更新于：2024-04-26
Azacitidine
阿扎胞苷
更新于：2024-04-26
概要
基本信息
药物类型 小分子化药 |
别名 4-amino-1-beta-D-ribofuranosyl-s-triazin-2(1H)-one、5-azacytidine、Aza-C + [20] |
靶点 |
作用机制 DNMT1抑制剂(DNA（胞嘧啶-5）-甲基转移酶-1抑制剂)、DNA甲基化抑制剂 |
在研适应症 |
非在研适应症 |
原研机构 |
最高研发阶段批准上市 |
首次获批日期 美国 (2004-05-19), |
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)、孤儿药 (日本)、加速审评 (欧盟) |
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结构
分子式C8H12N4O5 |
InChIKeyNMUSYJAQQFHJEW-KVTDHHQDSA-N |
CAS号320-67-2 |
关联
781
项与 阿扎胞苷 相关的临床试验A Phase Ib/II, Open Label, Proof-of-concept Study of Sabatolimab and Magrolimab-based Therapy for Patients With Acute Myeloid Leukemia or Myelodysplastic Syndrome
Study of Cladribine+Venetoclax After Failure of Venetoclax+Hypomethylating Agent in Monocytic AML
Phase I Study of HC-7366 With Azacitidine and Venetoclax for Acute Myeloid Leukemia
100 项与 阿扎胞苷 相关的临床结果
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100 项与 阿扎胞苷 相关的转化医学
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100 项与 阿扎胞苷 相关的专利（医药）
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5,923
项与 阿扎胞苷 相关的文献（医药）2106-07-05Oncotarget
Luminal STAT5 mediates H2AX promoter activity in distinct population of basal mammary epithelial cells
Article
作者: Barash, Itamar ; Reichenstein, Moshe ; Kisliouk, Tatiana ; Kfir, Shenhav ; Rauner, Gat
Deregulated STAT5 activity in the mammary gland causes parity-dependent tumorigenesis. Epithelial cell cultures transfected with constitutively active STAT5 express higher levels of the histone H2AX than their non-transfected counterparts. Higher H2AX expression may be involved in tumorigenesis. Here, we aimed to link high STAT5 activity to H2AX-GFP expression by looking for distinct types of mammary cells that express these proteins. In vitro and in transgenic mice, only 0.2 and 0.02%, respectively, of the cells expressed the H2AX-GFP hybrid gene. Its expression correlated with that of the endogenous H2AX gene, suggesting that detectable H2AX-GFP expression marks high levels of H2AX transcript. Methylation of the H2AX promoter characterized non-GFP-expressing H2AX-GFP cells and was inversely correlated with promoter activity. Administration of 5-azacytidine increased H2AX promoter activity in an activated STAT5-dependent manner. In transgenic mice, H2AX-GFP expression peaked at pregnancy. The number of H2AX-GFP-expressing cells and GFP expression decreased in a Stat5a-null background and increased in mice expressing the hyperactivated STAT5. Importantly, H2AX-GFP activity was allocated to basal mammary cells lacking stem-cell properties, whereas STAT5 hyperactivity was detected in the adjacent luminal cells. Knockdown of RANKL by siRNA suggested its involvement in signaling between the two layers. These results suggest paracrine activation of H2AX via promoter demethylation in specific populations of basal mammary cells that is induced by a signal from neighboring luminal cells with hyper STAT5 activity. This pathway provides an alternative route for the luminally confined STAT5 to affect basal mammary cell activity.
2024-12-31Hematology
Reduced duration and dosage of venetoclax is efficient in newly diagnosed patients with acute myeloid leukemia
Article
作者: Yan, Qiong ; Cui, Jingying ; Yuan, Guolin ; Chen, Xuexing ; Li, Chunfang
OBJECTIVES:
The combination of Venetoclax (VEN) and Azacitidine (AZA) increases survival outcomes and yields excellent responses in patients with acute myeloid leukemia (AML). However, dose reduction (or discontinuation) is commonly encountered due to therapy-related toxicity. Thus, this study aimed to investigate the efficiency and safety of a lower dosage of venetoclax for the treatment of AML.
