Histone demethylase LSD1 plays key roles during carcinogenesis, targeting LSD1 is becoming an emerging option for the treatment of cancers. Numerous LSD1 inhibitors have been reported to date, some of them such as TCP, ORY-1001, GSK-2879552, IMG-7289, INCB059872, CC-90011, and ORY-2001 currently undergo clinical assessment for cancer therapy, particularly for small lung cancer cells (SCLC) and acute myeloid leukemia (AML). This review is to provide a comprehensive overview of LSD1 inhibitors in clinical trials including molecular mechanistic studies, clinical efficacy, adverse drug reactions, and PD/PK studies and offer prospects in this field.

中文翻译：

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临床试验中的 LSD1/KDM1A 抑制剂：进展与前景。

组蛋白去甲基化酶 LSD1 在癌症发生过程中发挥着关键作用，靶向 LSD1 正在成为治疗癌症的新兴选择。迄今为止，已有多种LSD1抑制剂被报道，其中一些如TCP、ORY-1001、GSK-2879552、IMG-7289、INCB059872、CC-90011和ORY-2001目前正在接受癌症治疗的临床评估，特别是对于小肺癌细胞（SCLC）和急性髓性白血病（AML）。本综述旨在对LSD1抑制剂在临床试验中的分子机制研究、临床疗效、药物不良反应、PD/PK研究等方面进行全面综述，并展望该领域的前景。