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AttributesValues
rdf:type
rdfs:label
  • Nilotinib
rdfs:subClassOf
Has_Salt_Form
Concept_In_Subset
Semantic_Type
  • Pharmacologic Substance
Preferred_Name
  • Nilotinib
UMLS_CUI
  • C1721377
CAS_Registry
  • 641571-10-0
Accepted_Therapeutic_Use_For
  • Chronic myeloid leukemia; Philadelphia chromosome-positive acute lymphoblastic leukemia
FDA_UNII_Code
  • F41401512X
Contributing_Source
  • FDA
ALT_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.NCI-GLOSS
PDQ_Open_Trial_Search_ID
  • 435988
PDQ_Closed_Trial_Search_ID
  • 435988
Chemical_Formula
  • C28H22F3N7O
Legacy_Concept_Name
  • AMN107
CHEBI_ID
  • CHEBI:52172
FULL_SYN
  • 4-Methyl-3-((4-(3-pyridinyl)-2-pyrimidinyl)amino)-N-(5-(4-methyl-1H-imidazol-1-yl)-3-(trifluoromethyl)phenyl)benzamideSNNCI
  • NILOTINIBPTFDAF41401512X
  • TasignaPTNCI-GLOSSCDR0000581140
  • AMN 107CNNCI
  • TasignaBRNCI
  • NilotinibPTNCI
  • nilotinibPTNCI-GLOSSCDR0000575396
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
code
  • C48375
sameAs
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