CUDC-101 is a multitargeted inhibitor of histone deacetylase. It is designed to directly inhibit epidermal growth factor receptor (EGFR) and HER2 as well as class I and class II HDACs. It has been shown that CUDC-101 is able to effectively suppress the progression of a broad range of tumor types in both in vitro and in vivo xenograft models, including lapatinib- and erlotinib-resistant cancer cell lines. Mechanistic studies provide the evidence that CUDC-101 not only directly inhibits both EGFR and HER2 signaling but also indirectly attenuates the survival signaling pathways Akt, HER3, and MET.
Cheng-Jung Lai, Rudi Bao, Xu Tao, Jing Wang, Ruzanna Atoyan, Hui Qu, Da-Gong Wang, Ling Yin, Maria Samson, Jeffrey Forrester, Brian Zifcak, Guang-Xin Xu, Steven DellaRocca, Hai-Xiao Zhai, Xiong Cai, William E. Munger, Mitchell Keegan, Carmen V. Pepicelli, and Changgeng Qian. CUDC-101, a Multitargeted Inhibitor of Histone Deacetylase, Epidermal Growth Factor Receptor, and Human Epidermal Growth Factor Receptor 2, Exerts Potent Anticancer Activity. Cancer Res May 1, 2010 70; 3647.