Zotiraciclib
Developing New Innovative Treatments for Aggressive Cancers
High-grade gliomas represent the most aggressive brain cancers with the highest unmet need.1
Once diagnosed, patient prognosis is poor. Median overall survival for all high-grade gliomas—and glioblastoma, the most common high-grade glioma representing about half of all brain cancers—is dire. Improved treatment options are desperately needed.2
There is a significant need for transformative treatments that move beyond cytotoxic chemotherapy into targeted and innovative cancer treatments.
Zotiraciclib, Multi-Kinase Inhibitor
CDK9 is a predominant site of activity. Zotiraciclib also demonstrates a high level of inhibitory activity against CDK2, CDK5, CDK7 and ERK5.
Key Pathway Inhibition
| Kinase | IC50(nM) | Function | Indication |
|---|---|---|---|
| CDK9 | 3 | MYC depletion | Glioma, HCC, TNBC |
| CDK5 | 4 | DNA damage response | Glioma, TNBC |
| CDK2 | 5 | Cell cycle | Glioma, HCC, TNBC |
| CDK7 | 12 | mRNA transcription | Glioma, ovarian |
| ERK5 | 43 | Survival and differentiation | DIPG, TNBC |
1. Louis DN, Perry A, Reifenberger G, et al. The 2016 World Health Organization classification of tumors of the central nervous system: a summary. Acta Neuropathol. 2016;131(6):803-820. 2. Ostrom QT, Gittleman H, Truitt G, Boscia A, Kruchko C, Barnholtz-Sloan JS. CBTRUS statistical report: primary brain and other central nervous system tumors diagnosed in the United States in 2011-2015. Neuro Oncol. 2018;20(suppl 4):iv1-iv86. 3. Yan H, Parsons DW, Jin G, et al. IDH1 and IDH2 mutations in gliomas. N Engl J Med. 2009;360(8):765-773.