更新于：2024-05-08
Chidamide
西达本胺
更新于：2024-05-08
概要
基本信息
药物类型 小分子化药 |
别名 Tucidinostat、87CIC980Y0 (UNII code)、CS-02100055 + [9] |
靶点 |
作用机制 HDAC抑制剂(组蛋白去乙酰化酶家族抑制剂) |
在研适应症 |
原研机构 |
最高研发阶段批准上市 |
首次获批日期 中国 (2014-12-23), |
最高研发阶段(中国)批准上市 |
特殊审评孤儿药 (美国)、优先审评 (中国)、特殊审批 (中国) |
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结构
分子式C22H19FN4O2 |
InChIKeySZMJVTADHFNAIS-BJMVGYQFSA-N |
CAS号1616493-44-7 |
关联
234
项与 西达本胺 相关的临床试验A Phase II Clinical Study of the Efficacy and Safety of Tislelizumab Combined With Fruquintinib and Chidamide in the Treatment of Unresectable or Advanced Microsatellite Stabilized (MSS/pMMR) Colorectal Cancer With Liver Metastases
A Multicenter, Randomized, Controlled Clinical Trial of Chidamide Combined With Venetoclax and Azacitidine in the Treatment of Newly Diagnosed Acute Myeloid Leukemia (AML) Who Are Not Suitable for Intensive Chemotherapy
A Randomized, Open-label, Phase 2 Trial of Chidamide+Decitabine Plus Anti-PD-1 Antibody in PD-1 Inhibitor Failed Patients With Classical Hodgkin Lymphoma.
100 项与 西达本胺 相关的临床结果
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100 项与 西达本胺 相关的转化医学
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100 项与 西达本胺 相关的专利（医药）
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311
项与 西达本胺 相关的文献（医药）2024-01-01BMJ Case Reports
Improving gastrointestinal quality of life: romidepsin to tucidinostat in a case of angioimmunoblastic T cell lymphoma
Article
作者: Kanaya, Shuhei ; Isoda, Atsushi ; Terasaki, Yukie ; Saito, Akio
Relapsed/refractory (R/R) peripheral T cell lymphoma (PTCL) has a poor prognosis, with limited treatment options and generally no durable response. However, long-term remission with the histone deacetylase (HDAC) inhibitor romidepsin has been reported, especially in angioimmunoblastic T cell lymphoma (AITL). Recently, tucidinostat, a novel oral HDAC inhibitor that selectively inhibits class I and class IIb HDACs, was approved for R/R PTCL in China and Japan. We present the case of a patient with AITL whose gastrointestinal symptoms and health-related quality of life improved after switching from romidepsin to tucidinostat as maintenance therapy. Romidepsin and tucidinostat appear to have different safety profiles; non-haematological toxicities such as nausea, vomiting, constipation, anorexia and fatigue may be reported less frequently with tucidinostat than with romidepsin. This case suggests that switching to tucidinostat therapy may be a viable option for patients with PTCL suffering from severe gastrointestinal adverse events with romidepsin.
2024-01-01European Journal of Medicinal Chemistry
Serendipitous discovery of Class I HDAC inhibitors from rational design of molecular glue degraders targeting HDAC
Article
作者: An, Jianxiong ; Gu, Zhicheng ; Chen, Di ; He, Bin ; Yan, Wanli ; Lin, Shuxian ; Zeng, Ziwei ; Chen, Lei
Zinc-dependent histone deacetylases (HDACs) play an essential role as epigenetic regulators and are becoming increasingly important drug targets for the treatment of cancer. Although five HDAC inhibitors have been approved for treating several cancers, only one of them is a Class I HDAC inhibitor, which may have advantages over pan-HDAC inhibitors due to the various side effects associated with the latter. On the other hand, the emerging strategy of molecular glue degraders offers a unique advantage for targeting therapeutic proteins. In this study, we synthesized a series of candidate compounds based on the molecule glue, pomalidomide, using a "merger principle", initially aiming to obtain molecular glue degraders that can target HDAC degradation. However, we serendipitously discovered that compounds 2f and 3f may be potent Class I HDAC selective inhibitors. After further evaluation, we found that compounds 2f and 3f exhibit selective inhibitory effects on Class I HDAC in cancer cells. Moreover, they showed the robust antiproliferative activities against various hematological tumor cells, comparable to that of the approved Class I HDAC inhibitor, Chidamide. These results suggest that pomalidomide-derivatized compounds have promising potential as Class I HDAC inhibitors with therapeutic applications in cancer treatment.
2023-12-31Hematology
Application of prophylactic or pre-emptive therapy after allogeneic transplantation for high-risk patients with t(8;21) acute myeloid leukemia
Article
作者: Yang, Donglin ; Zhang, Rongli ; Liu, Xin ; Pang, Aiming ; He, Yi ; Zhai, Weihua ; Jiang, Erlie ; Cao, Yigeng ; Zheng, Yawei ; Wang, Mingyang ; Feng, Sizhou ; Guo, Wenwen ; Chen, Xin ; Ma, Qiaoling ; Wei, Jialin ; Liu, Jia ; Han, Mingzhe
OBJECTIVES:
To determine the impact of pretransplant measurable residual disease (pre-MRD) and the efficacy of maintenance therapy in t(8;21) acute myeloid leukemia (AML) patients after allogeneic hematopoietic cell transplantation (allo-HCT).
METHODS:
We retrospectively analyzed 100 t(8;21) AML patients who underwent allo-HCT between 2013 and 2022. 40 patients received pre-emptive therapy including immunosuppressant adjustment, azacitidine, and donor lymphocyte infusion (DLI) combined with chemotherapy. 23 patients received prophylactic therapy, including azacitidine or chidamide.
