Panobinostat (LBH589): a potent pan-deacetylase inhibitor with promising activity against hematologic and solid tumors
Panobinostat (LBH589): a potent pan-deacetylase inhibitor with promising activity against hematologic and solid tumors
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DOI：
10.2217/fon.09.36
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发表时间：
2009-06-01
期刊：
影响因子：
3.3
通讯作者：
Johnstone, Ricky W.
中科院分区：
文献类型：
--
作者：
Prince, H. Miles;Bishton, Mark J.;Johnstone, Ricky W.
脱乙酰酶抑制剂是一种结构多样的靶向抗肿瘤药物，已在体外和体内广泛的恶性肿瘤中表现出临床前活性。基于这种临床前活性，近年来几种脱乙酰酶抑制剂经历了快速的临床开发。其中，脱乙酰酶抑制剂帕比司他是研究最广泛的药物之一，在各种血液和实体瘤中具有广泛的药代动力学，药效学和剂量探索数据。此外，帕比司他已在I期和II期研究中显示出对各种血液恶性肿瘤（最显著的是淋巴瘤和骨髓恶性肿瘤）的有利临床活性。在这篇文章中，我们讨论了帕比司他的临床前数据和来自癌症患者I期和II期研究的新数据。
The deacetylase inhibitors are a structurally diverse class of targeted antineoplastic agents that have demonstrated in vitro and in vivo preclinical activity in a wide range of malignancies. Based on this preclinical activity, several deacetylase inhibitors have undergone rapid clinical development in recent years. Among these, the deacetylase inhibitor panobinostat is one of the most widely studied, with extensive pharmacokinetic, pharmacodynamic and dose-finding data available across a wide variety of hematologic and solid tumors. Furthermore, panobinostat has demonstrated favorable clinical activity against various hematologic malignancies, most notably lymphomas and myeloid malignancies in Phase I and II studies. In this article, we discuss the preclinical data on panobinostat and emerging data from Phase I and II studies in cancer patients.