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Version: 17.06d (Release date: 2017-06-26)
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Roflumilast (Code C76890)

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Terms & Properties

Preferred Name: Roflumilast

Definition: An orally available, long-acting inhibitor of phosphodiesterase (PDE) type 4 (PDE4), with anti-inflammatory and potential antineoplastic activities. Upon administration, roflumilast and its active metabolite roflumilast N-oxide selectively and competitively bind to and inhibit PDE4, which leads to an increase of both intracellular levels of cyclic-3',5'-adenosine monophosphate (cAMP) and cAMP-mediated signaling. cAMP prevents phosphorylation of spleen tyrosine kinase (SYK) and abrogates activation of the PI3K/AKT/mTOR signaling pathway, which may result in the induction of apoptosis. PDE4, a member of the PDE superfamily that hydrolyses cAMP and 3',5'-cyclic guanosine monophosphate (cGMP) to their inactive 5' monophosphates, is upregulated in a variety of cancers and may contribute to chemoresistance; it also plays a key role in inflammation, especially in inflammatory airway diseases.

Display Name: Roflumilast

Label: Roflumilast

NCI Thesaurus Code: C76890 (Search for linked caDSR metadata)  (search value sets)

NCI Metathesaurus Link: C0965618  (see NCI Metathesaurus info)

Synonyms & Abbreviations: (see Synonym Details)

External Source Codes: 
CAS Registry Number 162401-32-3 (see NLM ChemIDplus info)
PDQ Closed Trial Search ID 750521
PDQ Open Trial Search ID 750521 (check for NCI PDQ open clinical trial info)
UMLS CUI C0965618

Other Properties:
     Name Value (qualifiers indented underneath)
Accepted_Therapeutic_Use_For Chronic Obstructive Pulmonary Disease (COPD)
Chemical_Formula C17H14Cl2F2N2O3
code C76890
Contributing_Source CTRP
Contributing_Source FDA
Legacy_Concept_Name Roflumilast
Semantic_Type Pharmacologic Substance

Additional Concept Data: 
Defined Fully by Roles: No  


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