CHF6001 I: A Novel Highly Potent and Selective Phosphodiesterase 4 Inhibitor with Robust Anti-Inflammatory Activity and Suitable for Topical Pulmonary Administration

Nadia Moretto; Paola Caruso; Raffaella Bosco; Gessica Marchini; Fiorella Pastore; Elisabetta Armani; Gabriele Amari; Andrea Rizzi; Eleonora Ghidini; Renato De Fanti; Carmelida Capaldi; Laura Carzaniga; Emilio Hirsch; Carola Buccellati; Angelo Sala; Chiara Carnini; Riccardo Patacchini; Maurizio Delcanale; Maurizio Civelli; Gino Villetti; Fabrizio Facchinetti

doi:10.1124/jpet.114.220541

CHF6001 I: A Novel Highly Potent and Selective Phosphodiesterase 4 Inhibitor with Robust Anti-Inflammatory Activity and Suitable for Topical Pulmonary Administration

Journal of Pharmacology and Experimental Therapeutics ◽

10.1124/jpet.114.220541 ◽

2015 ◽

Vol 352 (3) ◽

pp. 559-567 ◽

Cited By ~ 40

Author(s):

Nadia Moretto ◽

Paola Caruso ◽

Raffaella Bosco ◽

Gessica Marchini ◽

Fiorella Pastore ◽

...

Keyword(s):

Inflammatory Activity ◽

Pulmonary Administration ◽

Phosphodiesterase 4 ◽

Anti Inflammatory ◽

Phosphodiesterase 4 Inhibitor

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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

Journal of Pharmacology and Experimental Therapeutics ◽

10.1124/jpet.114.220558 ◽

2015 ◽

Vol 352 (3) ◽

pp. 568-578 ◽

Cited By ~ 26

Author(s):

Gino Villetti ◽

Chiara Carnini ◽

Loredana Battipaglia ◽

Laurent Preynat ◽

Pier Tonino Bolzoni ◽

...

Keyword(s):

Therapeutic Window ◽

Pulmonary Administration ◽

Phosphodiesterase 4 ◽

Preclinical Pharmacology ◽

Anti Inflammatory ◽

Phosphodiesterase 4 Inhibitor

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Faculty Opinions recommendation of Apremilast, a cAMP phosphodiesterase-4 inhibitor, demonstrates anti-inflammatory activity in vitro and in a model of psoriasis.

Faculty Opinions – Post-Publication Peer Review of the Biomedical Literature ◽

10.3410/f.719848696.793517124 ◽

2016 ◽

Author(s):

Kamran Ghoreschi

Keyword(s):

Inflammatory Activity ◽

Camp Phosphodiesterase ◽

Phosphodiesterase 4 ◽

Anti Inflammatory ◽

Phosphodiesterase 4 Inhibitor

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Apremilast, a cAMP phosphodiesterase-4 inhibitor, demonstrates anti-inflammatory activity in vitro and in a model of psoriasis

British Journal of Pharmacology ◽

10.1111/j.1476-5381.2009.00559.x ◽

2009 ◽

Vol 159 (4) ◽

pp. 842-855 ◽

Cited By ~ 232

Author(s):

PH Schafer ◽

A Parton ◽

AK Gandhi ◽

L Capone ◽

M Adams ◽

...

Keyword(s):

Inflammatory Activity ◽

Camp Phosphodiesterase ◽

Phosphodiesterase 4 ◽

Anti Inflammatory ◽

Phosphodiesterase 4 Inhibitor

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DRM02, a novel phosphodiesterase-4 inhibitor with cutaneous anti-inflammatory activity

Tissue Barriers ◽

10.1080/21688370.2020.1765633 ◽

2020 ◽

Vol 8 (3) ◽

pp. 1765633

Author(s):

David W.C. Hunt ◽

Iordanka A. Ivanova ◽

Lina Dagnino

Keyword(s):

Inflammatory Activity ◽

Phosphodiesterase 4 ◽

Anti Inflammatory ◽

Phosphodiesterase 4 Inhibitor

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GS-5759, A Novel Bi-Functional Phosphodiesterase 4 Inhibitor And Long-Acting ²2-Adrenoceptor Agonist Has Potent Anti-Inflammatory Activity In Human Monocytes And Neutrophils

10.1164/ajrccm-conference.2012.185.1_meetingabstracts.a5703 ◽

2012 ◽

Author(s):

