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单词 nilotinib
释义
nilotinib
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. Check foractive clinical trials using this agent. or A substance being studied in the treatment of some types of cancer. Nimotuzumab binds to a protein called epidermal growth factor receptor (EGFR), which is found on some normal cells and some types of cancer cells. Blocking this protein may help keep cancer cells from growing. Nimotuzumab is a type of monoclonal antibody. Also called Theraloc.
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