2    Marriott, H.M.3    Whyte, M.K.4    Dockrell, D.H.5
  • 10
    • 84922067846 scopus 로고    scopus 로고
    • Safety, tolerability and pharmacokinetics of a new inhaled once-daily phosphodiesterase (PDE) 4 inhibitor in healthy volunteers
    • Esposito O, Mariotti F, Acerbi D, Compagnoni A, and Nandeuil MA (2013) Safety, tolerability and pharmacokinetics of a new inhaled once-daily phosphodiesterase (PDE) 4 inhibitor in healthy volunteers. Eu Respir J 42 (Suppl 57):736.
    • (2013) Eu Respir J , vol.42 , pp. 736
    • Esposito, O.1    Mariotti, F.2    Acerbi, D.3    Compagnoni, A.4    Nandeuil, M.A.5
  • 11
    • 1842738219 scopus 로고    scopus 로고
    • Dopamine inhibits responses of astroglia-enriched cultures to lipopolysaccharide via a beta-adrenoreceptor-mediated mechanism
    • Facchinetti F, Del Giudice E, Furegato S, Passarotto M, Arcidiacono D, and Leon A (2004) Dopamine inhibits responses of astroglia-enriched cultures to lipopolysaccharide via a beta-adrenoreceptor-mediated mechanism. J Neuroimmunol 150:29-36.
    • (2004) J Neuroimmunol , vol.150 , pp. 29-36
    • Facchinetti, F.1    Del Giudice, E.2    Furegato, S.3    Passarotto, M.4    Arcidiacono, D.5    Leon, A.6
  • 12
    • 33644811309 scopus 로고    scopus 로고
    • Phosphodiesterase inhibitors in airways disease
    • Fan Chung K (2006) Phosphodiesterase inhibitors in airways disease. Eur J Pharmacol 533:110-117.
    • (2006) Eur J Pharmacol , vol.533 , pp. 110-117
    • Fan Chung, K.1
  • 13
    • 0030997247 scopus 로고    scopus 로고
    • In vitro differentiation of human monocytes to macrophages: Change of PDE profile and its relationship to suppression of tumour necrosis factor-alpha release by PDE inhibitors
    • Gantner F, Kupferschmidt R, Schudt C, Wendel A, and Hatzelmann A (1997) In vitro differentiation of human monocytes to macrophages: change of PDE profile and its relationship to suppression of tumour necrosis factor-alpha release by PDE inhibitors. Br J Pharmacol 121:221-231.
    • (1997) Br J Pharmacol , vol.121 , pp. 221-231
    • Gantner, F.1    Kupferschmidt, R.2    Schudt, C.3    Wendel, A.4    Hatzelmann, A.5
  • 14
    • 79851471591 scopus 로고    scopus 로고
    • Roflumilast: First phosphodiesterase 4 inhibitor approved for treatment of COPD
    • Giembycz MA and Field SK (2010) Roflumilast: first phosphodiesterase 4 inhibitor approved for treatment of COPD. Drug Des Devel Ther 4 :147-158.
    • (2010) Drug Des Devel Ther , vol.4 , pp. 147-158
    • Giembycz, M.A.1    Field, S.K.2
  • 15
    • 0020393662 scopus 로고
    • A model for the regulation of the calmodulin-dependent enzymes erythrocyte Ca2+-transport ATPase and brain phosphodiesterase by activators and inhibitors
    • Gietzen K, Sadorf I, and Bader H (1982) A model for the regulation of the calmodulin-dependent enzymes erythrocyte Ca2+-transport ATPase and brain phosphodiesterase by activators and inhibitors. Biochem J 207:541-548.
    • (1982) Biochem J , vol.207 , pp. 541-548
    • Gietzen, K.1    Sadorf, I.2    Bader, H.3
  • 16
    • 77953105482 scopus 로고    scopus 로고
    • The preclinical pharmacology of roflumilast - A selective, oral phosphodiesterase 4 inhibitor in development for chronic obstructive pulmonary disease
    • Hatzelmann A, Morcillo EJ, Lungarella G, Adnot S, Sanjar S, Beume R, Schudt C, and Tenor H (2010) The preclinical pharmacology of roflumilast - a selective, oral phosphodiesterase 4 inhibitor in development for chronic obstructive pulmonary disease. Pulm Pharmacol Ther 23:235-256.
    • (2010) Pulm Pharmacol Ther , vol.23 , pp. 235-256
    • Hatzelmann, A.1    Morcillo, E.J.2    Lungarella, G.3    Adnot, S.4    Sanjar, S.5    Beume, R.6    Schudt, C.7    Tenor, H.8
  • 17
    • 0035084103 scopus 로고    scopus 로고
    • Anti-inflammatory and immunomodulatory potential of the novel PDE4 inhibitor roflumilast in vitro
    • Hatzelmann A and Schudt C (2001) Anti-inflammatory and immunomodulatory potential of the novel PDE4 inhibitor roflumilast in vitro. J Pharmacol Exp Ther 297:267-279.
