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Version: 16.11d (Release date: 2016-11-28)
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Nilotinib (Code C48375)

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Terms & Properties

Preferred Name: Nilotinib

Definition: An orally bioavailable aminopyrimidine-derivative Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity. Designed to overcome imatinib resistance, nilotinib binds to and stabilizes the inactive conformation of the kinase domain of the Abl protein of the Bcr-Abl fusion protein, resulting in the inhibition of the Bcr-Abl-mediated proliferation of Philadelphia chromosome-positive (Ph+) chronic myeloid leukemia (CML) cells. This agent also inhibits the receptor tyrosine kinases platelet-derived growth factor receptor (PDGF-R) and c-kit, a receptor tyrosine kinase mutated and constitutively activated in most gastrointestinal stromal tumors (GISTs). With a binding mode that is energetically more favorable than that of imatinib, nilotinib has been shown to have an approximately 20-fold increased potency in kinase and proliferation assays compared to imatinib.

NCI-GLOSS Definition: A drug used to treat certain types of chronic myelogenous leukemia (CML). It is used in patients who have not gotten better after treatment with other anticancer drugs or who are not able to take imatinib mesylate. It is also being studied in the treatment of other types of cancer. Nilotinib blocks a protein called BCR/ABL which is made in CML cells that contain the Philadelphia chromosome (an abnormal chromosome 22 that has part of chromosome 9 attached). It is a type of tyrosine kinase inhibitor.

Display Name: Nilotinib

Label: Nilotinib

NCI Thesaurus Code: C48375 (Search for linked caDSR metadata)  (search value sets)

NCI Metathesaurus Link: C1721377  (see NCI Metathesaurus info)

Synonyms & Abbreviations: (see Synonym Details)
4-Methyl-3-((4-(3-pyridinyl)-2-pyrimidinyl)amino)-N-(5-(4-methyl-1H-imidazol-1-yl)-3-(trifluoromethyl)phenyl)benzamide
AMN 107
Nilotinib
NILOTINIB
nilotinib
Tasigna

External Source Codes: 
CAS Registry Number 641571-10-0 (see NLM ChemIDplus info)
FDA UNII Code F41401512X
ChEBI ID CHEBI:52172 (see ChEBI info)
PDQ Closed Trial Search ID 435988
PDQ Open Trial Search ID 435988 (check for NCI PDQ open clinical trial info)
UMLS CUI C1721377

Other Properties:
Name Value (qualifiers indented underneath)
Accepted_Therapeutic_Use_For Chronic myeloid leukemia; Philadelphia chromosome-positive acute lymphoblastic leukemia
Chemical_Formula C28H22F3N7O
code C48375
Contributing_Source CTRP
Contributing_Source FDA
Legacy_Concept_Name AMN107
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=C48375

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