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本文引用的文献

1
Recent developments in epigenetic cancer therapeutics: clinical advancement and emerging trends.表观遗传学癌症治疗的最新进展:临床进展和新兴趋势。
J Biomed Sci. 2021 Apr 12;28(1):27. doi: 10.1186/s12929-021-00721-x.
2
Tazemetostat in advanced epithelioid sarcoma with loss of INI1/SMARCB1: an international, open-label, phase 2 basket study.Tazemetostat 治疗 INI1/SMARCB1 缺失的晚期上皮样肉瘤:一项国际、开放标签、2 期篮子研究。
Lancet Oncol. 2020 Nov;21(11):1423-1432. doi: 10.1016/S1470-2045(20)30451-4. Epub 2020 Oct 6.
3
Tazemetostat for patients with relapsed or refractory follicular lymphoma: an open-label, single-arm, multicentre, phase 2 trial.塔西美替尼治疗复发或难治性滤泡性淋巴瘤患者的疗效:一项开放标签、单臂、多中心、2 期临床试验。
Lancet Oncol. 2020 Nov;21(11):1433-1442. doi: 10.1016/S1470-2045(20)30441-1. Epub 2020 Oct 6.
4
EZH2-Targeted Therapies in Cancer: Hype or a Reality.EZH2 靶向治疗在癌症中的应用:炒作还是现实?
Cancer Res. 2020 Dec 15;80(24):5449-5458. doi: 10.1158/0008-5472.CAN-20-2147. Epub 2020 Sep 25.
5
EZH2 inhibition: a promising strategy to prevent cancer immune editing.EZH2 抑制:预防癌症免疫编辑的一种有前途的策略。
Epigenomics. 2020 Aug;12(16):1457-1476. doi: 10.2217/epi-2020-0186. Epub 2020 Sep 17.
6
EZH2: a novel target for cancer treatment.EZH2:癌症治疗的新靶点。
J Hematol Oncol. 2020 Jul 28;13(1):104. doi: 10.1186/s13045-020-00937-8.
7
The complex role of EZH2 in the tumor microenvironment: opportunities and challenges for immunotherapy combinations.EZH2 在肿瘤微环境中的复杂作用:免疫治疗联合的机遇与挑战。
Future Med Chem. 2020 Aug;12(15):1415-1430. doi: 10.4155/fmc-2020-0072. Epub 2020 Jul 29.
8
EZH2 abnormalities in lymphoid malignancies: underlying mechanisms and therapeutic implications.EZH2 异常在淋巴恶性肿瘤中的作用:潜在机制与治疗意义。
J Hematol Oncol. 2019 Nov 21;12(1):118. doi: 10.1186/s13045-019-0814-6.
9
The role and prospect of JMJD3 in stem cells and cancer.JMJD3 在干细胞和癌症中的作用和前景。
Biomed Pharmacother. 2019 Oct;118:109384. doi: 10.1016/j.biopha.2019.109384. Epub 2019 Sep 6.
10
Epigenetic Targets and their Inhibitors in Cancer Therapy.癌症治疗中的表观遗传学靶点及其抑制剂。
Curr Top Med Chem. 2018;18(28):2395-2419. doi: 10.2174/1568026619666181224095449.

他泽司他:EZH2抑制剂。

Tazemetostat: EZH2 Inhibitor.

作者信息

Straining Rachael, Eighmy William

机构信息

Yale New Haven Health Smilow Cancer Hospital, New Haven, Connecticut.

出版信息

J Adv Pract Oncol. 2022 Mar;13(2):158-163. doi: 10.6004/jadpro.2022.13.2.7. Epub 2022 Mar 25.

DOI:10.6004/jadpro.2022.13.2.7
PMID:35369397
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8955562/
Abstract

Epigenetic regulation is a novel approach to cancer treatment. Inhibition of enhancer of zeste homolog 2 () is a method to provide targeted epigenetic regulation. Tazemetostat is a first-in-class targeted epigenetic regulator that specifically inhibits EZH2. This new FDA-approved oral treatment received accelerated approval for patients with hematologic and solid malignancies. Tazemetostat was first approved for patients 16 years and older with metastatic or locally advanced epithelioid sarcoma not eligible for complete resection based on the results of an international open-label phase II basket trial. Another open-label multicenter phase II trial led to the approval for patients with relapsed or refractory follicular lymphoma with mutation who have received at least two prior systemic therapies or patients who have no satisfactory alternative treatment options. Tazemetostat as an oral EZH2 inhibitor provides a new effective and tolerable treatment option for these patients.

摘要

表观遗传调控是一种新型的癌症治疗方法。抑制zeste同源物2(EZH2)是一种实现靶向表观遗传调控的方法。他泽司他是首个获批的靶向表观遗传调节剂,可特异性抑制EZH2。这种新的经美国食品药品监督管理局(FDA)批准的口服治疗药物已获得加速批准,用于治疗血液系统恶性肿瘤和实体恶性肿瘤患者。基于一项国际开放标签II期篮子试验的结果,他泽司他首次获批用于治疗16岁及以上无法进行完全切除的转移性或局部晚期上皮样肉瘤患者。另一项开放标签多中心II期试验促使其获批用于治疗携带 突变、既往至少接受过两种全身治疗的复发或难治性滤泡性淋巴瘤患者,或没有满意替代治疗方案的患者。他泽司他作为一种口服EZH2抑制剂,为这些患者提供了一种新的有效且耐受性良好的治疗选择。