    • (2001) J Pharmacol Exp Ther , vol.297 , pp. 267-279
    • Hatzelmann, A.1    Schudt, C.2
  • 18
    • 84856082197 scopus 로고    scopus 로고
    • Anti-neutrophilic inflammatory activity of ASP3258, a novel phosphodiesterase type 4 inhibitor
    • Kubo S, Kobayashi M, Iwata M, Miyata K, Takahashi K, and Shimizu Y (2012) Anti-neutrophilic inflammatory activity of ASP3258, a novel phosphodiesterase type 4 inhibitor. Int Immunopharmacol 12:59-63.
    • (2012) Int Immunopharmacol , vol.12 , pp. 59-63
    • Kubo, S.1    Kobayashi, M.2    Iwata, M.3    Miyata, K.4    Takahashi, K.5    Shimizu, Y.6
  • 20
    • 77953821787 scopus 로고    scopus 로고
    • Cyclic nucleotide phosphodiesterase assay technology
    • MacKenzie SJ, Hastings SF, and Well C (2010) Cyclic nucleotide phosphodiesterase assay technology. Curr Prot Pharmacol 49(Suppl):12.1-26.
    • (2010) Curr Prot Pharmacol , vol.49 , pp. 12.1-26
    • MacKenzie, S.J.1    Hastings, S.F.2    Well, C.3
  • 24
    • 79960928267 scopus 로고    scopus 로고
    • Phosphodiesterase inhibitors in the treatment of inflammatory diseases
    • Page CP and Spina D (2011) Phosphodiesterase inhibitors in the treatment of inflammatory diseases. Handbook Exp Pharmacol 204:391-414.
    • (2011) Handbook Exp Pharmacol , vol.204 , pp. 391-414
    • Page, C.P.1    Spina, D.2
  • 25
    • 74949133079 scopus 로고    scopus 로고
    • PDE4 inhibitors: A review of current developments (2005 - 2009)
    • Pagès L, Gavaldà A, and Lehner MD (2009) PDE4 inhibitors: a review of current developments (2005 - 2009). Expert Opin Ther Pat 19:1501-1519.
    • (2009) Expert Opin Ther Pat , vol.19 , pp. 1501-1519
    • Pagès, L.1    Gavaldà, A.2    Lehner, M.D.3
  • 26
    • 62849095350 scopus 로고    scopus 로고
    • PDE4 inhibitors - A review of the current field
    • Press NJ and Banner KH (2009) PDE4 inhibitors - a review of the current field. Prog Med Chem 47:37-74.
    • (2009) Prog Med Chem , vol.47 , pp. 37-74
    • Press, N.J.1    Banner, K.H.2
  • 27
    • 34247471787 scopus 로고    scopus 로고
    • The neutrophil in chronic obstructive pulmonary disease
    • Quint JK and Wedzicha JA (2007) The neutrophil in chronic obstructive pulmonary disease. J Allergy Clin Immunol 119:1065-1071.
    • (2007) J Allergy Clin Immunol , vol.119 , pp. 1065-1071
    • Quint, J.K.1    Wedzicha, J.A.2
  • 29
    • 0026354677 scopus 로고
    • Influence of selective phosphodiesterase inhibitors on human neutrophil functions and levels of cAMP and Cai
    • Schudt C, Winder S, Forderkunz S, Hatzelmann A, and Ullrich V (1991) Influence of selective phosphodiesterase inhibitors on human neutrophil functions and levels of cAMP and Cai. Naunyn Schmiedebergs Arch Pharmacol 344:682-690.
    • (1991) Naunyn Schmiedebergs Arch Pharmacol , vol.344 , pp. 682-690
    • Schudt, C.1    Winder, S.2    Forderkunz, S.3    Hatzelmann, A.4    Ullrich, V.5
  • 30
    • 77952491177 scopus 로고    scopus 로고
    • The inhaled phosphodiesterase 4 inhibitor GSK256066 reduces allergen challenge responses in asthma
    • Singh D, Petavy F, Macdonald AJ, Lazaar AL, and O'Connor BJ (2010) The inhaled phosphodiesterase 4 inhibitor GSK256066 reduces allergen challenge responses in asthma. Respir Res 11:11-26.
