NCIt synonyms : 4-Methyl-3-((4-(3-pyridinyl)-2-pyrimidinyl)amino)-N-(5-(4-methyl-1H-imidazol-1-yl)-3-(trifluoromethyl)phenyl)benzamide; AMN107; AMN 107 Base Form;
NCIt 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.;
Alternative definition : NCI-GLOSS: 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.;