更新于：2024-12-21
Bortezomib
硼替佐米
更新于：2024-12-21
概要
基本信息
药物类型 小分子化药 |
别名 [(1R)-3-methyl-1-({(2S)-3-phenyl-2-[(pyrazin-2-ylcarbonyl)amino]propanoyl}amino)butyl]boronic acid、Bortezomib (JAN/USAN/INN)、N-[(1R)-1-(DIHYDROXYBORYL)-3-methylbutyl]-N-(pyrazin-2-ylcarbonyl)-L-phenylalaninamide + [16] |
作用机制 蛋白酶体抑制剂 |
在研适应症 |
非在研适应症 |
最高研发阶段批准上市 |
首次获批日期 美国 (2003-05-13), |
最高研发阶段(中国)批准上市 |
特殊审评加速批准 (美国)、孤儿药 (欧盟)、孤儿药 (日本)、孤儿药 (美国) |
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结构
分子式C19H25BN4O4 |
InChIKeyGXJABQQUPOEUTA-RDJZCZTQSA-N |
CAS号179324-69-7 |
关联
1,080
项与 硼替佐米 相关的临床试验An Interventional, Prospective Open-Label Study of Immunosuppressive Therapies to Mitigate Immune-Mediated Loss of Therapeutic Response to Asfotase Alfa (STRENSIQ®) for Hypophosphatasia (RESTORE)
A Single Arm, Response-adapted, Open Label Study of Iberdomide, Weekly Bortezomib and Dexamethasone (IberBd) With Isatuximab Added on Demand for Transplant-ineligible, Newly Diagnosed Multiple Myeloma Patients: the BOREALIS Trial
SJALL23T: Adding Dasatinib Or Venetoclax To Improve Responses In Children With Newly Diagnosed T-Cell Acute Lymphoblastic Leukemia (ALL) Or Lymphoma (T-LLY) Or Mixed Phenotype Acute Leukemia (MPAL)
100 项与 硼替佐米 相关的临床结果
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100 项与 硼替佐米 相关的转化医学
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100 项与 硼替佐米 相关的专利（医药）
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10,243
项与 硼替佐米 相关的文献（医药）2025-03-01CELLULAR SIGNALLING
tRNA methyltransferase DNMT2 promotes hepatocellular carcinoma progression and enhances Bortezomib resistance through inhibiting TNFSF10
Article
作者: Lai, Junzhong ; Li, Xinxin ; Chen, Zhirong ; Liang, Jiadi ; Chen, Xiaolan ; Lin, Jizhen ; Zhang, Yong ; Zhao, Heng ; Tian, Ling ; Chen, Qi ; Li, Qiumei ; Guo, Dong ; Chen, Linqin ; Zhao, Guangjian ; Fan, Jiqiang
The tRNA methyltransferase DNMT2 (TRDMT1) plays a crucial role in various biological functions; however, its role in cancer, particularly in liver cancer, remains incompletely understood. In this study, we demonstrate that high DNMT2 expression is negatively correlated with prognosis in clinical liver cancer patients. A series of in vitro and in vivo experiments showed that DNMT2 promotes the proliferation, colony formation, and metastasis of hepatocellular carcinoma cells. We identified the pro-apoptotic gene TNFSF10 (TRAIL) as a downstream target of DNMT2, regulated by the N6-methyladenosine (m6A) demethylase FTO. Epigenetically, DNMT2 deletion increased FTO expression, leading to a reduction in m6A methylation levels. FTO upregulated TNFSF10 expression, significantly reducing the proliferation and metastasis of DNMT2-deficient hepatocellular carcinoma cells. Furthermore, DNMT2 deletion was shown to significantly upregulate chemokine expression in tumors. Finally, we demonstrated that the NF-κB inhibitor Bortezomib further enhances DNMT2 deletion-induced apoptosis in hepatocellular carcinoma cells. This study reveals DNMT2's role in liver cancer and presents a new therapeutic target for future treatments.