METHODS:
This observational study analyzed the characteristics and outcomes of newly diagnosed AML patients who received 100 mg VEN combined with AZA for 14 days at our institution.
RESULTS:
A total of 36 patients were enrolled, and the median age at diagnosis was 64 years. After a median follow-up of 15 (range 4-29) months, the median overall survival (OS) and progression-free survival (PFS) for the whole cohort were 17 (4-29) months and 12 (1-28) months, respectively. Meanwhile, the overall response rate (ORR) was 69.4%, and the CRc rate was 66.7% in the whole cohort. Subgroup analysis revealed that NPM1 mutations and FAB-M5 subtype were associated with higher response rates, whereas the adverse ELN risk group was predictive of an inferior response. Moreover, ASXL1, NPM1, and IDH1/2 mutations negatively impacted PFS.
DISCUSSION:
Our study optimized the administration of venetoclax plus azacytidine for the treatment of AML patients. Response rates were favorable, with median survival in agreement with the findings of earlier reports, offering valuable insights for optimizing VEN-based regimens.
CONCLUSION:
In summary, the VEN combination regimen is effective for the treatment of newly diagnosed AML patients in the real world despite VEN dose reductions .
2024-12-31Hematology
Case report: Venetoclax plus Azacitidine in treatment of acute undifferentiated leukemia
Review
作者: Chen, Lin ; Mi, Ruihua ; Wei, Xudong ; Wang, Lin ; Cui, Yu ; Li, Dongbei
OBJECTIVES:
Acute undifferentiated leukemia (AUL) is a clinical rare leukemia with an overall poor prognosis. Currently, there are no well-established treatment guidelines for AUL, further exploration of optimal treatment options is now required.
METHODS:
We report an AUL patient who was complicated by a NRAS mutation and del5q was admitted to our hospital and we present the clinical features. In addition, we conducted a literature review.
RESULTS:
The "VA" scheme combines agents Venetoclax and Azacitidine that have synergistic therapeutic effect with a tolerable safety profile. There is no previous report of the "VA" scheme employed in AUL treatment. An AUL patient who was complicated by a NRAS mutation and del5q was admitted to our hospital. The "VA" scheme was administrated, and complete remission (CR) was achieved at the end of the first cycle. The patient then underwent HLA-identical sibling allogeneic hematopoietic stem cell transplantation.
DISCUSSION:
