loading...| Preferred Name |
Roflumilast |
|
| Synonyms |
|
|
| Definitions |
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. |
|
| ID |
http://purl.obolibrary.org/obo/NCIT_C76890 |
|
| Accepted_Therapeutic_Use_For |
Chronic Obstructive Pulmonary Disease (COPD) |
|
| CAS_Registry |
162401-32-3 |
|
| Chemical_Formula |
C17H14Cl2F2N2O3 |
|
| code |
C76890 |
|
| Contributing_Source |
CTRP FDA |
|
| 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 |
|
| FDA_UNII_Code |
0P6C6ZOP5U |
|
| Has_Target | ||
| in_subset |
http://purl.obolibrary.org/obo/NCIT_C63923 http://purl.obolibrary.org/obo/NCIT_C177537 http://purl.obolibrary.org/obo/NCIT_C116977 http://purl.obolibrary.org/obo/NCIT_C116978 http://purl.obolibrary.org/obo/NCIT_C128784 |
|
| Is_Value_For_GDC_Property | ||
| label |
Roflumilast |
|
| Legacy Concept Name |
Roflumilast |
|
| Maps_To |
Roflumilast |
|
| NCI_Drug_Dictionary_ID |
750521 |
|
| PDQ_Closed_Trial_Search_ID |
750521 |
|
| PDQ_Open_Trial_Search_ID |
750521 |
|
| Preferred_Name |
Roflumilast |
|
| prefixIRI |
NCIT:C76890 |
|
| prefLabel |
Roflumilast |
|
| Semantic_Type |
Pharmacologic Substance |
|
| UMLS_CUI |
C0965618 |
|
| subClassOf |