… Nilotinib was tested alongside imatinib and the Bcr-Abl/Src inhibitor dasatinib in 16 Bcl-Abl …
In vivo, the efficacy of nilotinib has been documented in Bcr-Abl + imatinib-sensitive and -…

… BCR–ABL between that of dasatinib and nilotinib, and inhibited only SFKs LCK and LYN
among SFKs. Both nilotinib … dasatinib-resistant T315A, F317L and F317V BCR–ABL mutations. …

… , nilotinib was 30 times more potent than imatinib in imatinib-sensitive CML cell lines, and
maintained activity in 32 of 33 imatinib-resistant BCR-ABL … in patients with imatinib-resistant …

… Two such agents are dasatinib and nilotinib. Whereas, like imatinib, x-ray analysis of crystal
structures of nilotinib in complex with the Abl kinase domain reveal that this agent binds to …

… Thirty-five different baseline mutations affecting 27 amino acid residues within the BCR-ABL
kinase domain were identified among the imatinib-resistant patients in this analysis. These …

… comparing nilotinib to the prototype kinase inhibitor imatinib, … Nilotinib was discovered following
re-engineering of imatinib, … potency and selectivity towards BCR-ABL1. Through evolving …

… Nilotinib Efficacy and Safety in Clinical Trials–Newly Diagnosed Pts) trial, nilotinib demonstrated
superior efficacy vs imatinib in … and BCR-ABL mutation status in pts from ENESTnd. …

… An optimal response is defined as a BCR-ABL 1 transcript … , and mutations in the BCR-ABL
kinase domain should also be … –response relationships of imatinib, nilotinib, and dasatinib …

… fit in the ABL kinase pocket [6, 7, 9]. … to imatinib and, unlike imatinib and nilotinib, binds
BCR-ABL in the active conformation [10, 11]. Bosutinib binds to an intermediate form of BCR-ABL […

… BCR-ABL and a more potent inhibitor than imatinib in vitro. Based on data from the Evaluating
Nilotinib … 3 trial in which nilotinib demonstrated superiority over imatinib, nilotinib has been …