TY - JOUR
T1 - AMN107
T2 - Tightening the grip of imatinib
AU - O'Hare, Thomas
AU - Walters, Denise K.
AU - Deininger, Michael W.N.
AU - Druker, Brian J.
N1 - Funding Information:
B.J.D. is supported by grants from the National Cancer Institute, The Leukemia and Lymphoma Society, and the Burroughs Wellcome Foundation, and by the Howard Hughes Medical Institute. M.W.D. is a Junior Faculty Scholar of the American Society of Hematology. We thank Eric Stoffregen for critical review of the manuscript.
PY - 2005/2
Y1 - 2005/2
N2 - The Abl inhibitor imatinib is a highly effective therapy for patients with chronic myeloid leukemia. Relapses are relatively uncommon in newly diagnosed patients, but are the rule in patients with more advanced disease. Mutations in the BCR-ABL gene are the most common cause of relapse. Working from the imatinib chemical structure, a higher-affinity family member, AMN107, was designed. AMN107 is approximately 20-fold more potent than imatinib, and this translates into improved inhibitory activity against most of the common BCR-ABL mutations. The implications of these results, and the potential role this and other novel ABL inhibitors may have in treating patients with CML, are discussed.
AB - The Abl inhibitor imatinib is a highly effective therapy for patients with chronic myeloid leukemia. Relapses are relatively uncommon in newly diagnosed patients, but are the rule in patients with more advanced disease. Mutations in the BCR-ABL gene are the most common cause of relapse. Working from the imatinib chemical structure, a higher-affinity family member, AMN107, was designed. AMN107 is approximately 20-fold more potent than imatinib, and this translates into improved inhibitory activity against most of the common BCR-ABL mutations. The implications of these results, and the potential role this and other novel ABL inhibitors may have in treating patients with CML, are discussed.
UR - http://www.scopus.com/inward/record.url?scp=13844251983&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=13844251983&partnerID=8YFLogxK
U2 - 10.1016/j.ccr.2005.01.020
DO - 10.1016/j.ccr.2005.01.020
M3 - Short survey
C2 - 15710324
AN - SCOPUS:13844251983
SN - 1535-6108
VL - 7
SP - 117
EP - 119
JO - Cancer Cell
JF - Cancer Cell
IS - 2
ER -