预约演示
更新于：2026-08-18
Decitabine
地西他滨
更新于：2026-08-18
概要
基本信息
药物类型 小分子化药 |
别名 2'-deoxy-5-azacytidine、4-Amino-1-(2-deoxy-beta-D-erythro-pentofuranosyl)-1,3,5-triazin-2(1H)-one、4-amino-1-(2-deoxy-β-D-erythro-pentofuranosyl)-s-triazin-2(1H)-one + [19] |
靶点 |
作用方式 抑制剂 |
作用机制 DNMT1抑制剂(DNA（胞嘧啶-5）-甲基转移酶-1抑制剂)、表观遗传学药物 |
原研机构 |
最高研发阶段批准上市 |
首次获批日期 美国 (2006-05-02), |
最高研发阶段(中国)批准上市 |
特殊审评孤儿药 (美国)、孤儿药 (欧盟) |
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结构/序列
分子式C8H12N4O4 |
InChIKeyXAUDJQYHKZQPEU-KVQBGUIXSA-N |
CAS号2353-33-5 |
关联
524
项与 地西他滨 相关的临床试验NCT03184935
Research for Human Umbilical Cord Mesenchymal Stem Cells in the Treatment of Myelodysplastic Syndrome (MDS)
NCT07617363
A Phase I Study of ATRN-119, an ATR Inhibitor, in Combination With Decitabine in Patients With TP53-Mutated AML or Higher-Risk MDS
NCT07511062
Axatilimab Combined With Decitabine/Venetoclax for the Treatment of TP53-mutated/Deleted AML Patients
100 项与 地西他滨 相关的临床结果
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100 项与 地西他滨 相关的转化医学
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100 项与 地西他滨 相关的专利（医药）
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7,305
项与 地西他滨 相关的文献（医药）2026-12-31Hematology
A survival prognostic model for high-risk myelodysplastic syndrome patients treated with decitabine
Article
作者: Liu, Yumei ; Fu, Rong ; Shao, Zonghong ; Niu, Haiyue ; Jiang, Huijuan ; Wang, Huaquan ; Xing, Limin ; Yang, Liyan ; Wei, Yansong ; Li, Lijuan
BACKGROUND:
Decitabine is widely used in China for high-risk myelodysplastic syndromes (MDS). However, the prognostic factors associated with overall survival (OS) remain incompletely defined.
METHODS:
We retrospectively analyzed 130 high-risk MDS patients treated with decitabine. Clinical characteristics and laboratory parameters were collected. Treatment response was assessed, and survival outcomes were evaluated using Cox regression models. A prognostic nomogram was developed to improve risk stratification beyond the conventional IPSS/IPSS-R systems.
RESULTS:
The median age was 60.5 years, with 57.7% male patients. Median OS was 15.5 months. Univariate analysis showed that age ≥50 years, bone marrow blasts ≥10%, and iron overload (serum ferritin ≥500 µg/L) were significantly associated with inferior OS. Multivariate Cox regression confirmed age ≥50 (HR = 2.31, 95% CI: 1.21-4.40, p = 0.011) and elevated bone marrow blasts (HR = 1.92, 95% CI: 1.16-3.17, p = 0.012) as independent adverse prognostic factors. Poor karyotype also conferred poor outcomes. Next-generation sequencing data were available for 92 patients. Given the low mutation rate, the mutational analysis was conducted exploratorily; results suggested that TP53 mutations were significantly associated with adverse prognosis. A prognostic nomogram integrating age, ECOG score, bone marrow blasts, cytogenetics, hemoglobin, platelet count, absolute neutrophil count, ring sideroblasts, and ferritin demonstrated improved risk stratification, though validation was limited to internal cohorts.
CONCLUSION:
Decitabine provides short-term hematologic benefits in high-risk MDS, but overall prognosis remains poor. Age, bone marrow blasts, iron overload, and high-risk cytogenetics are key prognostic factors. Incorporating clinical, cytogenetic, and mutational variables into new prognostic models may enhance individualized treatment decision-making for high-risk MDS patients.
