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Drug Evaluation

Phosphodiesterase-4 inhibitors as a novel approach for the treatment of respiratory disease: cilomilast

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Pages 109-124 | Published online: 07 Dec 2006

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Polyxeni Ntontsi, Aggeliki Detta, Petros Bakakos, Stelios Loukides & Georgios Hillas. (2019) Experimental and investigational phosphodiesterase inhibitors in development for asthma. Expert Opinion on Investigational Drugs 28:3, pages 261-266.
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Yung-Fong Tsai & Tsong-Long Hwang. (2015) Neutrophil elastase inhibitors: a patent review and potential applications for inflammatory lung diseases (2010 – 2014). Expert Opinion on Therapeutic Patents 25:10, pages 1145-1158.
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Noemi Busquets-Perez, Helena Marzo-Ortega & Paul Emery. (2013) Emerging drugs for axial spondyloarthritis including ankylosing spondylitis. Expert Opinion on Emerging Drugs 18:1, pages 71-86.
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Kazuhiro Ito & Nicolas Mercado. (2009) Therapeutic targets for new therapy for corticosteroid refractory asthma. Expert Opinion on Therapeutic Targets 13:9, pages 1053-1067.
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Sha ZHU, Genqing YANG, Xiaolan YANG, Yunsheng ZHAO, Xiang LI, Ping DENG, Yanling XIE, Zhiyong GAN, Yin LIU, Zhirong LI, Juan LIAO, Ming’an YU & Fei LIAO. (2009) Soluble Expression in Escherichia coli of Active Human Cyclic Nucleotide Phosphodiesterase Isoform 4B2 in Fusion with Maltose-Binding Protein. Bioscience, Biotechnology, and Biochemistry 73:4, pages 968-970.
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Bruce K Rubin & James B Fink. (2007) Novel medications for asthma: a look at the future. Expert Opinion on Investigational Drugs 16:6, pages 889-897.
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Articles from other publishers (33)

