Nilotinib Product Description
Nilotinib is a selective, oral inhibitor of tyrosine kinase with IC50 values of 20, 42, 31, 38, 29 and 41 nM for the autophosphorylation of native BCR-ABL (WT p210) and mutant BCR-ABL (E281K, E292K, F317L, M351T and F486S), respectively.
Nilotinib is an anti-cancer medication that is used to treat some types of leukemia, specifically Philadelphia chromosome positive chronic myeloid leukemia (Ph + CML). This medication is called a kinase inhibitor, which means that it works to halt the growth and spread of cancer cells. Nilotinib accomplishes this by inhibiting an abnormal protein that is responsible for instructing cancer cells to multiply. With this particular type of cancer, the body manufactures a great deal of abnormal white blood cells. Nilotinib is only prescribed after other cancer treatments, such as imatinib, have been tried and have not been sufficient.
Nilotinib (AMN107, trade name Tasigna), in the form of the hydrochloride monohydrate salt, is a small-molecule tyrosine kinase inhibitor approved for the treatment of imatinib-resistant chronic myelogenous leukemia. Structurally related to imatinib, it was developed based on the structure of the Abl-imatinib complex to address imatinib intolerance and resistance. Nilotinib is a selective Bcr-Abl kinase inhibitor that is 10-30 fold more potent than imatinib in inhibiting Bcr-Abl tyrosine kinase activity and proliferation of Bcr-Abl expressing cells.
