title: Bosutinib: a third generation tyrosine kinase inhibitor for the treatment of chronic myeloid leukemia.
abstract: Bosutinib is an oral tyrosine kinase inhibitor (TKI) with very potent dual inhibitory activity against SRC and abelson gene. Bosutinib was approved in 2012 for the treatment of resistant Philadelphia chromosome positive chronic myeloid leukemia (CML). Bosutinib is a very effective TKI against all phases of intolerant or resistant CML regardless of the presence or absence of an abelson gene domain mutation, except for cases with detectable T315I or V299L. Bosutinib is overall well tolerated and associated with a unique, but manageable toxicity profile. Factors that influence the prescribing pattern of this drug are complex and include physicians', and increasingly patients and families' preference, patients' comorbid conditions, schedule of administration, as well as financial factors. This paper provides an overview of CML, the TKI market, pharmacokinetics, pharmacodynamics, clinical efficacy, safety and tolerability of bosutinib.
authors.affiliation: Department of Hematology and Medical Oncology, Division of Hematology, Winship Cancer Institute of Emory University, 1365 Clifton Road, Room C1152, Atlanta, GA 30322, USA.
authors.forename: Brittany G
authors.initials: BG
authors.lastname: Hill
authors.forename: Vamsi K
authors.initials: VK
authors.lastname: Kota
authors.forename: Hanna Jean
authors.initials: HJ
authors.lastname: Khoury
mesh_terms: D000814:Aniline Compounds / Q000009:adverse effects / Q000493:pharmacokinetics / Q000494:pharmacology* / Q000627:therapeutic use*; D017277:Drug Approval; D006801:Humans; D015464:Leukemia, Myelogenous, Chronic, BCR-ABL Positive / Q000188:drug therapy*; D058990:Molecular Targeted Therapy; D009570:Nitriles / Q000009:adverse effects / Q000493:pharmacokinetics / Q000494:pharmacology* / Q000627:therapeutic use*; D047428:Protein Kinase Inhibitors / Q000009:adverse effects / Q000494:pharmacology / Q000627:therapeutic use*; D016315:Proto-Oncogene Proteins c-abl / Q000235:genetics; D011804:Quinolines / Q000009:adverse effects / Q000493:pharmacokinetics / Q000494:pharmacology* / Q000627:therapeutic use*; D014481:United States; D014486:United States Food and Drug Administration
chemical_list: D000814:Aniline Compounds; D009570:Nitriles; D047428:Protein Kinase Inhibitors; D011804:Quinolines; C471992:bosutinib; D016315:Proto-Oncogene Proteins c-abl
keywords: bosutinib; chronic myeloid leukemia; resistant; tyrosine kinase inhibitor