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

  • ACS Med Chem Lett. 2015 Apr 22;6(6):630-4. doi: 10.1021/ml500409n.
Todd B Sells  1 ,  Ryan Chau  1 ,  Jeffrey A Ecsedy  1 ,  Rachel E Gershman  1 ,  Kara Hoar  1 ,  Jessica Huck  1 ,  David A Janowick  1 ,  Vivek J Kadambi  1 ,  Patrick J LeRoy  1 ,  Matthew Stirling  1 ,  Stephen G Stroud  1 ,  Tricia J Vos  1 ,  Gabriel S Weatherhead  1 ,  Deborah R Wysong  1 ,  Mengkun Zhang  1 ,  Suresh K Balani  1 ,  Joseph B Bolen  1 ,  Mark G Manfredi  1 ,  Christopher F Claiborne  1
Affiliations
  • 1. Takeda Pharmaceuticals International Co. , 40 Landsdowne Street, Cambridge, Massachusetts 02139, United States.
PMID: 26101564 DOI: 10.1021/ml500409n
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.

Keywords
Alisertib; Aurora A kinase; MLN8054; MLN8237.