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Version: 17.06d (Release date: 2017-06-26)
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Delanzomib (Code C74075)

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Terms & Properties

Preferred Name: Delanzomib

Definition: An orally bioavailable synthetic P2 threonine boronic acid inhibitor of the chymotrypsin-like activity of the proteasome, with potential antineoplastic activity. Delanzomib represses the proteasomal degradation of a variety of proteins, including inhibitory kappaBalpha (IkappaBalpha), resulting in the cytoplasmic sequestration of the transcription factor NF-kappaB; inhibition of NF-kappaB nuclear translocation and transcriptional up-regulation of a variety of cell growth-promoting factors; and apoptotic cell death in susceptible tumor cell populations. In vitro studies indicate that this agent exhibits a favorable cytotoxicity profile toward normal human epithelial cells, bone marrow progenitors, and bone marrow-derived stromal cells relative to the proteasome inhibitor bortezomib. The intracellular protein IkappaBalpha functions as a primary inhibitor of the proinflammatory transcription factor NF-kappaB.

Display Name: Delanzomib

Label: Delanzomib

NCI Thesaurus Code: C74075 (Search for linked caDSR metadata)  (search value sets)

NCI Metathesaurus Link: C3467895  (see NCI Metathesaurus info)

Synonyms & Abbreviations: (see Synonym Details)
((1R)-1-((2S,3R)-3-hydroxy-2-(6-phenylpyridine-2-carboxamido)butanamido)-3-methylbutyl)boronic Acid
CEP 18770
Proteasome Inhibitor CEP 18770

External Source Codes: 
CAS Registry Number 847499-27-8 (see NLM ChemIDplus info)
FDA UNII Code 6IF28942WO
PDQ Closed Trial Search ID 583540
PDQ Open Trial Search ID 583540 (check for NCI PDQ open clinical trial info)
UMLS CUI C3467895

Other Properties:
     Name Value (qualifiers indented underneath)
Chemical_Formula C21H28BN3O5
code C74075
Contributing_Source CTRP
Contributing_Source FDA
Legacy_Concept_Name Proteasome_Inhibitor_CEP_18770
Semantic_Type Pharmacologic Substance

Additional Concept Data: 
Defined Fully by Roles: No  


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