    • (2010) Respir Res , vol.11 , pp. 11-26
    • Singh, D.1    Petavy, F.2    Macdonald, A.J.3    Lazaar, A.L.4    O'Connor, B.J.5
  • 31
    • 0030925148 scopus 로고    scopus 로고
    • Proposal for pharmacologically distinct conformers of PDE4 cyclic AMP phosphodiesterases
    • Souness JE and Rao S (1997) Proposal for pharmacologically distinct conformers of PDE4 cyclic AMP phosphodiesterases. Cell Signal 9:227-236.
    • (1997) Cell Signal , vol.9 , pp. 227-236
    • Souness, J.E.1    Rao, S.2
  • 32
    • 0344513958 scopus 로고    scopus 로고
    • Phosphodiesterase-4 inhibitors in the treatment of inflammatory lung disease
    • Spina D (2003) Phosphodiesterase-4 inhibitors in the treatment of inflammatory lung disease. Drugs 63:2575-2594.
    • (2003) Drugs , vol.63 , pp. 2575-2594
    • Spina, D.1
  • 33
    • 61449112246 scopus 로고    scopus 로고
    • Subtype selectivity in phosphodiesterase 4 (PDE4): A bottleneck in rational drug design
    • Srivani P, Usharani D, Jemmis ED, and Sastry GN (2008) Subtype selectivity in phosphodiesterase 4 (PDE4): a bottleneck in rational drug design. Curr Pharm Des 14:3854-3872.
    • (2008) Curr Pharm Des , vol.14 , pp. 3854-3872
    • Srivani, P.1    Usharani, D.2    Jemmis, E.D.3    Sastry, G.N.4
  • 34
    • 0015231739 scopus 로고
    • Multiple cyclic nucleotide phosphodiesterase activities from rat brain
    • Thompson WJ and Appleman MM (1971) Multiple cyclic nucleotide phosphodiesterase activities from rat brain. Biochemistry 10:311-316.
    • (1971) Biochemistry , vol.10 , pp. 311-316
    • Thompson, W.J.1    Appleman, M.M.2
  • 36
    • 66749187721 scopus 로고    scopus 로고
    • A controlled trial of 6-weeks' treatment with a novel inhaled phosphodiesterase type-4 inhibitor in COPD
    • Vestbo J, Tan L, Atkinson G, and Ward J; UK-500,001 Global Study Team (2009) A controlled trial of 6-weeks' treatment with a novel inhaled phosphodiesterase type-4 inhibitor in COPD. Eur Respir J 33:1039-1044.
    • (2009) Eur Respir J , vol.33 , pp. 1039-1044
    • Vestbo, J.1    Tan, L.2    Atkinson, G.3    Ward, J.4
  • 37
    • 84922041417 scopus 로고    scopus 로고
    • CHF6001 II: A novel phosphodiesterase 4 inhibitor, suitable for topical pulmonary administration - In vivo preclinical pharmacology profile defines a potent anti-inflammatory compound with a wide therapeutic window
    • Villetti G, Carnini C, Battipaglia L, Preynat L, Bolzoni PT, Bassani F, Caruso P, Bergamaschi M, Pisano AR, Puviani V, et al. (2015) CHF6001 II: a novel phosphodiesterase 4 inhibitor, suitable for topical pulmonary administration - in vivo preclinical pharmacology profile defines a potent anti-inflammatory compound with a wide therapeutic window. J Pharmacol Exp Ther 352:568-578.
    • (2015) J Pharmacol Exp Ther , vol.352 , pp. 568-578
    • Villetti, G.1    Carnini, C.2    Battipaglia, L.3    Preynat, L.4    Bolzoni, P.T.5    Bassani, F.6    Caruso, P.7    Bergamaschi, M.8    Pisano, A.R.9    Puviani, V.10
  • 38
    • 22944450858 scopus 로고    scopus 로고
    • Neutrophils and eosinophils: Clinical implications of their appearance, presence and disappearance in asthma and COPD
    • Watt AP, Schock BC, and Ennis M (2005) Neutrophils and eosinophils: clinical implications of their appearance, presence and disappearance in asthma and COPD. Curr Drug Targets Inflamm Allergy 4:415-423.
    • (2005) Curr Drug Targets Inflamm Allergy , vol.4 , pp. 415-423
    • Watt, A.P.1    Schock, B.C.2    Ennis, M.3
  • 39
    • 84882569009 scopus 로고    scopus 로고
    • Safety and tolerability of the inhaled phosphodiesterase 4 inhibitor GSK256066 in moderate COPD
    • Watz H, Mistry SJ, and Lazaar AL; IPC101939 investigators (2013) Safety and tolerability of the inhaled phosphodiesterase 4 inhibitor GSK256066 in moderate COPD. Pulm Pharmacol Ther 26:588-595.
    • (2013) Pulm Pharmacol Ther , vol.26 , pp. 588-595
    • Watz, H.1    Mistry, S.J.2    Lazaar, A.L.3


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