Aurora Kinase Inhibitors: Current Status and Outlook

A phase I study of danusertib (PHA-739358) in adult patients with accelerated or blastic phase chronic myeloid leukemia and Philadelphia chromosome-positive acute lymphoblastic leukemia resistant or intolerant to imatinib and/or other second generation c-ABL therapy

(2015) G. Borthakur et al.   HAEMATOLOGICA

Aurora Kinase Inhibition: A New Light in the Sky?

(2015) Spiros Linardopoulos et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of N-(4-(3-(2-Aminopyrimidin-4-yl)pyridin-2-yloxy)phenyl)-4-(4-methylthiophen-2-yl)phthalazin-1-amine (AMG 900), A Highly Selective, Orally Bioavailable Inhibitor of Aurora Kinases with Activity against Multidrug-Resistant Cancer Cell Lines

(2015) Stephanie Geuns-Meyer et al.   JOURNAL OF MEDICINAL CHEMISTRY

MLN8054 and Alisertib (MLN8237): Discovery of Selective Oral Aurora A Inhibitors

(2015) Todd B. Sells et al.   ACS Medicinal Chemistry Letters

A phase I study of danusertib (PHA-739358) in adult patients with accelerated or blastic phase chronic myeloid leukemia and Philadelphia chromosome-positive acute lymphoblastic leukemia resistant or intolerant to imatinib and/or other second generation c-ABL therapy

(2015) G. Borthakur et al.   HAEMATOLOGICA

Efficacy and safety of biweekly i.v. administrations of the Aurora kinase inhibitor danusertib hydrochloride in independent cohorts of patients with advanced or metastatic breast, ovarian, colorectal, pancreatic, small-cell and non-small-cell lung cancer: a multi-tumour, multi-institutional phase II study

(2014) P. Schoffski et al.   ANNALS OF ONCOLOGY

Drugging MYCN through an Allosteric Transition in Aurora Kinase A

(2014) William Clay Gustafson et al.   CANCER CELL

The selective Aurora-A kinase inhibitor MLN8237 (alisertib) potently inhibits proliferation of glioblastoma neurosphere tumor stem-like cells and potentiates the effects of temozolomide and ionizing radiation

(2014) Xin Hong et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

A Phase I Trial of AT9283 (a Selective Inhibitor of Aurora Kinases) in Children and Adolescents with Solid Tumors: A Cancer Research UK Study

(2014) L. Moreno et al.   CLINICAL CANCER RESEARCH

Stage I of a phase 2 study assessing the efficacy, safety, and tolerability of barasertib (AZD1152) versus low-dose cytosine arabinoside in elderly patients with acute myeloid leukemia

(2013) Hagop M. Kantarjian et al.   CANCER

Phase I Study Assessing the Safety and Tolerability of Barasertib (AZD1152) With Low-Dose Cytosine Arabinoside in Elderly Patients With AML

(2013) Hagop M. Kantarjian et al.   Clinical Lymphoma Myeloma & Leukemia

A Phase I and Pharmacodynamic Study of AT9283, a Small-Molecule Inhibitor of Aurora Kinases in Patients With Relapsed/Refractory Leukemia or Myelofibrosis

(2013) James Foran et al.   Clinical Lymphoma Myeloma & Leukemia

NCIC CTG IND.181: Phase I study of AT9283 given as a weekly 24 hour infusion in advanced malignancies

(2013) S. F. Dent et al.   INVESTIGATIONAL NEW DRUGS

Phase I study of MLN8237—investigational Aurora A kinase inhibitor—in relapsed/refractory multiple myeloma, Non-Hodgkin lymphoma and chronic lymphocytic leukemia

(2013) Kevin R. Kelly et al.   INVESTIGATIONAL NEW DRUGS

Phase II Study of Alisertib, a Selective Aurora A Kinase Inhibitor, in Relapsed and Refractory Aggressive B- and T-Cell Non-Hodgkin Lymphomas

(2013) Jonathan W. Friedberg et al.   JOURNAL OF CLINICAL ONCOLOGY

AMG 900, a Small-Molecule Inhibitor of Aurora Kinases, Potentiates the Activity of Microtubule-Targeting Agents in Human Metastatic Breast Cancer Models

(2013) Tammy L. Bush et al.   MOLECULAR CANCER THERAPEUTICS

Randomized phase II study of danusertib in patients with metastatic castration-resistant prostate cancer after docetaxel failure

(2012) Hielke J. Meulenbeld et al.   BJU INTERNATIONAL

Phase I study of the Aurora B kinase inhibitor barasertib (AZD1152) to assess the pharmacokinetics, metabolism and excretion in patients with acute myeloid leukemia

