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Drug Evaluation

Roflumilast: an oral, once-daily selective PDE-4 inhibitor for the management of COPD and asthma

, MD FRCPC
Pages 811-818 | Published online: 30 Apr 2008

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Mark A Giembycz & Stephen K Field. (2010) Roflumilast: first phosphodiesterase 4 inhibitor approved for treatment of COPD. Drug Design, Development and Therapy 4, pages 147-158.
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Nicholas J. Gross, Mark A. Giembycz & Stephen I. Rennard. (2010) Treatment of Chronic Obstructive Pulmonary Disease with Roflumilast, a New Phosphodiesterase 4 Inhibitor. COPD: Journal of Chronic Obstructive Pulmonary Disease 7:2, pages 141-153.
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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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Bachir Latli, Matt J. Hrapchak, Thomas G. Tampone, Rogelio P. Frutos & Heewon Lee. (2023) Carbon 14 and stable isotope synthesis of two potent and selective phosphodiesterase type 4 inhibitors. Journal of Labelled Compounds and Radiopharmaceuticals.
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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 .
Mustafa Çelebier, Aysegul Dogan, İncilay Süslü & Sacide Altınöz. (2021) Electrochemical Behavior and Square-Wave Stripping Voltammetric Determination of Roflumilast in Pharmaceutical Dosage Forms. Combinatorial Chemistry & High Throughput Screening 24:3, pages 400-408.
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Tadashi Honda & Iwao Ojima. 2021. The Curious World of Fluorinated Molecules. The Curious World of Fluorinated Molecules 241 276 .
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Lucienne Juillerat-Jeanneret, John-David Aubert, Josip Mikulic & Dela Golshayan. (2018) Fibrogenic Disorders in Human Diseases: From Inflammation to Organ Dysfunction. Journal of Medicinal Chemistry 61:22, pages 9811-9840.
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Dong-yang Liu, Zhi-guo Wang, Yuan Gao, Hui-min Zhang, Yu-xiang Zhang, Xiao-jun Wang & Dan Peng. (2018) Effect and safety of roflumilast for chronic obstructive pulmonary disease in Chinese patients. Medicine 97:7, pages e9864.
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Xiaojing Liu & Zhihong Chen. (2017) The pathophysiological role of mitochondrial oxidative stress in lung diseases. Journal of Translational Medicine 15:1.
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Yousheng Wang & Hengming Ke. 2017. Phosphodiesterases: CNS Functions and Diseases. Phosphodiesterases: CNS Functions and Diseases 463 471 .
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Agnieszka J. Rybarczyk-Pirek, Marlena Łukomska-Rogala, Sławomir Wojtulewski & Marcin Palusiak. (2015) N -Oxide as a Proton Accepting Group in Multicomponent Crystals: X-ray and Theoretical Studies on New p -Nitropyridine- N -oxide Co-Crystals . Crystal Growth & Design 15:12, pages 5802-5815.
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Rabah Ahmed Taha Serya, Abeer Hussin Abbas, Nasser Saad Mohamed Ismail, Ahmed Esmat & Dalal Abdelrahman Abou El Ella. (2015) Design, Synthesis and Biological Evaluation of Novel Quinazoline-Based Anti-inflammatory Agents Acting as PDE4B Inhibitors. CHEMICAL & PHARMACEUTICAL BULLETIN Chemical and Pharmaceutical Bulletin 63:2, pages 102-116.
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Peng Zhao, Shang-Ke Chen, Ying-Hong Cai, Xiao Lu, Zhe Li, Yuen-Kit Cheng, Cuixian Zhang, Xiaopeng Hu, Xixin He & Hai-Bin Luo. (2013) The molecular basis for the inhibition of phosphodiesterase-4D by three natural resveratrol analogs. Isolation, molecular docking, molecular dynamics simulations, binding free energy, and bioassay. Biochimica et Biophysica Acta (BBA) - Proteins and Proteomics 1834:10, pages 2089-2096.