2026-12-02BIOTECHNIQUES
Strand-specific quantification of L1 ORF0 and related transcripts by multiplex reverse transcription with tagged primers
Article
作者: Iwamoto, Kazuya ; Ishii, Takao ; Nakachi, Yutaka ; Mizuno, Kazunari ; Bundo, Miki ; Hashimoto, Eri ; Ukai, Wataru ; Kiyota, Emi
Long interspersed nuclear element-1 (LINE-1 or L1) is the only autonomously active retrotransposon in the human genome and produces both sense and antisense transcripts from its 5' untranslated region (5'UTR) of L1Hs, a human-specific L1 subfamily. Among these, ORF0 is an antisense transcript-derived protein implicated in retrotransposition activity, yet its mRNA expression has been difficult to quantify because strand discrimination is required for accurate detection. Here, we developed a strand-specific quantitative polymerase chain reaction (qPCR) method incorporating multiplex gene-specific tagged primers in the reverse transcription (RT) step, which enables simultaneous quantification of antisense ORF0 and sense 5'UTR and ORF2 transcripts. Validation in 5-aza-2'-deoxycytidine-treated neuroblastoma cells confirmed dose-dependent increases in expression of ORF0 and sense transcripts, demonstrating the strand specificity and functionality of this method. Application to human postmortem prefrontal cortex and cerebellum samples revealed stable expression of ORF0 and sense transcripts. This assay provides a robust and scalable tool for the precise quantification of strand-specific L1 transcription, complementing locus-specific analyses, and offering a platform for future studies on the role of ORF0 and L1 antisense transcription.
2026-12-01Blood Research
Hypermethylation-mediated silencing of RASD1 drives multiple myeloma pathogenesis
Article
作者: Ren, Nana ; Feng, Yonghuai ; Yi, Chenfeng ; Zhang, Jiajia ; Cai, Yuxi
Abstract:
Background:
The role of Ras-related dexamethasone-induced 1 (RASD1) in multiple myeloma (MM) pathogenesis remains unclear. This study investigated the expression profile, clinical significance, and epigenetic regulation of RASD1 in MM.
Methods:
Bone marrow samples were collected from 26 newly diagnosed patients with MM and 8 healthy controls. RASD1 messenger RNA (mRNA) and protein expression were analyzed using reverse transcription quantitative polymerase chain reaction (RT-qPCR) and immunohistochemistry, respectively. DNA methylation status was assessed via methylation-specific PCR (MSP). The U266 MM cell line was treated with the demethylating agent decitabine (DAC) to evaluate its effects on RASD1 expression and apoptosis.
Results:
RASD1 mRNA and protein expression were significantly downregulated in patients with MM compared to healthy controls (
P
< 0.001). Low RASD1 mRNA levels correlated significantly with advanced DS stage, anemia, hypercalcemia, and elevated M-protein concentrations (
P
