title: MLN8054 and Alisertib (MLN8237): Discovery of Selective Oral Aurora A Inhibitors.
abstract: The Aurora kinases are essential for cell mitosis, and the dysregulation of Aurora A and B have been linked to the etiology of human cancers. Investigational agents MLN8054 (8) and alisertib (MLN8237, 10) have been identified as high affinity, selective, orally bioavailable inhibitors of Aurora A that have advanced into human clinical trials. Alisertib (10) is currently being evaluated in multiple Phase II and III clinical trials in hematological malignancies and solid tumors.
authors.affiliation: Takeda Pharmaceuticals International Co. , 40 Landsdowne Street, Cambridge, Massachusetts 02139, United States.
authors.forename: Todd B
authors.initials: TB
authors.lastname: Sells
authors.affiliation: Takeda Pharmaceuticals International Co. , 40 Landsdowne Street, Cambridge, Massachusetts 02139, United States.
authors.forename: Ryan
authors.initials: R
authors.lastname: Chau
authors.affiliation: Takeda Pharmaceuticals International Co. , 40 Landsdowne Street, Cambridge, Massachusetts 02139, United States.
authors.forename: Jeffrey A
authors.initials: JA
authors.lastname: Ecsedy
authors.affiliation: Takeda Pharmaceuticals International Co. , 40 Landsdowne Street, Cambridge, Massachusetts 02139, United States.
authors.forename: Rachel E
authors.initials: RE
authors.lastname: Gershman
authors.affiliation: Takeda Pharmaceuticals International Co. , 40 Landsdowne Street, Cambridge, Massachusetts 02139, United States.
authors.forename: Kara
authors.initials: K
authors.lastname: Hoar
authors.affiliation: Takeda Pharmaceuticals International Co. , 40 Landsdowne Street, Cambridge, Massachusetts 02139, United States.
authors.forename: Jessica
authors.initials: J
authors.lastname: Huck
authors.affiliation: Takeda Pharmaceuticals International Co. , 40 Landsdowne Street, Cambridge, Massachusetts 02139, United States.
authors.forename: David A
authors.initials: DA
authors.lastname: Janowick
authors.affiliation: Takeda Pharmaceuticals International Co. , 40 Landsdowne Street, Cambridge, Massachusetts 02139, United States.
authors.forename: Vivek J
authors.initials: VJ
authors.lastname: Kadambi
authors.affiliation: Takeda Pharmaceuticals International Co. , 40 Landsdowne Street, Cambridge, Massachusetts 02139, United States.
authors.forename: Patrick J
authors.initials: PJ
authors.lastname: LeRoy
authors.affiliation: Takeda Pharmaceuticals International Co. , 40 Landsdowne Street, Cambridge, Massachusetts 02139, United States.
authors.forename: Matthew
authors.initials: M
authors.lastname: Stirling
authors.affiliation: Takeda Pharmaceuticals International Co. , 40 Landsdowne Street, Cambridge, Massachusetts 02139, United States.
authors.forename: Stephen G
authors.initials: SG
authors.lastname: Stroud
authors.affiliation: Takeda Pharmaceuticals International Co. , 40 Landsdowne Street, Cambridge, Massachusetts 02139, United States.
authors.forename: Tricia J
authors.initials: TJ
authors.lastname: Vos
authors.affiliation: Takeda Pharmaceuticals International Co. , 40 Landsdowne Street, Cambridge, Massachusetts 02139, United States.
authors.forename: Gabriel S
authors.initials: GS
authors.lastname: Weatherhead
authors.affiliation: Takeda Pharmaceuticals International Co. , 40 Landsdowne Street, Cambridge, Massachusetts 02139, United States.
authors.forename: Deborah R
authors.initials: DR
authors.lastname: Wysong
authors.affiliation: Takeda Pharmaceuticals International Co. , 40 Landsdowne Street, Cambridge, Massachusetts 02139, United States.
authors.forename: Mengkun
authors.initials: M
authors.lastname: Zhang
authors.affiliation: Takeda Pharmaceuticals International Co. , 40 Landsdowne Street, Cambridge, Massachusetts 02139, United States.
authors.forename: Suresh K
authors.initials: SK
authors.lastname: Balani
authors.affiliation: Takeda Pharmaceuticals International Co. , 40 Landsdowne Street, Cambridge, Massachusetts 02139, United States.
authors.forename: Joseph B
authors.initials: JB
authors.lastname: Bolen
authors.affiliation: Takeda Pharmaceuticals International Co. , 40 Landsdowne Street, Cambridge, Massachusetts 02139, United States.
authors.forename: Mark G
authors.initials: MG
authors.lastname: Manfredi
authors.affiliation: Takeda Pharmaceuticals International Co. , 40 Landsdowne Street, Cambridge, Massachusetts 02139, United States.
authors.forename: Christopher F
authors.initials: CF
authors.lastname: Claiborne
keywords: Alisertib; Aurora A kinase; MLN8054; MLN8237