Thaler Florian
Drug Discovery Unit, European Institute of Oncology, Via Adamello 16, 20139 Milan, Italy.
Pharm Pat Anal. 2012 Mar;1(1):75-90. doi: 10.4155/ppa.11.3.
Histone deacetylases (HDACs) have become an important target for the treatment of cancer and other diseases. Currently, more than ten HDAC inhibitors have entered clinical studies and two of them have already reached the market. The hydroxamic acid derivative SAHA (also known as vorinostat or Zolinza®) and the cyclic depsipeptide FK228 (romidepsin or Istodax®) have gained approval from the US FDA for the treatment of cutaneous T-cell lymphoma. Nevertheless, there has been a continuous effort aimed at discovering a new generation of clinical candidates with improved pharmaceutical properties. This review provides a summary of the most recent patents published from mid-2009 to mid-2011.
组蛋白脱乙酰酶（HDACs）已成为治疗癌症和其他疾病的重要靶点。目前，十多种HDAC抑制剂已进入临床研究阶段，其中两种已上市。异羟肟酸衍生物SAHA（也称为伏立诺他或Zolinza®）和环缩肽FK228（罗米地辛或Istodax®）已获得美国食品药品监督管理局（FDA）批准用于治疗皮肤T细胞淋巴瘤。尽管如此，人们仍在不断努力寻找具有更好药学性质的新一代临床候选药物。本综述总结了2009年年中至2011年年中发表的最新专利。
