title: BMS-354825: a novel drug with potential for the treatment of imatinib-resistant chronic myeloid leukaemia.
abstract: The BCR-ABL tyrosine kinase inhibitor imatinib has greatly improved the outcome for patients with chronic myeloid leukaemia (CML). Unfortunately, mutations causing resistance to imatinib are leading to relapses in some patients. In addition to inhibiting the wild-type BCR-ABL, BMS-354825 inhibited 14 of 15 BCR-ABL mutants. BMS-354825 treatment of immunodeficient mice prevented the progression of the disease in mice treated with the most clinical common imatinib-resistant mutant Met351Thr. The safety and efficacy of BMS-354825 is presently being evaluated in a phase I/II clinical trial in CML patients with imatinib resistance. The frequency of clinical use of BMS-3548125 in CML patients will depend on its efficacy/safety profile in clinical trial.
authors.affiliation: Doggrell Biomedical Communications, 47 Caronia Crescent, Lynfield, Auckland, New Zealand. s_doggrell@yahoo.com
authors.forename: Sheila A
authors.initials: SA
authors.lastname: Doggrell
mesh_terms: D000818:Animals; D001549:Benzamides; D000069439:Dasatinib; D019008:Drug Resistance, Neoplasm / Q000502:physiology; D015507:Drugs, Investigational / Q000737:chemistry / Q000627:therapeutic use*; D006801:Humans; D000068877:Imatinib Mesylate; D015464:Leukemia, Myelogenous, Chronic, BCR-ABL Positive / Q000097:blood / Q000188:drug therapy*; D051379:Mice; D010879:Piperazines / Q000737:chemistry / Q000627:therapeutic use*; D011743:Pyrimidines / Q000737:chemistry / Q000627:therapeutic use*; D013844:Thiazoles / Q000737:chemistry / Q000627:therapeutic use*
chemical_list: D001549:Benzamides; D015507:Drugs, Investigational; D010879:Piperazines; D011743:Pyrimidines; D013844:Thiazoles; D000068877:Imatinib Mesylate; D000069439:Dasatinib