Eric A. Sorensen ◽

Stacey L. Tannheimer ◽

Aaron C. Haran ◽

Clifford D. Wright ◽

Michael Salmon

Keyword(s):

Inflammatory Activity ◽

Human Monocytes ◽

Phosphodiesterase 4 ◽

Adrenoceptor Agonist ◽

Anti Inflammatory ◽

Long Acting ◽

Phosphodiesterase 4 Inhibitor

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TAS-203, an oral phosphodiesterase 4 inhibitor, exerts anti-inflammatory activities in a rat airway inflammation model

European Journal of Pharmacology ◽

10.1016/j.ejphar.2019.01.068 ◽

2019 ◽

Vol 849 ◽

pp. 22-29 ◽

Cited By ~ 2

Author(s):

Shunsuke Demizu ◽

Naomasa Asaka ◽

Hiroyuki Kawahara ◽

Eiji Sasaki

Keyword(s):

Airway Inflammation ◽

Phosphodiesterase 4 ◽

Inflammation Model ◽

Anti Inflammatory ◽

Phosphodiesterase 4 Inhibitor

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A Novel Nonsteroidal, Topical Anti-inflammatory, Phosphodiesterase 4 Inhibitor, Crisaborole Ointment, Reduced Pruritus and Signs of Atopic Dermatitis in 2 Phase 3 Studies in Children and Adults

10.1542/peds.141.1_meetingabstract.251 ◽

2018 ◽

Author(s):

Adelaide A. Hebert ◽

Lawrence F. Eichenfield ◽

Mark G. Lebwohl ◽

Amy S. Paller ◽

Eric L. Simpson ◽

...

Keyword(s):

Atopic Dermatitis ◽

Phase 3 ◽

Phosphodiesterase 4 ◽

Anti Inflammatory ◽

Phosphodiesterase 4 Inhibitor

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SAT-356-Anti-metabolic, anti-inflammatory and anti-fibrotic properties of ART-, a novel phosphodiesterase 4 inhibitor as a potential clinical candidate for non-alcoholic steatohepatitis

Journal of Hepatology ◽

10.1016/s0618-8278(19)31586-5 ◽

2019 ◽

Vol 70 (1) ◽

pp. e796

Author(s):

Yuichiro Amano ◽

Shuntarou Tsuchiya ◽

Mitsuharu Matsumoto ◽

Hikaru Ueno ◽

Nobuhiro Nishigaki ◽

...

Keyword(s):

Phosphodiesterase 4 ◽

Alcoholic Steatohepatitis ◽

Anti Inflammatory ◽

Phosphodiesterase 4 Inhibitor ◽

Clinical Candidate

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Phosphodiesterase 4 inhibitor and phosphodiesterase 5 inhibitor combination therapy has antifibrotic and anti-inflammatory effects in mdx mice with Duchenne muscular dystrophy

Proceedings for Annual Meeting of The Japanese Pharmacological Society ◽

10.1254/jpssuppl.93.0_2-o-070 ◽

2020 ◽

Vol 93 (0) ◽

pp. 2-O-070

Author(s):

Yasunori Nio ◽

Masayuki Tanaka ◽

Yoshihiko Hirozane ◽

Yo Muraki ◽

Takanori Matsuo ◽

...

Keyword(s):

Duchenne Muscular Dystrophy ◽

Muscular Dystrophy ◽

Combination Therapy ◽

Mdx Mice ◽

Phosphodiesterase 5 Inhibitor ◽

Phosphodiesterase 4 ◽

Anti Inflammatory ◽

Phosphodiesterase 5 ◽

Phosphodiesterase 4 Inhibitor ◽

Inhibitor Combination

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Phase 3 Studies Treating Children and Adult Patients with Mild to Moderate Atopic Dermatitis with Crisaborole Ointment, a Novel, Nonsteroidal, Topical Anti-inflammatory, Phosphodiesterase 4 Inhibitor

10.1542/peds.141.1_meetingabstract.275 ◽

2018 ◽

Author(s):

Amy S. Paller ◽

Wynnis L. Tom ◽

Mark G. Lebwohl ◽

Mark Boguniewicz ◽

Lawrence F. Eichenfield ◽

...

Keyword(s):

Atopic Dermatitis ◽

Adult Patients ◽

Phase 3 ◽

Phosphodiesterase 4 ◽

Anti Inflammatory ◽

Phosphodiesterase 4 Inhibitor

Download Full-text