(2012) Mike Dennis et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

Pediatric Phase I Trial and Pharmacokinetic Study of MLN8237, an Investigational Oral Selective Small-Molecule Inhibitor of Aurora Kinase A: A Children's Oncology Group Phase I Consortium Study

(2012) Y. P. Mosse et al.   CLINICAL CANCER RESEARCH

Phase I Pharmacokinetic/Pharmacodynamic Study of MLN8237, an Investigational, Oral, Selective Aurora A Kinase Inhibitor, in Patients with Advanced Solid Tumors

(2012) A. Cervantes et al.   CLINICAL CANCER RESEARCH

Phase I Study of Aurora A Kinase Inhibitor MLN8237 in Advanced Solid Tumors: Safety, Pharmacokinetics, Pharmacodynamics, and Bioavailability of Two Oral Formulations

(2012) E. C. Dees et al.   CLINICAL CANCER RESEARCH

Phase II study of MLN8237 (alisertib), an investigational Aurora A kinase inhibitor, in patients with platinum-resistant or -refractory epithelial ovarian, fallopian tube, or primary peritoneal carcinoma

(2012) Ursula A. Matulonis et al.   GYNECOLOGIC ONCOLOGY

Targeting Aurora A kinase activity with the investigational agent alisertib increases the efficacy of cytarabine through a FOXO-dependent mechanism

(2012) Kevin R. Kelly et al.   INTERNATIONAL JOURNAL OF CANCER

Phase I study of barasertib (AZD1152), a selective inhibitor of Aurora B kinase, in patients with advanced solid tumors

(2012) Gary K. Schwartz et al.   INVESTIGATIONAL NEW DRUGS

Optimization of Imidazo[4,5-b]pyridine-Based Kinase Inhibitors: Identification of a Dual FLT3/Aurora Kinase Inhibitor as an Orally Bioavailable Preclinical Development Candidate for the Treatment of Acute Myeloid Leukemia

(2012) Vassilios Bavetsias et al.   JOURNAL OF MEDICINAL CHEMISTRY

Selective FLT3 inhibition of FLT3-ITD+ acute myeloid leukaemia resulting in secondary D835Y mutation: a model for emerging clinical resistance patterns

(2012) A S Moore et al.   LEUKEMIA

The chromosomal passenger complex (CPC): from easy rider to the godfather of mitosis

(2012) Mar Carmena et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

A phase I dose escalation study of AT9283, a small molecule inhibitor of aurora kinases, in patients with advanced solid malignancies

(2011) H.- T. Arkenau et al.   ANNALS OF ONCOLOGY

Phase 1/2 study to assess the safety, efficacy, and pharmacokinetics of barasertib (AZD1152) in patients with advanced acute myeloid leukemia

(2011) B. Lowenberg et al.   BLOOD

Efficacy and pharmacokinetic/pharmacodynamic evaluation of the Aurora kinase A inhibitor MLN8237 against preclinical models of pediatric cancer

(2011) Hernan Carol et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

Aurora B kinase inhibition in mitosis: Strategies for optimizing the use of Aurora kinase inhibitors such as AT9283

(2011) Jayne Curry et al.   CELL CYCLE

The Aurora B kinase inhibitor AZD1152 sensitizes cancer cells to fractionated irradiation and induces mitotic catastrophe

(2011) Yungan Tao et al.   CELL CYCLE

Characterization of Alisertib (MLN8237), an Investigational Small-Molecule Inhibitor of Aurora A Kinase Using Novel In Vivo Pharmacodynamic Assays

(2011) M. G. Manfredi et al.   CLINICAL CANCER RESEARCH

A Complex of Kif18b and MCAK Promotes Microtubule Depolymerization and Is Negatively Regulated by Aurora Kinases

(2011) Marvin E. Tanenbaum et al.   CURRENT BIOLOGY

Phase I, open-label, multicentre, dose-escalation, pharmacokinetic and pharmacodynamic trial of the oral aurora kinase inhibitor PF-03814735 in advanced solid tumours

(2011) Patrick Schöffski et al.   EUROPEAN JOURNAL OF CANCER

The clinical development of FLT3 inhibitors in acute myeloid leukemia

(2011) Steven Knapper   EXPERT OPINION ON INVESTIGATIONAL DRUGS

AT9283, a novel aurora kinase inhibitor, suppresses tumor growth in aggressive B-cell lymphomas

(2011) Wenqing Qi et al.   INTERNATIONAL JOURNAL OF CANCER

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

(2011) Kosuke Tsuboi et al.   LEUKEMIA RESEARCH

The Aurora Kinase Inhibitor CCT137690 Downregulates MYCN and Sensitizes MYCN-Amplified Neuroblastoma In Vivo

(2011) A. Faisal et al.   MOLECULAR CANCER THERAPEUTICS

Overexpression of Active Aurora-C Kinase Results in Cell Transformation and Tumour Formation

(2011) Jabbar Khan et al.   PLoS One

Clinical evaluation of AZD1152, an i.v. inhibitor of Aurora B kinase, in patients with solid malignant tumors

(2010) D. S. Boss et al.   ANNALS OF ONCOLOGY

Will newer tyrosine kinase inhibitors have an impact in AML?

