phosphodiesterase 4 inhibitors


Summary: Compounds that specifically inhibit PHOSPHODIESTERASE 4.

Top Publications

  1. Chou A, D Urzo A. New therapy for managing moderate to severe chronic obstructive pulmonary disease. Can Fam Physician. 2014;60:352-4 pubmed
  2. Zou Z, Chen J, Feng H, Cheng Y, Wang H, Zhou Z, et al. Novel Phosphodiesterase 4 Inhibitor FCPR03 Alleviates Lipopolysaccharide-Induced Neuroinflammation by Regulation of the cAMP/PKA/CREB Signaling Pathway and NF-?B Inhibition. J Pharmacol Exp Ther. 2017;362:67-77 pubmed publisher
    ..Our findings suggest that FCPR03 inhibits the neuroinflammatory response through the activation of cAMP/PKA/CREB signaling pathway and NF-?B inhibition. ..
  3. Eichenfield L, Call R, Forsha D, Fowler J, Hebert A, Spellman M, et al. Long-term safety of crisaborole ointment 2% in children and adults with mild to moderate atopic dermatitis. J Am Acad Dermatol. 2017;77:641-649.e5 pubmed publisher
    ..2%). Nine patients (1.7%) discontinued the long-term study because of TEAEs. Long-term efficacy was not analyzed. Crisaborole ointment had a low frequency of treatment-related AEs over 48 weeks of treatment of patients with AD. ..
  4. White W, Cooke G, Kowey P, Calverley P, Bredenbröker D, Goehring U, et al. Cardiovascular safety in patients receiving roflumilast for the treatment of COPD. Chest. 2013;144:758-765 pubmed publisher
    ..Potential cardiovascular benefits of roflumilast should be evaluated in future controlled clinical trials. ..
  5. Ahidjo B, Bishai W. Phosphodiesterase inhibitors as adjunctive therapies for tuberculosis. EBioMedicine. 2016;4:7-8 pubmed publisher
  6. Jarnagin K, Chanda S, Coronado D, Ciaravino V, Zane L, Guttman Yassky E, et al. Crisaborole Topical Ointment, 2%: A Nonsteroidal, Topical, Anti-Inflammatory Phosphodiesterase 4 Inhibitor in Clinical Development for the Treatment of Atopic Dermatitis. J Drugs Dermatol. 2016;15:390-6 pubmed
  7. Kistemaker L, Oenema T, Baarsma H, Bos I, Schmidt M, Facchinetti F, et al. The PDE4 inhibitor CHF-6001 and LAMAs inhibit bronchoconstriction-induced remodeling in lung slices. Am J Physiol Lung Cell Mol Physiol. 2017;313:L507-L515 pubmed publisher
    ..The combination of CHF-6001 and anticholinergics was more effective than the individual compounds. This cooperativity might be explained by the distinct mechanisms of action inhibiting TGF-? release and bronchoconstriction. ..
  8. Hasegawa F, Kawamura K, Tsuchikawa H, Murata M. Stable C-N axial chirality in 1-aryluracil scaffold and differences in in vitro metabolic clearance between atropisomers of PDE4 inhibitor. Bioorg Med Chem. 2017;25:4506-4511 pubmed publisher
    ..This finding demonstrates the potential utility of stable C-N bond atropisomers in the development of chiral drugs. ..
  9. Niccolini F, Wilson H, Pagano G, Coello C, Mehta M, Searle G, et al. Loss of phosphodiesterase 4 in Parkinson disease: Relevance to cognitive deficits. Neurology. 2017;89:586-593 pubmed publisher
    ..Our findings demonstrate loss of PDE4 expression in the striato-thalamo-cortical circuit, which is associated with deficits of spatial working memory in patients with PD. ..

More Information


  1. Long T, Rojo Arreola L, Shi D, El Sakkary N, Jarnagin K, Rock F, et al. Phenotypic, chemical and functional characterization of cyclic nucleotide phosphodiesterase 4 (PDE4) as a potential anthelmintic drug target. PLoS Negl Trop Dis. 2017;11:e0005680 pubmed publisher
    ..Transgenic C. elegans is highlighted as a potential screening tool to optimize small molecule chemistries to flatworm molecular drug targets. ..
  2. Çifci G, Aviyente V, Akten E, Monard G. Assessing protein-ligand binding modes with computational tools: the case of PDE4B. J Comput Aided Mol Des. 2017;31:563-575 pubmed publisher
  3. Albrecht W, Unger A, Bauer S, Laufer S. Discovery of N-{4-[5-(4-Fluorophenyl)-3-methyl-2-methylsulfanyl-3H-imidazol-4-yl]-pyridin-2-yl}-acetamide (CBS-3595), a Dual p38? MAPK/PDE-4 Inhibitor with Activity against TNF?-Related Diseases. J Med Chem. 2017;60:5290-5305 pubmed publisher
  4. Eichenfield L, Stein Gold L. Addressing the immunopathogenesis of atopic dermatitis: advances in topical and systemic treatment. Semin Cutan Med Surg. 2017;36:S45-S48 pubmed publisher
    ..The phase III clinical trial results of the systemic medication dupilumab, an inhibitor of the IL-4 receptor ? subunit (which inhibits both IL-4 and IL-13 signaling), are currently being reviewed by the FDA. ..
  5. Lima K, Vago J, Caux T, Negreiros Lima G, Sugimoto M, Tavares L, et al. The resolution of acute inflammation induced by cyclic AMP is dependent on annexin A1. J Biol Chem. 2017;292:13758-13773 pubmed publisher
    ..Our results show that AnxA1 is at least one of the endogenous determinants mediating the pro-resolving properties of cAMP-elevating agents and cAMP-mimetic drugs. ..