Finding an easy way to harmonize: a review of advances in clinical research and combination strategies of EZH2 inhibitors

• Published in: Clinical epigenetics 2021-03, Vol.13 (1), p.62-62, Article 62
• Main Authors: Li, Chen, Wang, Yan, Gong, Yueqing, Zhang, Tengrui, Huang, Jiaqi, Tan, Zhen, Xue, Lixiang
• Format: Article
• Language: English
• Subjects: Antineoplastic Agents - pharmacology; Antineoplastic Agents - therapeutic use; Antitumor activity; Biomedical Research - statistics & numerical data; Cancer; Cancer therapies; Chemotherapy; Clinical trials; Competition; Drug dosages; Endocrine therapy; Enhancer of Zeste Homolog 2 Protein - antagonists & inhibitors; Enhancer of Zeste Homolog 2 Protein - genetics; Enhancer of Zeste Homolog 2 Protein - therapeutic use; Enzyme Inhibitors - pharmacology; Enzyme Inhibitors - therapeutic use; Enzymes; Epigenetics; FDA approval; Health aspects; Humans; Immunotherapy; Immunotherapy - methods; Immunotherapy - statistics & numerical data; Lymphoma; Medical research; Medicine, Experimental; Melanoma; Metastasis; Molecular Targeted Therapy - methods; Mutation; Neoplasms - therapy; Non-Hodgkin's lymphomas; Prostate cancer; Review; Solid tumors; Tumors
• ISSN: 1868-7075; 1868-7083; 1868-7083; 1868-7075
• DOI: 10.1186/s13148-021-01045-1

Enhancer of zeste homolog 2 inhibitors (EZH2i) have garnered increased attention owing to their anticancer activity by targeting EZH2, a well-known cancer-promoting factor. However, some lymphomas are resistant to EZH2i, and EZH2i treatment alone is ineffective in case of EZH2-overexpressing solid tumors. The anti-cancer efficacy of EZH2i may be improved through safe and effective combinations of these drugs with other treatment modalities. Preclinical evidence indicates that combining EZH2i with other therapies, such as immunotherapy, chemotherapy, targeted therapy, and endocrine therapy, has complementary or synergistic antitumor effects. Therefore, elucidating the underlying mechanisms of the individual constituents of the combination therapies is fundamental for their clinical application. In this review, we have summarized notable clinical trials and preclinical studies using EZH2i, their progress, and combinations of EZH2i with different therapeutic modalities, aiming to provide new insights for tumor treatment.