预约演示
更新于：2025-12-17
Acipimox
阿昔莫司
更新于：2025-12-17
概要
基本信息
原研机构 |
在研机构 |
非在研机构- |
权益机构- |
最高研发阶段批准上市 |
首次获批日期 意大利 (1985-01-01), |
最高研发阶段(中国)批准上市 |
特殊审评- |
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结构/序列
分子式C6H6N2O3 |
InChIKeyDJQOOSBJCLSSEY-UHFFFAOYSA-N |
CAS号51037-30-0 |
关联
56
项与 阿昔莫司 相关的临床试验CTR20254277
一项评估ACIERT缓释片在健康成年研究参与者中的相对生物利用度的IA期临床研究
CTR20252319
阿昔莫司胶囊空腹及餐后人体生物等效性研究
CTR20244698
阿昔莫司胶囊空腹及餐后人体生物等效性研究
100 项与 阿昔莫司 相关的临床结果
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100 项与 阿昔莫司 相关的转化医学
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100 项与 阿昔莫司 相关的专利（医药）
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356
项与 阿昔莫司 相关的文献（医药）2025-12-01Advanced Science
Dynamic Arginine Methylation of YBX1 Relay Controls Its Phase Separation and Chemoradiotherapy Resistance in Rectal Cancer
Article
作者: Yunxing Shi ; Shuanglin Luo ; Liang Huang ; Ziwei Zeng ; Taixuan Wan ; Shaoru Liu ; Huashan Liu ; Yunfei Yuan ; Wenxin Li ; Li Xiong ; Zhenxing Liang ; Liang Kang
Abstract:
Although neoadjuvant chemoradiotherapy is the standard treatment and significantly improves prognosis of locally advanced rectal cancer, patients may develop primary or secondary therapy resistance. Here, through functional screening, we identify PRMT3 as a key driver of chemoradiotherapy resistance in rectal cancer. PRMT3 induces the arginine methylation of Y‐box binding protein 1 (YBX1), which suppresses YBX1's capacity for phase separation in cytoplasm and is imperative for its nucleus translocation. Subsequently, lysine‐specific demethylase 4A (KDM4A) demethylates YBX1 to unmask the R247 residue and promote its phase separation in the nucleus, which strengthens its ability to transcriptionally regulate expressions of ATP‐binding cassette (ABC) transporters and homologous recombination (HR) repair genes and reinforces chemoradiotherapy resistance. Of particular translational importance, high‐throughput FDA‐approved drugs library screening identifies acipimox as a potent PRMT3 inhibitor and chemoradiotherapy sensitizer. This study offers a tangible prospect for improving therapeutic outcomes in rectal cancer patients in a clinically relevant setting.
2025-08-29MEDICINE
Severe drug-induced liver injury from acipimox and telmisartan co-administration: A case report and review of literature
Review
作者: Liu, Dan ; Liu, Shu
Rationale::
Drug-induced liver injury (DILI) is a prevalent and critical etiology of acute liver failure that often results in substantial health complications and mortality. Acipimox is a pharmacological agent used for lipid reduction, whereas telmisartan is prescribed for hypertension management. We report a case of severe DILI attributed to the concomitant use of acipimox and telmisartan, and we analyze the potential underlying mechanisms.
Patient concerns::
A 58-year-old female was admitted to our hospital with anorexia lasting >6 months. The patient had a history of taking oral antihypertensive medication (telmisartan) and lipid-lowering medications (atorvastatin and acipimox), with suspected DILI.
Diagnoses::
The patient was diagnosed with DILI.
Interventions::
After discontinuation of the suspected hepatotoxic agents telmisartan and acipimox, the patient received anti-inflammatory therapy with glucocorticoids along with hepatoprotective treatment including glutathione, S-adenosylmethionine, and bicyclol.
Outcomes::
The patient’s liver function has substantially normalized.
Lessons::
This study is the first to highlight a significant case of severe liver injury resulting from concurrent administration of acipimox and telmisartan, which is potentially influenced by factors such as age, sex, drug interactions, and genetic polymorphisms. This study aimed to emphasize the significance of implementing precise and individualized treatment strategies for managing drug combinations for patients with multiple comorbidities.
2025-08-01ADVANCED FUNCTIONAL MATERIALS
Coordination‐Dissociation Induced T1‐Weighted Magnetic Resonance Imaging Responses in a spn‐Type MOF for Potential Drug Release Monitoring
作者: Chen, Zhenxia ; Gong, Yimin ; Wu, Tianze ; Yang, Yannan ; Zhou, Yaming ; Weng, Jingting ; Ling, Yun ; Qiu, Tianze ; Luo, Dan ; Yin, Bo ; Li, Jianing
Abstract:
Developing novel nanoplatforms capable of monitoring drug release by identifiable magnetic resonance imaging (MRI) responses is a great promising yet challenging task. Here, a novel isoreticular chemistry strategy is introduced to enable a spn‐type metal–organic framework (MOF) with T1‐weighted MRI turned‐on response to the drug release via a coordination‐dissociation process. Post‐synthetic functionalization endows the structure with a high longitudinal relaxivity r1 of 12.63 mm−1 s−1 as well as abundant accessible coordination sites to catch carboxylate probes and drugs. Mechanism studies reveal a size‐dependent decrease in relaxivity as the coordinated carboxylate probes increase in size, with bulk benzoic acid showing the largest identifiable reduction at 71%. In vitro model studies further validate the MRI signals response respectively by coordinating four drugs with aromatic carboxylate groups. Finally, in vivo experiments confirm the feasibility of using this coordination‐dissociation‐induced MRI response to monitor drug release. This proof‐of‐principle study demonstrates a practical pathway for designing MOF‐based nanoplatforms for responsive MRI, paving the way for enhanced non‐invasive drug monitoring techniques.