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Judith A. Siuciak & William J. Pitts. 2012. Targets and Emerging Therapies for Schizophrenia. Targets and Emerging Therapies for Schizophrenia 85 113 .
Gabriel Eckermann, Gezim Lahu, Nassr Nassr & Thomas D. Bethke. (2012) Absence of Pharmacokinetic Interaction Between Roflumilast and Digoxin in Healthy Adults. The Journal of Clinical Pharmacology 52:2, pages 251-257.
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Stefan Ückert, Eginhard S. Waldkirch, Joachim E. Sonnenberg, Peter Sandner, Markus A. Kuczyk & Petter Hedlund. (2011) Expression and Distribution of Phosphodiesterase Isoenzymes in the Human Seminal Vesicles. The Journal of Sexual Medicine 8:11, pages 3058-3065.
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SANG-DO LEE, DAVID S. C. HUI, AZIAH A. MAHAYIDDIN, CAMILO C. ROA JR, KHENG HOE KWA, UDO-MICHAEL GOEHRING, DIRK BREDENBRÖKER & HAN-PIN KUO. (2011) Roflumilast in Asian patients with COPD: A randomized placebo-controlled trial. Respirology 16:8, pages 1249-1257.
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Klaus F. Rabe. (2011) Update on roflumilast, a phosphodiesterase 4 inhibitor for the treatment of chronic obstructive pulmonary disease. British Journal of Pharmacology 163:1, pages 53-67.
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Gezim Lahu, Nassr Nassr, Rolf Herzog, Martin Elmlinger, Peter Ruth, Markus Hinder & Andreas Huennemeyer. (2011) Effect of Steady-State Enoxacin on Single-Dose Pharmacokinetics of Roflumilast and Roflumilast N-Oxide. The Journal of Clinical Pharmacology 51:4, pages 586-593.
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Bora InceogluKaren WagnerNils H. SchebbChristophe MorisseauSteven L. Jinks, Arzu UluChristine HegedusTristan RoseRobert Brosnan & Bruce D. Hammock. (2011) Analgesia mediated by soluble epoxide hydrolase inhibitors is dependent on cAMP. Proceedings of the National Academy of Sciences 108:12, pages 5093-5097.
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Stephen K. Field. (2011) Roflumilast, a Novel Phosphodiesterase 4 Inhibitor, for COPD Patients with a History of Exacerbations. Clinical Medicine Insights: Circulatory, Respiratory and Pulmonary Medicine 5, pages CCRPM.S7049.
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Joanne Bronson, Murali Dhar, William Ewing & Nils Lonberg. 2011. 433 502 .
Chris Rundfeldt, Katarzyna Socała & Piotr Wlaź. (2010) The atypical anxiolytic drug, tofisopam, selectively blocks phosphodiesterase isoenzymes and is active in the mouse model of negative symptoms of psychosis. Journal of Neural Transmission 117:11, pages 1319-1325.
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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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Pierfrancesco Biagini, Claudio Biancalani, Alessia Graziano, Nicoletta Cesari, Maria Paola Giovannoni, Agostino Cilibrizzi, Vittorio Dal Piaz, Claudia Vergelli, Letizia Crocetti, Maurizio Delcanale, Elisabetta Armani, Andrea Rizzi, Paola Puccini, Paola Maria Gallo, Daniele Spinabelli & Paola Caruso. (2010) Functionalized pyrazoles and pyrazolo[3,4-d]pyridazinones: Synthesis and evaluation of their phosphodiesterase 4 inhibitory activity. Bioorganic & Medicinal Chemistry 18:10, pages 3506-3517.
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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 747 790 .
Shashi P. Singh, Neerad C. Mishra, Jules Rir-sima-ah, Mathew Campen, Viswanath Kurup, Seddigheh Razani-Boroujerdi & Mohan L. Sopori. (2009) Maternal Exposure to Secondhand Cigarette Smoke Primes the Lung for Induction of Phosphodiesterase-4D5 Isozyme and Exacerbated Th2 Responses: Rolipram Attenuates the Airway Hyperreactivity and Muscarinic Receptor Expression but Not Lung Inflammation and Atopy. The Journal of Immunology 183:3, pages 2115-2121.
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