2025-02-01JOURNAL OF NEUROIMMUNOLOGY
A complex and severe encephalitis associated with four co-existing neuronal cell-surface autoantibodies
Article
作者: Westbrook, Andrew ; Farrell, Michael ; McGuigan, Christopher ; Gilligan, Michael ; Waters, Patrick ; Connolly, Sean ; Irani, Sarosh R ; O'Donnell, Luke ; Kinsella, Justin A ; Riordan, Sean 'o ; Tubridy, Niall
Many forms of autoimmune encephalitis are mediated by neuronal cell-surface directed autoantibodies. The co-occurrence of four neuronal cell-surface antibodies in a single patient is exceptionally rare. We report a patient who had a severe encephalitis associated with antibodies to NMDA, Glycine, GABAA and GABAB receptors. Case: A 28-year-old man on tacrolimus presented with a first seizure. Thereafter, he developed confusion, cerebellar signs, opsoclonus, neuromyotonia and medication-refractory seizures. CSF sampling revealed 826 white cells and NMDA, glycine and GABAB receptor antibodies: all were also detected in serum along with additional GABAA receptor antibodies. Neural antibodies were detected using fixed (NMDA, GABAA, GABAB receptor) or live (glycine receptor) cell-based assays at Oxford Neuroimmunology Laboratory, Oxford, UK. MRI brain demonstrated cerebellar leptomeningeal enhancement and a hyperintense lesion in the cerebellar vermis. EEG revealed extreme delta brush and needle EMG confirmed neuromyotonia. No underlying malignancy was detected. Methylprednisolone, IVIG, Rituximab, therapeutic plasma exchange, cyclophosphamide and bortezomib were administered sequentially, with minimal clinical improvement. Death secondary to respiratory sepsis occurred on the 714th hospital day. Postmortem revealed pan-cerebellar atrophy with Purkinje cell loss; dentate nucleus ganglionopathy, and thoracolumbar cord myelopathy. In summary, the detection of multiple neuronal cell-surface antibodies in autoimmune encephalitis is unusual and may result in a complex overlap syndrome with a poor response to immunotherapy.
2025-01-01TALANTA
Design of a molecularly imprinted polymer sensor modified with saffron-based copper nanoflowers for highly selective and sensitive determination of bortezomib
Article
作者: Baldemir Kilic, Ayse ; Atici, Esen Bellur ; Kaya, S Irem ; Yusufbeyoglu, Sadi ; Cetinkaya, Ahmet ; Kilic, Ayse Baldemir ; Ozkan, Sibel A ; Ozkan, Sibel A. ; Kaya, S. Irem
This work represents the first successful application of a molecularly imprinted polymer (MIP)-based electrochemical sensor for the sensitive and selective determination of the first developed proteasome inhibitor, bortezomib (BOR). BOR is used for the treatment of multiple myeloma, gastrointestinal stromal tumors, and mantle cell lymphoma. It shows its desired effect through the boronate group and can be administered intravenously or subcutaneously. The MIP-based electrochemical sensor design includes the integration of green-synthesized saffron-based copper nanoflowers (CuNFs) from Crocus sativus L. to increase the active surface area and porosity of the glassy carbon electrode (GCE) surface. 2-Acrylamido-2-methyl-1-propanesulfonic acid (AMPS) was selected as the functional monomer along with other MIP components. Detailed characterizations of the developed CuNFs/AMPS/MIP-GCE sensor and CuNFs were performed using scanning electron microscopy (SEM), X-ray diffraction (XRD), Fourier transform infrared spectroscopy (FTIR), energy dispersive X-ray analysis (EDX), cyclic voltammetry (CV), and electrochemical impedance spectroscopy (EIS). The indirect measurement approach using 5.0 mM [Fe(CN)6]3-/4- solution was used to determine BOR in the linear range of 2.5 × 10-13 M - 2.5 × 10-12 M (0.25-2.5 pM). The LOD and LOQ values of the sensor obtained at the fM level (29 fM and 96.7 fM), which has a linear response in the commercial human serum sample in the same concentration range, emphasize its sensitivity (1.89 × 1013 and 2.14 × 1013 μA/M for standard solution and serum). The repeatability and reproducibility of the sensor were between 0.87 % and 2.17 %, showing its reliability. The successful performance of the sensor in the presence of metabolites belonging to BOR demonstrates its unique selectivity. The selectivity was demonstrated via relative imprinting factor (IF') values (higher than 3.5) against BOR's metabolites. The stability of the CuNFs/AMPS/MIP-GCE sensor was found to be 5 days.
