title: A Phase I study to assess the safety, pharmacokinetics and efficacy of barasertib (AZD1152), an Aurora B kinase inhibitor, in Japanese patients with advanced acute myeloid leukemia.
abstract: Barasertib (AZD1152) is a highly potent and selective Aurora B kinase inhibitor. The safety, efficacy and pharmacokinetic (PK) profile of barasertib were investigated in Japanese patients with advanced acute myeloid leukemia. Barasertib (50-1200mg) was administered as a continuous 7-day intravenous infusion every 21 days. No dose-limiting toxicities were reported and barasertib 1200mg was chosen for further evaluation in Japanese patients. Neutropenia and febrile neutropenia were the most commonly reported adverse events. The PK profile was similar to Western patients. A promising overall hematologic response rate of 19% was achieved, which warrants further investigation in these patients.
authors.affiliation: Tokai University Hospital, Isehara, Japan. 0ammd006@is.icc.u-tokai.ac.jp
authors.forename: Kosuke
authors.initials: K
authors.lastname: Tsuboi
authors.forename: Toshiya
authors.initials: T
authors.lastname: Yokozawa
authors.forename: Toru
authors.initials: T
authors.lastname: Sakura
authors.forename: Takashi
authors.initials: T
authors.lastname: Watanabe
authors.forename: Shin
authors.initials: S
authors.lastname: Fujisawa
authors.forename: Takahiro
authors.initials: T
authors.lastname: Yamauchi
authors.forename: Naokuni
authors.initials: N
authors.lastname: Uike
authors.forename: Kiyoshi
authors.initials: K
authors.lastname: Ando
authors.forename: Rika
authors.initials: R
authors.lastname: Kihara
authors.forename: Kensei
authors.initials: K
authors.lastname: Tobinai
authors.forename: Hiroya
authors.initials: H
authors.lastname: Asou
authors.forename: Tomomitsu
authors.initials: T
authors.lastname: Hotta
authors.forename: Shuichi
authors.initials: S
authors.lastname: Miyawaki
mesh_terms: D000328:Adult; D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000009:adverse effects / Q000493:pharmacokinetics*; D044466:Asian People; D064107:Aurora Kinase B; D064127:Aurora Kinases; D004305:Dose-Response Relationship, Drug; D004334:Drug Administration Schedule; D064420:Drug-Related Side Effects and Adverse Reactions; D004791:Enzyme Inhibitors / Q000008:administration & dosage / Q000009:adverse effects / Q000493:pharmacokinetics*; D005260:Female; D006801:Humans; D015470:Leukemia, Myeloid, Acute / Q000188:drug therapy / Q000473:pathology; D007958:Leukocyte Count; D008297:Male; D008875:Middle Aged; D009503:Neutropenia / Q000473:pathology; D010755:Organophosphates / Q000008:administration & dosage / Q000009:adverse effects / Q000493:pharmacokinetics*; D017346:Protein Serine-Threonine Kinases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D011799:Quinazolines / Q000008:administration & dosage / Q000009:adverse effects / Q000493:pharmacokinetics*; D016896:Treatment Outcome
chemical_list: C520647:2-((3-((4-((5-(2-((3-fluorophenyl)amino)-2-oxoethyl)-1H-pyrazol-3-yl)amino)quinazolin-7-yl)oxy)propyl)(ethyl)amino)ethyl dihydrogen phosphate; D000970:Antineoplastic Agents; D004791:Enzyme Inhibitors; D010755:Organophosphates; D011799:Quinazolines; C576921:AURKB protein, human; D064107:Aurora Kinase B; D064127:Aurora Kinases; D017346:Protein Serine-Threonine Kinases