MLN8054 and Alisertib (MLN8237): Discovery of Selective Oral Aurora A Inhibitors
- Todd B. Sells (1359936)
- Ryan Chau (1359909)
- Jeffrey A. Ecsedy (1359933)
- Rachel E. Gershman (1359960)
- Kara Hoar (1359942)
- Jessica Huck (1359930)
- David A. Janowick (1359954)
- Vivek J. Kadambi (1359912)
- Patrick J. LeRoy (1359951)
- Matthew Stirling (1359924)
- Stephen G. Stroud (1359945)
- Tricia J. Vos (1359939)
- Gabriel S. Weatherhead (1359921)
- Deborah R. Wysong (1359948)
- Mengkun Zhang (1359918)
- Suresh K. Balani (1359957)
- Joseph B. Bolen (1359906)
- Mark G. Manfredi (1359915)
- Christopher F. Claiborne (1359927)
Publication date
December 2015
DOIAbstract
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 (<b>8</b>) and alisertib (MLN8237, <b>10</b>) have been identified as high affinity, selective, orally bioavailable inhibitors of Aurora A that have advanced into human clinical trials. Alisertib (<b>10</b>) is currently being evaluated in multiple Phase II and III clinical trials in hematological malignancies and solid tumors
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