新型同型选择性组蛋白去乙酰化酶抑制剂MGCD0103具有可观的抗肿瘤活性。
Promising antitumor activity with MGCD0103, a novel isotype-selective histone deacetylase inhibitor.
作者信息
Le Tourneau Christophe, Siu Lillian L
机构信息
University of Toronto, University Health Network, Princess Margaret Hospital, Division of Medical Oncology and Hematology, 610 University Avenue, Suite 5-718, Toronto M5G 2M9, Canada.
出版信息
Expert Opin Investig Drugs. 2008 Aug;17(8):1247-54. doi: 10.1517/13543784.17.8.1247.
BACKGROUND
Histone deacetylases (HDACs), which target histones as well as non-histone proteins as substrates, have the potential to regulate aberrant gene expression and restore normal growth control in malignancies.
OBJECTIVE
This review provides an updated summary of preclinical and clinical experience with the oral isotype-selective HDAC inhibitor MGCD0103 in cancer.
METHODS
Data presented in abstract form from international conferences or journal articles found within a PubMed search of article up to May 2008 are described in this review.
RESULTS/CONCLUSIONS: MGCD0103 appears tolerable and exhibits favorable pharmacokinetic and pharmacodynamic profiles with evidence of target inhibition in surrogate tissues. Clinical and pharmacodynamic data support a three-times-weekly administration at a 90-mg fixed dose. MGCD0103 displays promising antitumor activity in hematological and lymphoproliferative diseases.
背景
组蛋白去乙酰化酶（HDACs）以组蛋白以及非组蛋白为底物，有调节异常基因表达和恢复恶性肿瘤中正常生长控制的潜力。
目的
本综述提供了口服同型选择性HDAC抑制剂MGCD0103治疗癌症的临床前和临床经验的最新总结。
方法
本综述描述了通过在PubMed中检索截至2008年5月的文章，从国际会议或期刊文章中以摘要形式呈现的数据。
结果/结论：MGCD0103似乎耐受性良好，具有良好的药代动力学和药效学特征，在替代组织中有靶点抑制的证据。临床和药效学数据支持每周三次、90毫克固定剂量的给药方案。MGCD0103在血液学和淋巴增殖性疾病中显示出有前景的抗肿瘤活性。
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