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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)
3-Cyclopropylmethoxy-N-(3,5-dichloropyridin-4-yl)-4-(difluoromethoxy)benzamide
B9302-107
BY217
BYK20869
Daliresp
Roflumilast
ROFLUMILAST

External Source Codes: 
CAS Registry Number 162401-32-3 (see NLM ChemIDplus info)
FDA UNII Code 0P6C6ZOP5U
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  

URL: https://ncit.nci.nih.gov/ncitbrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&code=C76890

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