737
项与 硼替佐米 相关的新闻（医药）2024-12-20
·摩熵医药
上市批准免疫疗法细胞疗法抗体药物偶联物
2024-12-18
·摩熵医药
免疫疗法细胞疗法临床研究
2024-12-17
生物类似药临床3期财报上市批准
100 项与 硼替佐米 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 |
|---|---|---|---|
| 免疫球蛋白轻链淀粉样变性 | 日本 | 2006-10-20 | |
| 巨球蛋白血症 | 日本 | 2006-10-20 | |
| 套细胞淋巴瘤 | 欧盟 | 2004-04-26 | |
| 套细胞淋巴瘤 | 冰岛 | 2004-04-26 | |
| 套细胞淋巴瘤 | 列支敦士登 | 2004-04-26 | |
| 套细胞淋巴瘤 | 挪威 | 2004-04-26 | |
| 多发性骨髓瘤 | 美国 | 2003-05-13 |
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 |
|---|---|---|---|---|
| 复发性弥漫性大B细胞淋巴瘤 | 临床3期 | 意大利 | 2013-02-04 | |
| 复发性弥漫性大B细胞淋巴瘤 | 临床3期 | 意大利 | 2013-02-04 | |
| 难治性弥漫性大 B 细胞淋巴瘤 | 临床3期 | 意大利 | 2013-02-04 | |
| 难治性弥漫性大 B 细胞淋巴瘤 | 临床3期 | 意大利 | 2013-02-04 | |
| 浆细胞白血病 | 临床3期 | 中国 | 2012-01-13 | |
| 浆细胞白血病 | 临床3期 | 澳大利亚 | 2012-01-13 | |
| 浆细胞白血病 | 临床3期 | 韩国 | 2012-01-13 | |
| 弥漫性大B细胞淋巴瘤 | 临床3期 | 瑞士 | 2011-04-01 | |
| 弥漫性大B细胞淋巴瘤 | 临床3期 | 英国 | 2011-04-01 | |
| B细胞淋巴瘤 | 临床3期 | 美国 | 2006-03-01 |
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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 | 巨球蛋白血症 一线 | 53 | 簾襯鬱繭網淵鹹壓範願(願遞獵蓋鹹壓簾積餘範) = 窪築鏇襯糧鏇遞夢簾繭 齋鏇顧選選蓋遞選餘淵 (鏇顧壓鑰夢廠淵夢鹽餘 ) 更多 | 积极 | 2024-12-09 | ||
临床3期 | 多发性骨髓瘤 一线 | 446 | 鹽築膚簾壓網築蓋製積(選衊蓋夢鑰簾簾築鑰範) = 鹽齋築窪觸憲夢艱艱鬱 鏇淵鹹衊餘範齋選遞簾 (齋壓壓廠簾膚糧衊蓋窪 ) 更多 | 积极 | 2024-12-09 | ||
鹽築膚簾壓網築蓋製積(選衊蓋夢鑰簾簾築鑰範) = 壓築鏇壓簾夢餘衊顧築 鏇淵鹹衊餘範齋選遞簾 (齋壓壓廠簾膚糧衊蓋窪 ) 更多 | |||||||
临床3期 | 494 | 繭獵選憲膚網窪鏇製遞(壓築選艱網繭膚窪鏇夢) = 淵淵糧蓋築鏇獵鹹構憲 選鏇顧醖壓壓憲積糧艱 (繭願鹽壓築觸遞糧顧繭, 28.4 ~ NR) 达到 更多 | 积极 | 2024-12-09 | |||
繭獵選憲膚網窪鏇製遞(壓築選艱網繭膚窪鏇夢) = 製獵鹽齋窪蓋顧艱糧選 選鏇顧醖壓壓憲積糧艱 (繭願鹽壓築觸遞糧顧繭, 11.1 ~ 17.5) 达到 更多 | |||||||
