School of Pharmacy, College of Pharmacy, Taipei Medical University, Taipei, Taiwan.
TMU Research Center for Drug Discovery, Taipei Medical University, Taipei, Taiwan.
Expert Opin Ther Pat. 2023 Jan-Jun;33(5):349-369. doi: 10.1080/13543776.2023.2219393. Epub 2023 Jun 2.
Histone deacetylase (HDAC) inhibitors have been considered as an attractive strategy to reverse aberrant epigenetic changes associated with cancer treatments. The use of HDAC inhibitors in various cancer types has continued to develop for decades, bringing several novel HDAC inhibitors successfully into clinical trials. The combination use of HDAC inhibitors with other agents have also been developed and have demonstrated superior efficacy compared to that of monotherapy in recent studies. Hence, development of new anticancer treatment and therapeutic regimen is necessary.
This review summarizes a comprehensive review of the patent literature from 2020 to 2022 including HDAC inhibitors and their use as anticancer agents (searched from European Patent Office, 2020-2022). The approved and developing HDAC inhibitors are described. It also provides perspectives on the challenges and future opportunities.
Although hundreds of clinical trials of HDAC inhibitors are still going on, the application for HDAC inhibitors has been limited at present . Not only in the anticancer treatment, but also non-oncology disease therapies are being investigated eagerly. Recently, applications of HDAC inhibitors in non-oncology diseases have also been revealed and proceeded to clinical trials. New indications for HDAC inhibitors are needed urgently in the future.
组蛋白去乙酰化酶(HDAC)抑制剂已被认为是一种有吸引力的策略,可以逆转与癌症治疗相关的异常表观遗传变化。几十年来,HDAC 抑制剂在各种癌症类型中的应用不断发展,将几种新型 HDAC 抑制剂成功推向临床试验。HDAC 抑制剂与其他药物联合使用也在不断开发,并在最近的研究中显示出比单药治疗更好的疗效。因此,有必要开发新的抗癌治疗方法和治疗方案。
本综述总结了 2020 年至 2022 年专利文献的全面综述,包括 HDAC 抑制剂及其作为抗癌药物的用途(从欧洲专利局 2020 年至 2022 年检索)。描述了已批准和正在开发的 HDAC 抑制剂。它还提供了对挑战和未来机遇的看法。
尽管仍有数百项 HDAC 抑制剂的临床试验正在进行,但目前 HDAC 抑制剂的应用受到限制。不仅在癌症治疗中,非肿瘤疾病的治疗也在被积极研究。最近,HDAC 抑制剂在非肿瘤疾病中的应用也被揭示并进入临床试验。未来迫切需要 HDAC 抑制剂的新适应症。