Baochan Du, Min Luo, Changyu Ren & Jifa Zhang. (2023) PDE4 inhibitors for disease therapy: advances and future perspective. Future Medicinal Chemistry.
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Martin Alexander Schick & Nicolas Schlegel. (2022) Clinical Implication of Phosphodiesterase-4-Inhibition. International Journal of Molecular Sciences 23:3, pages 1209.
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Donald J. AbrahamJohn G. Montana, Hazel J. Dyke, J. Craig Fox & Nicholas C. Ray. 2003. Burger's Medicinal Chemistry and Drug Discovery. Burger's Medicinal Chemistry and Drug Discovery 1 47 .
Wei‐Yu Chen, Chih‐Hsueh Lin, Yu‐Sheng Lee, Pei‐Chen Tsao & Mei‐Jy Jeng. (2020) Pathophysiological effects of intravenous phosphodiesterase type 4 inhibitor in addition to surfactant lavage in meconium‐injured newborn piglet lungs. Pediatric Pulmonology 55:9, pages 2272-2282.
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Matthias C. HüttenMarkus FehrholzFranziska M. KonradDaan OpheldersClementine KleintjesBarbara OttensmeierOwen Brad SpillerKirsten GlaserBoris W. KramerSteffen Kunzmann. (2019) Detrimental Effects of an Inhaled Phosphodiesterase-4 Inhibitor on Lung Inflammation in Ventilated Preterm Lambs Exposed to Chorioamnionitis Are Dose Dependent. Journal of Aerosol Medicine and Pulmonary Drug Delivery 32:6, pages 396-404.
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Yung-Fong Tsai, Chun-Yu Chen, Wen-Yi Chang, Yu-Ting Syu & Tsong-Long Hwang. (2019) Resveratrol suppresses neutrophil activation via inhibition of Src family kinases to attenuate lung injury. Free Radical Biology and Medicine 145, pages 67-77.
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Cheng-Yu Lin, Ching-Yun Hsu, Ahmed O. Elzoghby, Ahmed Alalaiwe, Tsong-Long Hwang & Jia-You Fang. (2019) Oleic acid as the active agent and lipid matrix in cilomilast-loaded nanocarriers to assist PDE4 inhibition of activated neutrophils for mitigating psoriasis-like lesions. Acta Biomaterialia 90, pages 350-361.
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Jian Luo, Ling Yang, Jing Yang, Dan Yang, Bi-Cui Liu, Dan Liu, Bin-Miao Liang & Chun-Tao Liu. (2018) Efficacy and safety of phosphodiesterase 4 inhibitors in patients with asthma: A systematic review and meta-analysis. Respirology 23:5, pages 467-477.
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Laura Carzaniga, Gabriele Amari, Andrea Rizzi, Carmelida Capaldi, Renato De Fanti, Eleonora Ghidini, Gino Villetti, Chiara Carnini, Nadia Moretto, Fabrizio Facchinetti, Paola Caruso, Gessica Marchini, Loredana Battipaglia, Riccardo Patacchini, Valentina Cenacchi, Roberta Volta, Francesco Amadei, Alice Pappani, Silvia Capacchi, Valentina Bagnacani, Maurizio Delcanale, Paola Puccini, Silvia Catinella, Maurizio Civelli & Elisabetta Armani. (2017) Discovery and Optimization of Thiazolidinyl and Pyrrolidinyl Derivatives as Inhaled PDE4 Inhibitors for Respiratory Diseases. Journal of Medicinal Chemistry 60:24, pages 10026-10046.
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Brijeshkumar S. Patel, Pavan Prabhala, Brian G. Oliver & Alaina J. Ammit. (2015) Inhibitors of Phosphodiesterase 4, but Not Phosphodiesterase 3, Increase β 2 -Agonist–Induced Expression of Antiinflammatory Mitogen-Activated Protein Kinase Phosphatase 1 in Airway Smooth Muscle Cells . American Journal of Respiratory Cell and Molecular Biology 52:5, pages 634-640.
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Olga Bruno, Roberta Ricciarelli, Jos Prickaerts, Linda Parker & Ernesto Fedele. (2014) PDE4D inhibitors: A potential strategy for the treatment of memory impairment?. Neuropharmacology 85, pages 290-292.
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TING ZHANG & XIANGDONG ZHOU. (2014) Clinical application of expectorant therapy in chronic inflammatory airway diseases (Review). Experimental and Therapeutic Medicine 7:4, pages 763-767.
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Frank Wunder, Ramona Quednau, Andreas Geerts, Martina Barg & Adrian Tersteegen. (2013) Characterization of the Cellular Activity of PDE 4 Inhibitors Using Two Novel PDE 4 Reporter Cell Lines. Molecular Pharmaceutics 10:10, pages 3697-3705.
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Petr A. Zhmurov, Alexey Yu. Sukhorukov, Vladimir I. Chupakhin, Yulia V. Khomutova, Sema L. Ioffe & Vladimir A. Tartakovsky. (2013) Synthesis of PDE IV inhibitors. First asymmetric synthesis of two of GlaxoSmithKline's highly potent Rolipram analogues. Organic & Biomolecular Chemistry 11:46, pages 8082.
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Jan Lötvall & Bo Lundbäck. 2012. Advances in Combination Therapy for Asthma and COPD. Advances in Combination Therapy for Asthma and COPD 296 310 .
Alexey Yu. Sukhorukov, Yaroslav D. Boyko, Sema L. Ioffe, Yulia A. Khomutova, Yulia V. Nelyubina & Vladimir A. Tartakovsky. (2011) Synthesis of PDE IVb Inhibitors. 1. Asymmetric Synthesis and Stereochemical Assignment of (+)- and (−)-7-[3-(Cyclopentyloxy)-4-methoxyphenyl]hexahydro-3 H -pyrrolizin-3-one . The Journal of Organic Chemistry 76:19, pages 7893-7900.
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Andrew J. Halayko & Pawan Sharma. 2011. Inflammation and Allergy Drug Design. Inflammation and Allergy Drug Design 163 171 .
Arata Yanagisawa, Masashi Taga, Toshiyuki Atsumi, Koichiro Nishimura, Kyoji Ando, Tsuyoshi Taguchi, Hiroshi Tsumuki, Iwao Chujo & Shin-ichiro Mohri. (2011) Process Development of the PDE4 Inhibitor K-34. Organic Process Research & Development 15:2, pages 376-381.
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Arata Yanagisawa, Koichiro Nishimura, Kyoji Ando, Tetsuya Nezu, Ayako Maki, Sachiko Kato, Wakako Tamaki, Eiichiro Imai & Shin-ichiro Mohri. (2010) A Practical Synthesis of the PDE4 Inhibitor, KW-4490. Organic Process Research & Development 14:5, pages 1182-1187.
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Renee Aspiotis, Denis Deschênes, Daniel Dubé, Yves Girard, Zheng Huang, France Laliberté, Susana Liu, Robert Papp, Donald W. Nicholson & Robert N. Young. (2010) The discovery and synthesis of highly potent subtype selective phosphodiesterase 4D inhibitors. Bioorganic & Medicinal Chemistry Letters 20:18, pages 5502-5505.
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Armin Hatzelmann, Esteban J. Morcillo, Giuseppe Lungarella, Serge Adnot, Shahin Sanjar, Rolf Beume, Christian Schudt & Hermann Tenor. (2010) The preclinical pharmacology of roflumilast – A selective, oral phosphodiesterase 4 inhibitor in development for chronic obstructive pulmonary disease. Pulmonary Pharmacology & Therapeutics 23:4, pages 235-256.
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Xinglong JiangGeorge T. LeeEdwin B. VillhauerKapa PrasadMahavir Prashad. (2010) A Scalable Synthesis of a 1,7-Naphthyridine Derivative, a PDE-4 Inhibitor. Organic Process Research & Development 14:4, pages 883-889.
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Susan Lu, Nancy Liu, S. Balachandra Dass, Theodore F. Reiss & Barbara A. Knorr. (2009) Randomized, placebo-controlled study of a selective PDE4 inhibitor in the treatment of asthma. Respiratory Medicine 103:3, pages 342-347.
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Chizumi Nomura-Furuwatari, Shigeyuki Wakitani, Yusuke Hashimoto, Yuuki Imai, Yoichi Ohta, Keisuke Nakagawa, Yoshihiro Nakao, Kazushi Takayama, Tomoya Manaka & Kunio Takaoka. (2008) Expression profiles of phosphodiesterase 4D splicing variants in osteoblastic cells. Journal of Bone and Mineral Metabolism 26:2, pages 152-158.
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Amanda P. Skoumbourdis, Ruili Huang, Noel Southall, William Leister, Vicky Guo, Ming-Hsuang Cho, James Inglese, Marshall Nirenberg, Christopher P. Austin, Menghang Xia & Craig J. Thomas. (2008) Identification of a potent new chemotype for the selective inhibition of PDE4. Bioorganic & Medicinal Chemistry Letters 18:4, pages 1297-1303.
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Nicolas Daguès, Valérie Pawlowski, Cécile Sobry, Gilles Hanton, Françoise Borde, Sylvain Soler, Jean-Louis Freslon & Stephan Chevalier. (2007) Investigation of the Molecular Mechanisms Preceding PDE4 Inhibitor-Induced Vasculopathy in Rats: Tissue Inhibitor of Metalloproteinase 1, a Potential Predictive Biomarker. Toxicological Sciences 100:1, pages 238-247.
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