(2010) Mark J. Levis   BEST PRACTICE & RESEARCH CLINICAL HAEMATOLOGY

Activity of the multitargeted kinase inhibitor, AT9283, in imatinib-resistant BCR-ABL-positive leukemic cells

(2010) R. Tanaka et al.   BLOOD

Preclinical Evaluation of AMG 900, a Novel Potent and Highly Selective Pan-Aurora Kinase Inhibitor with Activity in Taxane-Resistant Tumor Cell Lines

(2010) M. Payton et al.   CANCER RESEARCH

Aurora-A expressing tumour cells are deficient for homology-directed DNA double strand-break repair and sensitive to PARP inhibition

(2010) Tony Sourisseau et al.   EMBO Molecular Medicine

The novel Aurora A kinase inhibitor MLN8237 is active in resistant chronic myeloid leukaemia and significantly increases the efficacy of nilotinib

(2010) Kevin R. Kelly et al.   JOURNAL OF CELLULAR AND MOLECULAR MEDICINE

Aurora kinase inhibitors: novel small molecules with promising activity in acute myeloid and Philadelphia-positive leukemias

(2010) A S Moore et al.   LEUKEMIA

Aurora-C Kinase Deficiency Causes Cytokinesis Failure in Meiosis I and Production of Large Polyploid Oocytes in Mice

(2010) Kuo-Tai Yang et al.   MOLECULAR BIOLOGY OF THE CELL

The FLT3 Internal Tandem Duplication Mutation Is a Secondary Target of the Aurora B Kinase Inhibitor AZD1152-HQPA in Acute Myelogenous Leukemia Cells

(2010) M. Grundy et al.   MOLECULAR CANCER THERAPEUTICS

PF-03814735, an Orally Bioavailable Small Molecule Aurora Kinase Inhibitor for Cancer Therapy

(2010) Jitesh P. Jani et al.   MOLECULAR CANCER THERAPEUTICS

Stabilization of N-Myc Is a Critical Function of Aurora A in Human Neuroblastoma

(2009) Tobias Otto et al.   CANCER CELL

AZD1152 Rapidly and Negatively Affects the Growth and Survival of Human Acute Myeloid Leukemia Cells In vitro and In vivo

(2009) A. Oke et al.   CANCER RESEARCH

A Phase I Dose-Escalation Study of Danusertib (PHA-739358) Administered as a 24-Hour Infusion with and without Granulocyte Colony-Stimulating Factor in a 14-Day Cycle in Patients with Advanced Solid Tumors

(2009) R. B. Cohen et al.   CLINICAL CANCER RESEARCH

Phase I Pharmacokinetic and Pharmacodynamic Study of the Aurora Kinase Inhibitor Danusertib in Patients With Advanced or Metastatic Solid Tumors

(2009) Neeltje Steeghs et al.   JOURNAL OF CLINICAL ONCOLOGY

Determinants for the efficiency of anticancer drugs targeting either Aurora-A or Aurora-B kinases in human colon carcinoma cells

(2009) P. Kaestner et al.   MOLECULAR CANCER THERAPEUTICS

Aurora Kinases as Anticancer Drug Targets

(2008) O. Gautschi et al.   CLINICAL CANCER RESEARCH

Effects of the aurora kinase inhibitors AZD1152-HQPA and ZM447439 on growth arrest and polyploidy in acute myeloid leukemia cell lines and primary blasts

(2008) E. Walsby et al.   HAEMATOLOGICA

Fragment-Based Discovery of the Pyrazol-4-yl Urea (AT9283), a Multitargeted Kinase Inhibitor with Potent Aurora Kinase Activity†

(2008) Steven Howard et al.   JOURNAL OF MEDICINAL CHEMISTRY

Polo-like kinase-1 is activated by aurora A to promote checkpoint recovery

(2008) Libor Macůrek et al.   NATURE

Bora and the Kinase Aurora A Cooperatively Activate the Kinase Plk1 and Control Mitotic Entry

(2008) A. Seki et al.   SCIENCE