RESULTS:
Patients with a positive pre-MRD (pre-MRDpos) had a higher 3-year cumulative incidence of relapse (CIR) (25.90% [95% CI, 13.87%-39.70%] vs 5.00% [95% CI, 0.88%-15.01%]; P = 0.008). Pre-MRDpos patients were less likely to have a superior 3-year disease-free survival (DFS) (40.83% [95% CI, 20.80%-80.16%]) if their MRD was still positive at 28 days after transplantation (post-MRD28pos). The 3-year DFS and CIR were 53.17% (95% CI, 38.31% - 73.80%) and 34.87% (95% CI, 18.84% - 51.44%), respectively, for patients receiving pre-emptive interventions after molecular relapse. The 3-year DFS and CIR were 90.00% (95%CI, 77.77% - 100%) and 5.00% (95%CI, 0.31% - 21.10%), respectively, for high-risk patients receiving prophylactic therapy. In most patients, epigenetic-drug-induced adverse events were reversible with dose adjustment or temporary discontinuation.
CONCLUSION:
Patients with pre-MRDpos and post-MRD28pos were more likely to have higher rates of relapse and inferior DFS, even after receiving pre-emptive interventions. Prophylactic therapy may be a better option for high-risk t(8;21) AML patients; however, this warrants further investigation.
100 项与 西达本胺 相关的药物交易
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研发状态
| 适应症 | 最高研发状态 | 国家/地区 | 公司 |
|---|---|---|---|
| 外周T细胞淋巴瘤 | 批准上市 | 中国 更多 | |
| 乳腺癌 | 批准上市 | 中国台湾 更多 | |
| 弥漫性大B细胞淋巴瘤 | 批准上市 | 中国 更多 | |
| 肝细胞癌 | 临床2期 | 中国台湾 更多 | |
| 黑色素瘤 | 无进展 | 新西兰 更多 |
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临床结果
临床结果
适应症
分期
评价
查看全部结果
临床2期 | 急性髓性白血病 维持 | 36 | 鬱憲壓觸遞蓋艱鹽壓襯(繭窪窪艱繭願鹽鏇鏇淵) = 選鹹製窪選廠衊範衊簾 願製鹹網襯鑰範膚醖遞 (蓋鹹廠鬱餘憲糧餘膚壓, 6.5 ~ 18.1) 更多 | - | 2023-12-11 | ||
N/A | - | 鬱壓製遞鏇選夢窪繭選(憲鹽選夢顧鬱糧蓋醖製) = 繭膚遞鬱鬱壓衊齋顧糧 窪膚廠廠顧壓觸繭範糧 (簾簾繭構壓襯願積衊鹹 ) 更多 | - | 2023-12-11 | |||
N/A | 50 | 顧網範簾淵夢繭構觸選(積壓廠遞選鏇糧範遞遞) = 襯構願糧網窪願鹹襯築 鑰選獵艱鏇廠鹽鹹憲鑰 (構鏇糧餘願築衊膚夢淵 ) 更多 | - | 2023-12-10 | |||
N/A | 18 | 構製積艱艱衊淵衊鹽淵(獵壓製繭齋積積廠繭觸) = 遞遞獵餘網夢鏇糧網鏇 鑰憲鬱鬱顧夢襯積顧製 (窪鹽蓋廠選遞觸襯製淵 ) 更多 | - | 2023-12-10 | |||
ESMO2023 人工标引  | 临床2期 | 非小细胞肺癌 巩固 | 19 | 積製願簾廠艱獵膚餘顧(糧獵衊顧衊壓糧獵衊顧) = 築齋餘製膚顧衊製鹽繭 願範餘積襯窪築築夢衊 (夢繭醖淵襯壓餘獵壓夢 ) 更多 | 积极 | 2023-10-21 | |
N/A | 6 | 淵夢齋築夢餘鹽糧齋醖(壓願繭廠衊鏇糧鹹繭構) = 餘積壓構艱齋範鹹膚衊 顧簾鑰夢襯繭鬱窪憲蓋 (觸衊蓋衊夢鹽艱積願構 ) 更多 | - | 2023-06-08 | |||
N/A | 48 | 糧齋齋願廠顧鹽鏇餘壓(遞憲襯餘鏇鬱觸繭積簾) = 選繭鑰繭壓壓鏇夢蓋製 醖鑰鬱襯願壓廠憲繭醖 (鏇製願窪顧艱網簾膚廠 ) 更多 | - | 2023-06-08 | |||
临床2期 | 23 | Chidamide with azacitidine and CHOP | 願構網築遞積糧夢壓遞(築窪膚獵壓糧鬱獵遞獵) = 衊襯築鑰壓願顧繭醖繭 觸鬱網鑰構獵艱糧淵齋 (醖觸繭艱淵範淵繭鏇餘 ) 更多 | - | 2023-06-08 | ||
临床2期 | 35 | chemotherapy+Chidamide | 範壓簾糧鏇齋簾鹹簾鹽(鹹顧淵鏇鹽鹽廠齋衊範) = 鬱蓋醖鏇夢鬱網範鬱蓋 夢觸齋淵齋衊鏇襯淵觸 (糧鹽艱築積壓鹹壓簾繭, 23.2 ~ 53.7) 更多 | 积极 | 2023-05-31 | ||
临床2期 | 非小细胞肺癌 一线 | 20 | 積淵鏇觸鹽壓淵艱蓋衊(衊餘遞顧選網繭壓築簾) = 鹽蓋遞鑰齋淵襯餘遞鏇 窪顧鏇構鑰衊積廠獵蓋 (蓋範鏇廠齋醖鏇窪網窪, 56.0 ~ 94.0) 更多 | 积极 | 2023-05-31 |
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