Alisertib (MLN8237) is an orally available , investigational, reversible, ATP-competitive, selective aurora A kinase inhibitor developed by Takeda.[1] Inhibition of Aurora Kinase A leads to disruption of mitotic spindle apparatus assembly, disruption of chromosome segregation, and inhibition of cell proliferation.[2] [3]
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Preferred IUPAC name
4-{[9-Chloro-7-(2-fluoro-6-methoxyphenyl)-5H-pyrimido[5,4-d][2]benzazepin-2-yl]amino}-2-methoxybenzoic acid | |
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Properties | |
C27H20ClFN4O4 | |
Molar mass | 518.93 g·mol−1 |
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
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Takeda investigated alisertib as a treatment for relapsed or refractory peripheral T-cell lymphoma[4][5] and development was paused in 2015[6] till Puma Biotechnology licensed global rights to alisertib from Takeda in 2022. [7][8]
References
edit- ^ Friedberg, JW; Mahadevan, D; Cebula, E; Persky, D; Lossos, I; Agarwal, AB; Jung, J; Burack, R; Zhou, X; Leonard, EJ; Fingert, H; Danaee, H; Bernstein, SH (Jan 1, 2014). "Phase II study of alisertib, a selective Aurora A kinase inhibitor, in relapsed and refractory aggressive B- and T-cell non-Hodgkin lymphomas". Journal of Clinical Oncology. 32 (1): 44–50. doi:10.1200/JCO.2012.46.8793. PMC 3867644. PMID 24043741.
- ^ Manfredi, Mark G.; Ecsedy, Jeffrey A.; Chakravarty, Arijit; Silverman, Lee; Zhang, Mengkun; Hoar, Kara M.; Stroud, Stephen G.; Chen, Wei; Shinde, Vaishali; Huck, Jessica J.; Wysong, Deborah R.; Janowick, David A.; Hyer, Marc L.; Leroy, Patrick J.; Gershman, Rachel E. (2011-12-15). "Characterization of Alisertib (MLN8237), an investigational small-molecule inhibitor of aurora A kinase using novel in vivo pharmacodynamic assays". Clinical Cancer Research: An Official Journal of the American Association for Cancer Research. 17 (24): 7614–7624. doi:10.1158/1078-0432.CCR-11-1536. ISSN 1557-3265. PMID 22016509.
- ^ Niu, Huifeng; Manfredi, Mark; Ecsedy, Jeffrey A. (2015-08-24). "Scientific Rationale Supporting the Clinical Development Strategy for the Investigational Aurora A Kinase Inhibitor Alisertib in Cancer". Frontiers in Oncology. 5: 189. doi:10.3389/fonc.2015.00189. ISSN 2234-943X. PMC 4547019. PMID 26380220.
- ^ "Millennium Initiates Pivotal Phase 3 Trial of MLN8237 in Patients With Relapsed or Refractory Peripheral T-cell Lymphoma". Takeda Pharmaceutical Company Limited; Millennium Pharmaceuticals, Inc. March 6, 2012. Retrieved 20 March 2014.
- ^ "Research and Development Pipeline (As of February 5, 2014)" (PDF). Takeda Pharmaceutical Company Limited. February 5, 2014. p. 2. Retrieved 20 March 2014.
- ^ "Takeda Announces Termination of Alisertib Phase 3 Trial in Relapsed or Refractory Peripheral T-cell Lymphoma".
- ^ Taylor, Nick Paul (September 21, 2022). "Puma pounces on failed Takeda drug, snapping up cancer prospect for knockdown price".
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: CS1 maint: url-status (link) - ^ Taylor, Phil (September 21, 2022). "Takeda farms out cancer drug alisertib to Puma Biotech".
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