2. Academic Validation
  3. MLN8054 and Alisertib (MLN8237): Discovery of Selective Oral Aurora A Inhibitors

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

Affiliation

  • 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.

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