Medicinal Chemistry Reviews

Volume 52, Chapter 26

Case History:  Epidaza® (Chidamide):  A Novel Oral Histone Deacetylase Inhibitor with Subtype Selectivity for Cancer Treatment

Xian P. Lu, Zhi B. Li, Zhi Q. Ning, De S. Pan, Song Shan, Xia Guo, Hai X. Cao, Jin D. Yu, and Qian J. Yang

1.          Introduction                                                                                                               497

2.         Discovery of Chidamide                                                                                           498

            2.1        Identification of Chemical Scaffold Inhibiting HDACs                              498

            2.2       Medicinal Chemistry Efforts Aimed at the Discovery of New 

                        Selective HDAC Inhibitor                                                                              499

            2.3       Multiplicity of Anticancer Mechanism                                                         503

3.         Preclinical Profiles of Chidamide                                                                            504

4.         Clinical Development of Chidamide                                                                       506

            4.1        A Phase I Clinical Study                                                                                506

            4.2       Exploratory and Pivotal Phase II Clinical Studies on PTCL                       508

5.         Conclusions                                                                                                               510

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