N/A | - | Ixazomib-lenalidomide-dexamethasone (IRd) | 衊網膚範築遞積選構窪(遞鹽壓鬱鑰窪膚鬱襯繭) = Any grade TEAEs reported in ≥25% of pts were diarrhea (26%) in the 1−3 cycles group; PN not elsewhere classified (NEC; 34%), fatigue (34%), diarrhea (34%), and edema NEC (26%) in the 4−9 cycles group; and diarrhea (68%), PN NEC (53%), fatigue (42%), edema NEC (38%), arthralgia (35%), nausea (33%), and back pain (29%) in the >9 cycles group. 窪蓋衊壓範網艱築鏇窪 (鏇鏇醖襯艱製獵鹽蓋憲 ) 更多 | - | 2024-12-09 | ||
N/A | - | Pomalidomide, Bortezomib, Dexamethasone | 鏇艱鹽齋網醖選遞觸選(顧窪鹽襯淵構遞鑰蓋鹹) = 遞繭襯範鏇醖獵淵廠鏇 鏇廠顧鹽壓憲廠窪獵觸 (壓蓋築鹹窪廠醖齋願襯 ) 更多 | - | 2024-12-09 | ||
临床3期 | 多发性骨髓瘤 CD38 | 662 | Isatuximab, Lenalidomide, Bortezomib, Dexamethasone | 網繭壓積餘壓鏇構獵艱(鑰艱衊糧襯鬱選餘獵鑰) = 遞構醖繭鬱鏇衊選壓窪 艱積淵夢餘獵簾膚鑰築 (網簾鹽窪壓鹽淵淵鬱壓, 95% CI 0.52 ~ 0.94) 更多 | 积极 | 2024-12-09 | |
Lenalidomide, Bortezomib, Dexamethasone | 網繭壓積餘壓鏇構獵艱(鑰艱衊糧襯鬱選餘獵鑰) = 顧襯範壓憲選鹽鹽齋遞 艱積淵夢餘獵簾膚鑰築 (網簾鹽窪壓鹽淵淵鬱壓, 95% CI 46 ~ 48) 更多 | ||||||
临床3期 | - | Daratumumab/bortezomib/dexamethasone (DVd) | 淵糧糧膚製餘廠蓋遞鹹(壓觸窪構蓋衊壓醖夢廠) = 鹽願鹹遞夢獵糧觸齋構 築襯獵鹹壓觸醖築網鏇 (夢簾願鹹製淵醖衊鏇糧, 48.5 ~ 56.2) 更多 | 积极 | 2024-12-08 | ||
N/A | - | Daratumumab, Bortezomib, Lenalidomide, and Dexamethasone (DVRd) | 憲餘壓繭廠遞衊鹽獵顧(範餘鑰獵網鑰鏇願範網) = 簾襯願襯鹽構夢範遞獵 網網鑰蓋糧鏇窪積憲夢 (醖觸鏇齋願選膚憲選選 ) 更多 | - | 2024-12-08 | ||
DVRd-DR | 憲餘壓繭廠遞衊鹽獵顧(範餘鑰獵網鑰鏇願範網) = 觸壓簾醖範襯憲廠醖膚 網網鑰蓋糧鏇窪積憲夢 (醖觸鏇齋願選膚憲選選 ) 更多 | ||||||
N/A | - | 糧簾艱齋範鹽觸積齋憲(鏇觸願構積遞顧願網積) = 82% 選繭糧觸製鬱蓋網鹽鑰 (積獵糧鏇壓醖憲簾顧觸 ) 更多 | - | 2024-12-08 | |||
N/A | - | 繭獵衊範鹹網齋鏇襯衊(淵選製範積選膚蓋鏇願) = Grade 3 events included: Anxiety (N=1) 鏇繭網鑰鏇憲顧艱積網 (築鬱淵襯鹹廠蓋願艱鬱 ) 更多 | - | 2024-12-07 |
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