Target General Infomation
Target ID
T47941
Former ID
TTDC00170
Target Name
PDE4
Synonyms
PDE4; Phosphodiesterase 4
Target Type
Successful
Disease Atopic dermatitis [ICD9: 691.8, 692.9; ICD10: L00-L99]
Asthma [ICD10: J45]
Asthma; Chronic obstructive pulmonary disease [ICD9: 490-492, 493, 494-496; ICD10: J40-J44, J47, J45]
Cough [ICD9: 786.2; ICD10: R05]
Chronic obstructive pulmonary disease [ICD9: 490-492, 494-496; ICD10: J40-J44, J47]
Emphysema; Bronchitis; Chronic obstructive pulmonary disease [ICD9: 460-519, 466, 490, 490-492, 491, 492, 494-496; ICD10: J00-J99, J20-J21, J40-J44, J42, J43, J47]
Psoriasis [ICD9: 696; ICD10: L40]
Unspecified [ICD code not available]
Function
Hydrolyzes the second messenger cAMP, which is a key regulator of many important physiological processes||Hydrolyzes the second messenger cAMP, which is a key regulator of many important physiological processes. May be involved in mediating central nervous system effects of therapeutic agents ranging from antidepressants to antiasthmatic and anti-inflammatory agents
BioChemical Class
Phosphoric diester hydrolases
Target Validation
T47941
UniProt ID
EC Number
EC 3.1.4.17
Drugs and Mode of Action
Drug(s) Apremilast Drug Info Approved Psoriasis [1], [2]
crisaborole Drug Info Approved Atopic dermatitis [3]
Oxtriphylline Drug Info Approved Cough [4]
Roflumilast Drug Info Approved Asthma [5], [6]
AN2728 Drug Info Phase 3 Atopic dermatitis [7]
Arofylline Drug Info Phase 3 Chronic obstructive pulmonary disease [8]
E6005 Drug Info Phase 2 Atopic dermatitis [9]
IC-485 Drug Info Phase 2 Chronic obstructive pulmonary disease [8]
ONO-6126 Drug Info Phase 2 Chronic obstructive pulmonary disease [8]
Roflumilast Drug Info Withdrawn from market Chronic obstructive pulmonary disease [10], [6]
Capridine-beta Drug Info Discontinued in Phase 4 Psoriasis [11]
Cilomilast Drug Info Discontinued in Phase 3 Emphysema; Bronchitis; Chronic obstructive pulmonary disease [12], [13]
Cilomilast Drug Info Discontinued in Phase 2 Asthma; Chronic obstructive pulmonary disease [12], [13]
GW842470X Drug Info Discontinued in Phase 2 Atopic dermatitis [10]
Roflumilast Drug Info Discontinued in Phase 2 Atopic dermatitis [10], [6]
Inhibitor (R)-Rolipram Drug Info [14], [15]
(S)-Rolipram Drug Info [14], [15]
AN2728 Drug Info [16]
Apremilast Drug Info [1]
Arofylline Drug Info [8]
Capridine-beta Drug Info [17], [18]
Cilomilast Drug Info [8]
E6005 Drug Info [19]
GW842470X Drug Info [10]
IC-485 Drug Info [8]
ONO-6126 Drug Info [8]
Modulator crisaborole Drug Info [3]
CT-5357 Drug Info [20]
Oxtriphylline Drug Info [21]
PDE 4 inhibitor (inflammation) Drug Info [20]
PDE 4 inhibitor (respiratory) Drug Info [20]
PDE4 Drug Info [20]
Roflumilast Drug Info [5]
SDZ-PDI-747 Drug Info [20]
References
REF 1Emerging drugs for psoriasis. Expert Opin Emerg Drugs. 2009 Mar;14(1):145-63.
REF 2(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7372).
REF 32016 FDA drug approvals. Nat Rev Drug Discov. 2017 Feb 2;16(2):73-76. doi: 10.1038/nrd.2017.14.
REF 4FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 086742.
REF 52011 FDA drug approvals. Nat Rev Drug Discov. 2012 Feb 1;11(2):91-4.
REF 6(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6962).
REF 7ClinicalTrials.gov (NCT02118792) Safety and Efficacy of AN2728 Topical Ointment, 2% in Children, Adolescents, and Adults (Aged 2 Years and Older) With Atopic Dermatitis. U.S. National Institutes of Health.
REF 8Emerging drugs for the treatment of chronic obstructive pulmonary disease. Expert Opin Emerg Drugs. 2006 May;11(2):275-91.
REF 9ClinicalTrials.gov (NCT01461941) A Phase 2 Study of E6005 in Patients With Atopic Dermatitis. U.S. National Institutes of Health.
REF 10Emerging drugs for atopic dermatitis. Expert Opin Emerg Drugs. 2009 Mar;14(1):165-79.
REF 112014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81.
REF 12Emerging drugs for asthma. Expert Opin Emerg Drugs. 2008 Dec;13(4):643-53.
REF 13(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7407).
REF 14Phosphodiesterase 4 in osteoblastic osteosarcoma cells as a potential target for growth inhibition. Anticancer Drugs. 2003 Jun;14(5):377-81.
REF 15PDE4 inhibitors roflumilast and rolipram augment PGE2 inhibition of TGF-{beta}1-stimulated fibroblasts. Am J Physiol Lung Cell Mol Physiol. 2009 Jun;296(6):L959-69. Epub 2009 Mar 20.
REF 16AN-2728, a PDE4 inhibitor for the potential topical treatment of psoriasis and atopic dermatitis. Curr Opin Investig Drugs. 2009 Nov;10(11):1236-42.
REF 17CC-10004 . Curr Opin Investig Drugs. 2005 May;6(5):518-25.
REF 18Highly selective phosphodiesterase 4 inhibitors for the treatment of allergic skin diseases and psoriasis. Inflamm Allergy Drug Targets. 2007 Mar;6(1):17-26.
REF 19Antipruritic effect of the topical phosphodiesterase 4 inhibitor E6005 ameliorates skin lesions in a mouse atopic dermatitis model. J Pharmacol Exp Ther. 2013 Jul;346(1):105-12.
REF 20The ChEMBL database in 2017.
REF 21Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.

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