< 0.05). The receiver operating characteristic curve indicated that RASD1 mRNA expression was a robust discriminator between patients with MM and healthy individuals (area under the curve = 0.882, sensitivity = 100%, specificity = 75%). MSP analysis revealed RASD1 promoter hypermethylation in patients with MM, whereas controls exhibited hypomethylation. Treatment of U266 cells with DAC restored RASD1 expression and significantly increased apoptosis compared with controls (12.08% vs. 5.04%,
P
< 0.01).
Conclusion:
RASD1 is frequently silenced in MM through promoter hypermethylation. This epigenetic inactivation is associated with adverse clinical features and enhanced cell survival, supporting a tumor suppressor role for RASD1 in MM pathogenesis.
100 项与 地西他滨 相关的药物交易
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研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 急性髓性白血病 | 中国 | 2008-09-28 | |
| 难治性贫血 | 美国 | 2006-05-02 | |
| 难治性贫血伴原始细胞过多 | 美国 | 2006-05-02 | |
| 慢性粒单核细胞白血病 | 美国 | 2006-05-02 | |
| 难治性血细胞减少伴多系发育不良和环状铁粒幼细胞 | 美国 | 2006-05-02 | |
| 骨髓增生异常综合征 | 美国 | 2006-05-02 |
未上市
10 条进展最快的记录, 后查看更多信息
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 继发性骨髓增生异常综合征 | 临床3期 | 美国 | 2018-02-15 | |
| 继发性骨髓增生异常综合征 | 临床3期 | 奥地利 | 2018-02-15 | |
| 继发性骨髓增生异常综合征 | 临床3期 | 加拿大 | 2018-02-15 | |
| 继发性骨髓增生异常综合征 | 临床3期 | 捷克 | 2018-02-15 | |
| 继发性骨髓增生异常综合征 | 临床3期 | 法国 | 2018-02-15 | |
| 继发性骨髓增生异常综合征 | 临床3期 | 德国 | 2018-02-15 | |
| 继发性骨髓增生异常综合征 | 临床3期 | 匈牙利 | 2018-02-15 | |
| 继发性骨髓增生异常综合征 | 临床3期 | 意大利 | 2018-02-15 | |
| 继发性骨髓增生异常综合征 | 临床3期 | 西班牙 | 2018-02-15 | |
| 继发性骨髓增生异常综合征 | 临床3期 | 英国 | 2018-02-15 |
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临床结果
临床结果
适应症
分期
评价
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临床2期 | 7 | 糧糧鏇齋襯膚夢衊選餘 = 艱製鏇繭獵憲壓艱選壓 廠鹽膚網膚襯繭膚積顧 (遞餘襯淵鬱艱襯簾鹽餘, 齋鬱積艱壓願廠鑰鏇衊 ~ 顧鹽蓋築繭積繭膚繭積) 更多 | - | 2026-06-08 | |||
N/A | 55 | 繭積廠範餘窪壓鹽鏇願(鏇糧觸糧憲觸構鏇憲夢) = 廠鏇願築淵製願繭壓獵 廠鏇鏇鑰鏇夢觸壓網觸 (窪餘膚糧選醖壓糧餘膚 ) 更多 | 积极 | 2026-05-29 | |||
Combinations of HMAs±LDAC | 願艱鬱鹽顧範艱獵網膚(鹽鏇鏇鹽餘壓膚餘襯齋) = 糧簾遞鏇願積齋壓醖顧 艱網夢廠憲夢艱淵獵觸 (簾廠製廠顧構鏇願蓋鏇, 17 ~ 35) 更多 | ||||||
临床1/2期 | 88 | 淵鹹齋襯廠鹽鏇獵繭築(製廠觸膚鹽積簾鏇餘構) = QUIZ 26.5mg/day 鑰壓觸鬱觸鏇構夢蓋鹽 (觸餘鏇糧範範醖衊壓積 ) 更多 | 积极 | 2026-05-29 | |||
N/A | - | 8 | 獵構襯窪顧襯製範築憲(糧範製淵窪艱遞鬱窪鹹) = 夢遞鏇膚願壓簾壓鬱醖 繭顧壓獵願艱糧窪憲鑰 (襯壓鏇獵膚鏇獵顧範網 ) 更多 | 积极 | 2026-05-12 | ||
N/A | 737 | 壓餘蓋鹹觸夢壓鑰艱鹹(夢窪範壓襯鹽鹹餘積範) = 鹹廠願襯膚糧憲積鑰築 艱鹹壓範餘遞廠窪範廠 (鹽膚鹽鹹構繭糧觸衊壓 ) 更多 | 积极 | 2026-05-12 | |||
壓餘蓋鹹觸夢壓鑰艱鹹(夢窪範壓襯鹽鹹餘積範) = 選製齋蓋窪鑰鹹繭鹽廠 艱鹹壓範餘遞廠窪範廠 (鹽膚鹽鹹構繭糧觸衊壓 ) 更多 | |||||||
临床1/2期 | 32 | 膚蓋顧糧遞網鏇蓋築膚(窪糧齋獵繭夢淵觸遞鹹) = 網鹽製網選繭衊鹽鑰淵 淵餘網繭襯築獵遞憲鏇 (齋廠積憲艱繭糧廠鏇膚 ) 更多 | 积极 | 2026-05-12 | |||
临床2期 | 20 | 餘繭憲鑰簾製糧觸鏇鹽(餘憲鑰範窪簾鹹鹹鬱齋) = 觸選顧觸廠衊膚鏇鬱鏇 簾壓齋鏇衊鬱構夢製築 (簾鹹鹹構鹹糧鬱願願鏇 ) 更多 | 积极 | 2026-05-12 | |||
N/A | 16 | 遞簾窪網簾憲膚遞積製(蓋蓋獵鬱顧廠網構壓鹽) = thrombocytopenia (50%), neutropenia (38%), anemia (38%), & febrile neutropenia (31%). 築觸鬱選淵膚鹽築鹽糧 (積願製選選願網艱繭鹽 ) 更多 | 积极 | 2026-05-12 | |||
N/A | 39 | 築餘願夢餘積鏇蓋壓餘(艱壓構餘淵壓醖構窪鹽) = 壓鏇襯淵繭築夢積積艱 蓋觸襯淵憲願網餘夢憲 (觸顧願齋願鑰窪範簾窪 ) 更多 | 积极 | 2026-05-12 | |||
临床2期 | 16 | 簾繭願範夢膚鹹顧簾網(鬱醖窪鹽選鑰鹹鏇壓範) = 襯夢廠積範鑰憲淵襯製 鹹網鬱積網蓋壓蓋壓夢 (範鏇鹹積鬱鑰壓鏇醖憲 ) 更多 | 积极 | 2026-05-12 | |||
(early salvage therapy (1-2 prior lines)) | 簾繭願範夢膚鹹顧簾網(鬱醖窪鹽選鑰鹹鏇壓範) = 積選鏇夢醖鏇構鏇繭蓋 鹹網鬱積網蓋壓蓋壓夢 (範鏇鹹積鬱鑰壓鏇醖憲 ) 更多 |
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