100 项与 阿昔莫司 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 |
|---|---|---|---|
| 家族性高胆固醇血症 | 英国 | 2003-05-02 | |
| IV型高脂蛋白血症 | 英国 | 2003-05-02 | |
| 高胆固醇血症 | 中国 | 1994-06-03 | |
| 高甘油三酯血症 | 中国 | 1994-06-03 | |
| 高脂血症 | 意大利 | 1985-01-01 |
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 |
|---|---|---|---|---|
| IIb型高脂蛋白血症 | 临床1期 | 中国 | 2025-11-06 | |
| 2型糖尿病 | 临床阶段不明 | 美国 | 2011-06-01 |
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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3期 | 28 | (T1 Diabetes, Acipimox) | 鬱夢鏇構構憲夢齋廠遞(淵鏇襯願獵構觸簾壓鹹) = 窪鏇選鬱糧憲選齋齋鹹 壓繭齋獵艱繭襯顧繭齋 (鏇鬱觸膚製繭衊構艱顧, 1.52) 更多 | - | 2022-01-21 | ||
placebo (T1 Diabetes, Placebo) | 鬱夢鏇構構憲夢齋廠遞(淵鏇襯願獵構觸簾壓鹹) = 構窪構簾壓淵願鬱艱鏇 壓繭齋獵艱繭襯顧繭齋 (鏇鬱觸膚製繭衊構艱顧, 1.45) 更多 | ||||||
N/A | 13 | (Acipimox) | 衊簾鹹鹽鹽蓋艱觸製積(壓獵繭網觸範遞構觸遞) = 鏇醖選構廠鬱繭網積窪 齋蓋鹽壓夢醖夢襯憲襯 (鑰夢簾鏇鹹醖繭醖遞蓋, 16.9) 更多 | - | 2021-12-03 | ||
Placebo (Placebo) | 衊簾鹹鹽鹽蓋艱觸製積(壓獵繭網觸範遞構觸遞) = 齋構願餘齋選觸獵壓廠 齋蓋鹽壓夢醖夢襯憲襯 (鑰夢簾鏇鹹醖繭醖遞蓋, 11.8) 更多 | ||||||
N/A | - | 鹹獵範鏇鹽觸糧廠糧鹽(蓋繭淵遞齋淵築鏇鏇獵) = 壓窪憲遞夢遞鏇製淵餘 鬱壓糧襯繭願壓衊糧選 (襯醖願廠網壓繭範齋淵 ) 更多 | - | 2017-12-01 | |||
Placebo | 鹹獵範鏇鹽觸糧廠糧鹽(蓋繭淵遞齋淵築鏇鏇獵) = 鏇積廠夢夢齋觸鑰糧構 鬱壓糧襯繭願壓衊糧選 (襯醖願廠網壓繭範齋淵 ) 更多 | ||||||
临床2/3期 | 8 | (Acipimox+) | 衊觸願繭願網網築繭繭(鬱艱構鏇糧網廠製蓋鹽) = 選觸鹽鹽齋製鬱齋蓋簾 夢遞憲醖淵繭齋蓋膚構 (獵膚築憲艱鹽鏇鏇觸遞, 0.1) 更多 | - | 2017-04-04 | ||
Placebo Oral Capsule (Placebo) | 衊觸願繭願網網築繭繭(鬱艱構鏇糧網廠製蓋鹽) = 鏇壓獵獵簾夢襯壓顧艱 夢遞憲醖淵繭齋蓋膚構 (獵膚築憲艱鹽鏇鏇觸遞, 0.1) 更多 | ||||||
临床2期 | 39 | (Acipimox) | 構鏇齋觸鬱淵繭構衊鹽(淵範鏇鏇襯構衊遞艱觸) = 繭艱衊構糧鏇膚襯鑰網 願窪觸構遞積獵願鹽顧 (餘獵鹽餘選壓襯鑰鑰壓, 9.6) 更多 | - | 2016-02-03 | ||
Placebo (Placebo) | 構鏇齋觸鬱淵繭構衊鹽(淵範鏇鏇襯構衊遞艱觸) = 鑰蓋夢繭衊壓鏇顧艱衊 願窪觸構遞積獵願鹽顧 (餘獵鹽餘選壓襯鑰鑰壓, 10.8) 更多 | ||||||
N/A | 23 | 鏇餘憲廠襯簾構網襯鏇(窪窪遞膚鹽憲鑰築壓鏇) = 膚製襯鬱膚憲夢蓋鬱醖 鹹製醖網鬱窪淵鹹築獵 (壓壓淵廠築膚醖餘鬱遞 ) 更多 | - | 2006-11-01 | |||
Placebo | 鏇餘憲廠襯簾構網襯鏇(窪窪遞膚鹽憲鑰築壓鏇) = 構築願願繭醖簾憲願遞 鹹製醖網鬱窪淵鹹築獵 (壓壓淵廠築膚醖餘鬱遞 ) 更多 |
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