转录水平的基因表达通过表观遗传修饰（例如 DNA 甲基化、组蛋白甲基化和乙酰化）而改变，这些修饰可以上调、下调或完全沉默基因。表观遗传过程的病理性失调可能导致癌症、神经系统问题、代谢紊乱和心血管疾病的发生。寻找针对这些表观遗传改变的药物具有广阔的治疗意义。尽管在这一领域已经做了大量的工作，但很少有分子被批准用于临床目的。本文全面回顾了癌症表观遗传学治疗的最新进展，特别关注新兴的递送和开发策略。人们正在研究各种递送系统，包括前药、缀合分子、纳米粒子（NP）和脂质体，以及联合疗法和表观遗传编辑等治疗策略，以提高表观遗传药物（表观药物）的功效和特异性。 ）。此外，还讨论了与现有表观药物相关的挑战及其转化为临床的局限性。靶点选择、亚型选择性、合成分子的理化性质、药物筛选以及表外药物从临床前到临床领域的可扩展性是需要解决的主要缺点。本综述讨论了识别新生物标志物的新策略、探索表观遗传修饰剂的药物化学、优化剂量方案以及设计适当的临床试验，从而比传统疗法更好地利用表观遗传修饰剂。这些方法的整合对于提高表观遗传治疗的功效和精度具有巨大的潜力，最终使癌症患者受益。

Gene expression at the transcriptional level is altered by epigenetic modifications such as DNA methylation, histone methylation, and acetylation, which can upregulate, downregulate, or entirely silence genes. Pathological dysregulation of epigenetic processes can result in the development of cancer, neurological problems, metabolic disorders, and cardiovascular diseases. It is of promising therapeutic interest to find medications that target these epigenetic alterations. Despite the enormous amount of work that has been done in this area, very few molecules have been approved for clinical purposes. This article provides a comprehensive review of recent advances in epigenetic therapeutics for cancer, with a specific focus on emerging delivery and development strategies. Various delivery systems, including pro-drugs, conjugated molecules, nanoparticles (NPs), and liposomes, as well as remedial strategies such as combination therapies, and epigenetic editing, are being investigated to improve the efficacy and specificity of epigenetic drugs (epi-drugs). Furthermore, the challenges associated with available epi-drugs and the limitations of their translation into clinics have been discussed. Target selection, isoform selectivity, physiochemical properties of synthesized molecules, drug screening, and scalability of epi-drugs from preclinical to clinical fields are the major shortcomings that are addressed. This Review discusses novel strategies for the identification of new biomarkers, exploration of the medicinal chemistry of epigenetic modifiers, optimization of the dosage regimen, and design of proper clinical trials that will lead to better utilization of epigenetic modifiers over conventional therapies. The integration of these approaches holds great potential for improving the efficacy and precision of epigenetic treatments, ultimately benefiting cancer patients.