While the novel anticancer agent CPI-613, currently in clinical trials, is primarily known to affect multiple cancer cell energy metabolic processes and pathways, here we demonstrate that CPI-613 also shows cancer-cell-cycle-specific effects on BxPC3 (human pancreatic) cancer cells, SF539 (human gliosarcoma) cells, and H460 (human non-small cell lung cancer) cells but not on non-transformed NIH3T3 (murine fibroblast) cells. Specifically, gene microarray data demonstrates that CPI-613 affects signal transduction pathways and genes related to cell cycle maintenance and progression as well as energetic metabolic processes and pathways. The total RNA production was also significantly reduced in cancer cells treated with CPI-613 compared to non treated controls. Multiple cyclins, p27, p19, and CDK2 are specifically noted to be downregulated in cancer cells treated with this drug, thereby halting the cell cycle at multiple points. Further study of this phenomenon may lead to additional indications for CPI-613 treatment.

Citation Format: {Authors}. {Abstract title} [abstract]. In: Proceedings of the 103rd Annual Meeting of the American Association for Cancer Research; 2012 Mar 31-Apr 4; Chicago, IL. Philadelphia (PA): AACR; Cancer Res 2012;72(8 Suppl):Abstract nr 3807. doi:1538-7445.AM2012-3807