Pharmacologic Substance
nilotinib
Brand Names:
Tasigna
Effect:
Cellular Proliferation Alteration
May Treat:
Leukemia, Myeloid, Accelerated Phase;
Leukemia, Myeloid, Chronic-Phase
More Information:
Definitions related to nilotinib:
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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 Dictionary of Cancer TermsU.S. National Cancer Institute, 2021
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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 ThesaurusU.S. National Cancer Institute, 2021
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