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Version: 17.08d (Release date: 2017-08-28)
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Neratinib (Code C49094)

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Terms & Properties

Preferred Name: Neratinib

Definition: An orally available, 6,7-disubstituted-4-anilinoquinoline-3-carbonitrile irreversible inhibitor of the HER-2 receptor tyrosine kinase with potential antineoplastic activity. Neratinib binds to the HER-2 receptor irreversibly, thereby reducing autophosphorylation in cells, apparently by targeting a cysteine residue in the ATP-binding pocket of the receptor. Treatment of cells with this agent results in inhibition of downstream signal transduction events and cell cycle regulatory pathways; arrest at the G1-S (Gap 1/DNA synthesis)-phase transition of the cell division cycle; and ultimately decreased cellular proliferation. Neratinib also inhibits the epidermal growth factor receptor (EGFR) kinase and the proliferation of EGFR-dependent cells.

Display Name: Neratinib

Label: Neratinib

NCI Thesaurus Code: C49094 (Search for linked caDSR metadata)  (search value sets)

NCI Metathesaurus Link: C1704439  (see NCI Metathesaurus info)

Synonyms & Abbreviations: (see Synonym Details)
2-Butenamide, N-(4-((3-chloro-4-(2-pyridinylmethoxy)phenyl)amino)-3-cyano-7-ethoxy-6-quinolinyl)-4-(dimethylamino)-, (2E)-
HKI 272
PB 272

External Source Codes: 
CAS Registry Number 698387-09-6 (see NLM ChemIDplus info)
ChEBI ID CHEBI:61397 (see ChEBI info)
PDQ Closed Trial Search ID 453548
PDQ Open Trial Search ID 453548 (check for NCI PDQ open clinical trial info)
UMLS CUI C1704439

Other Properties:
     Name Value (qualifiers indented underneath)
Accepted_Therapeutic_Use_For early stage HER2-overexpressed/amplified breast cancer
Chemical_Formula C30H29ClN6O3
code C49094
Contributing_Source CTRP
Contributing_Source FDA
Legacy_Concept_Name KI-272
Semantic_Type Pharmacologic Substance

Additional Concept Data: 
Defined Fully by Roles: No  


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