Nilotinib.
Therapy with imatinib mesylate is a standard of care for most patients with Philadelphia chromosome-positive chronic myeloid leukemia (CML). However, resistance or intolerance to imatinib develops in a considerable number of patients leading to relapse or discontinuation of treatment. Nilotinib is a rationally designed second-generation tyrosine kinase inhibitor (TKI) with improved affinity and specificity against the BCR-ABL kinase, when compared with imatinib. Considerable efficacy after imatinib failure has been demonstrated in clinical trials leading to nilotinib's current approval as second-line therapy for CML in chronic and accelerated phase (AP). The role of nilotinib as first-line treatment for CML, in combinatorial strategies and in the context of specific BCR-ABL mutations, requires future studies.
Quintás-Cardama
Alfonso
A
Medizinische Klinik m.S Hämatologie und Onkologie, Charité-Universitätsmedizin Berlin, Germany. Philipp.lecoutre@charite.de
Kim
Theo Daniel
TD
Cataldo
Vince
V
le Coutre
Philipp
P
D000818:Animals; D000970:Antineoplastic Agents / Q000627:therapeutic use*; D002986:Clinical Trials as Topic; D019008:Drug Resistance, Neoplasm; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy*; D011743:Pyrimidines / Q000009:adverse effects / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use*
D000970:Antineoplastic Agents; D011743:Pyrimidines; C498826:nilotinib