Xu Y, Zhang P, Liu Y
Department of Internal Medicine, Henan Cancer Hospital & Affiliated Cancer Hospital of Zhengzhou University, Zhengzhou, China.
Drugs Today (Barc). 2017 Mar;53(3):167-176. doi: 10.1358/dot.2017.53.3.2595452.
Chidamide is the first oral subtype-selective histone deacetylase inhibitor (HDACI) approved in China as well as the first HDACI of the benzamide class approved for the treatment of relapsed and refractory peripheral T-cell lymphoma (PTCL). This review addresses detailed information regarding chidamide, including the mechanism of action, preclinical pharmacology, pharmacokinetics and metabolism, clinical studies and application, safety, drug interactions and ongoing clinical trials. Although twice-weekly chidamide monotherapy has been recommended based on the evidence from preclinical and clinical studies with tolerable toxicities, its clinical efficacy could be further increased by combination with multidrug chemotherapy or chemo-free regimens. Further investigations into the mechanism of chidamide will facilitate the identification of optimal combined therapy approaches and suitable treatment populations. This review will contribute to a comprehensive understanding and better use of chidamide in clinical practice.
西达本胺是中国首个获批的口服亚型选择性组蛋白去乙酰化酶抑制剂（HDACI），也是首个获批用于治疗复发难治性外周T细胞淋巴瘤（PTCL）的苯甲酰胺类HDACI。本综述阐述了关于西达本胺的详细信息，包括作用机制、临床前药理学、药代动力学和代谢、临床研究与应用、安全性、药物相互作用以及正在进行的临床试验。尽管基于临床前和临床研究证据，推荐每周两次的西达本胺单药治疗且毒性可耐受，但其临床疗效可通过与多药化疗或无化疗方案联合使用而进一步提高。对西达本胺作用机制的进一步研究将有助于确定最佳联合治疗方法和合适的治疗人群。本综述将有助于在临床实践中全面了解和更好地使用西达本胺。