The "VA" scheme has been extensively used in AML treatment, but its application in AUL treatment has not yet been reported. This study is the first to report an AUL patient treated with the "VA" scheme and achieved CR. Our result preliminarily suggested the effectiveness and safety of the "VA" scheme in AUL treatment, but validation is required in more clinical samples. The "VA" scheme provides a new treatment option for AUL patients and deserves further clinical promotion.
782
项与 阿扎胞苷 相关的新闻（医药）2024-04-26
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2024-04-26
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2024-04-25
ASCO会议临床结果
100 项与 阿扎胞苷 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 |
|---|---|---|---|
| 急性髓性白血病 | 批准上市 | 挪威 更多 | |
| 慢性粒单核细胞白血病 | 批准上市 | 欧盟 更多 | |
| 骨髓增生异常综合征 | 批准上市 | 美国 更多 | |
| 血小板减少症 | 临床3期 | 希腊 更多 | |
| 输血依赖性贫血 | 临床3期 | 意大利 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
N/A | 14 | Arm A (AZA + ATRA) | 鏇鑰鑰淵糧積鏇繭淵選(遞鬱鏇艱構鑰糧衊鬱選) = 壓淵餘鏇願構構蓋窪壓 構齋鬱衊淵鑰顧襯窪糧 (憲膚窪簾蓋遞積窪淵構 ) 更多 | 积极 | 2024-04-05 | ||
鏇鑰鑰淵糧積鏇繭淵選(遞鬱鏇艱構鑰糧衊鬱選) = 蓋餘鑰遞鹽糧繭顧淵獵 構齋鬱衊淵鑰顧襯窪糧 (憲膚窪簾蓋遞積窪淵構 ) 更多 | |||||||
临床1期 | 复发性急性髓细胞白血病 MCL-1 | NOXA | pro-apoptotic BCL2 family members | 16 | 廠蓋壓積夢醖顧衊壓鏇(膚築鬱範製願齋觸衊鑰) = 窪鬱艱襯鑰鏇顧衊壓顧 廠壓衊醖衊選願壓選範 (窪艱艱壓艱鑰網廠淵積 ) 更多 | 积极 | 2024-04-04 | ||
廠蓋壓積夢醖顧衊壓鏇(膚築鬱範製願齋觸衊鑰) = 壓顧鹽廠鏇簾築顧壓齋 廠壓衊醖衊選願壓選範 (窪艱艱壓艱鑰網廠淵積 ) 更多 | |||||||
临床2期 | 急性髓性白血病 维持 | 35 | Azacitidine 50 mg/m2 + Venetoclax 400 mg (7 days) | 餘醖膚簾遞衊糧鹹憲鹽(願夢鹹廠願積願齋鬱鹹) = 衊糧繭衊鹽壓範積鹹淵 獵選鹹遞範繭鏇獵選築 (襯憲鹽築窪窪淵顧膚夢, 20.2 ~ not calculable) | - | 2024-04-01 | |
临床2期 | 51 | Sorafenib plus venetoclax, azacitidine, and homoharringtonine (VAH) | 壓鏇顧糧蓋艱製選遞範(鹽願製鹽糧蓋鬱製糧壓) = 壓遞醖獵遞糧廠鏇遞齋 壓壓廠繭鬱獵廠繭範壓 (構範範積糧齋鹽繭鑰齋 ) 更多 | 积极 | 2024-02-01 | ||
临床1/2期 | - | Azacitidine, Venetoclax, and Gilteritinib | 夢蓋壓膚襯醖鹹積願鬱(選簾網夢顧糧簾觸鹹簾) = 壓築鑰憲鑰窪餘鹹築觸 範醖襯遞築製觸鏇鹹鏇 (膚築鏇鬱選膚願遞範壓 ) | 积极 | 2024-01-26 | ||
临床1/2期 | 急性髓性白血病 IDH2-mutant | - | 範窪夢齋齋簾繭遞鑰築(鑰齋淵壓網鹽繭夢遞餘) = 廠顧膚願餘鏇膚淵構鬱 齋夢壓糧鬱鑰製艱齋淵 (鹽鹹範鏇範繭觸築選窪 ) | - | 2024-01-23 | ||
Enasidenib + Azacitidine combination therapy | 範窪夢齋齋簾繭遞鑰築(鑰齋淵壓網鹽繭夢遞餘) = 餘餘夢網窪壓醖製範醖 齋夢壓糧鬱鑰製艱齋淵 (鹽鹹範鏇範繭觸築選窪 ) | ||||||
临床2期 | 急性髓性白血病 巩固 | 123 | CLAD-LDAC-Ven | 簾鹹醖鬱鬱淵鹽製鹽願(鹽鹹鑰壓壓觸憲範觸壓) = 構襯鹽衊鏇鑰構壓製鑰 構遞憲觸範膚鏇繭簾構 (鬱夢膚構鹹憲鹽醖蓋壓 ) 更多 | - | 2023-12-11 | |
N/A | - | 廠窪壓獵網網壓醖鏇遞(選築醖積遞憲製遞齋廠) = 觸遞憲壓壓製獵簾憲憲 構選淵壓繭鹹簾獵簾鑰 (製廠齋網鑰積遞製積衊 ) 更多 | - | 2023-12-11 | |||
临床2期 | 41 | 築製衊鹽糧獵觸襯簾觸(遞廠壓鑰淵網積艱壓簾) = 願獵觸鬱簾夢艱簾齋鏇 夢淵鏇鬱糧衊憲構範廠 (鑰餘醖衊網網齋製蓋壓 ) 更多 | - | 2023-12-11 | |||
N/A | 髓系肿瘤 维持 | - | 衊觸鹽築淵鬱鹹醖齋憲(憲觸窪襯鹹顧積鏇範選) = 壓網鑰鏇蓋範鬱憲積願 顧繭鏇壓積壓願淵顧衊 (選鑰鑰鹹蓋製製齋鹽鹽 ) 更多 | - | 2023-12-11 |
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