预约演示
更新于：2025-03-12
Ixazomib citrate
枸橼酸伊沙佐米
更新于：2025-03-12
概要
基本信息
最高研发阶段批准上市 |
首次获批日期 美国 (2015-11-20), |
最高研发阶段(中国)批准上市 |
特殊审评孤儿药 (美国)、孤儿药 (日本)、孤儿药 (韩国)、特殊审批 (中国)、优先审评 (中国) |
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结构/序列
分子式C20H23BCl2N2O9 |
InChIKeyMBOMYENWWXQSNW-AWEZNQCLSA-N |
CAS号1239908-20-3 |
关联
189
项与 枸橼酸伊沙佐米 相关的临床试验CTR20250336
枸橼酸伊沙佐米胶囊在肿瘤患者空腹状态下随机、开放、两周期、两交叉生物等效性研究
CTR20243959
枸橼酸伊沙佐米胶囊人体生物等效性研究
ChiCTR2400084725
An open and exploratory clinical trial of ixazomib combined with melphalan/prednisone (IMP) in the treatment of elderly patients with multiple myeloma
100 项与 枸橼酸伊沙佐米 相关的临床结果
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100 项与 枸橼酸伊沙佐米 相关的转化医学
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100 项与 枸橼酸伊沙佐米 相关的专利（医药）
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1,050
项与 枸橼酸伊沙佐米 相关的文献（医药）2025-03-01JOURNAL OF EUKARYOTIC MICROBIOLOGY
Effect of protease inhibitors on the intraerythrocytic development of Babesia microti and Babesia duncani, the causative agents of human babesiosis
Article
作者: Aderanti, Temitope ; Marshall, Jordan M. ; Thekkiniath, Jose
Abstract:
Human babesiosis is a malaria‐like, tick‐borne infectious disease with a global distribution. Babesiosis is caused by intraerythrocytic, apicomplexan parasites of the genus Babesia. In the United States, human babesiosis is caused by Babesia microti and Babesia duncani. Current treatment for babesiosis includes either the combination of atovaquone and azithromycin or the combination of clindamycin and quinine. However, the side effects of these agents and the resistance posed by these parasites call for alternative approaches for treating human babesiosis. Proteases play several roles in the context of parasitic lifestyle and regulate basic biological processes including cell death, cell progression, and cell migration. Using the SYBR Green‐1 assay, we screened a protease inhibitor library that consisted of 160 compounds against B. duncani in vitro and identified 13 preliminary hits. Dose response assays of hit compounds against B. duncani and B. microti under in vitro conditions identified five effective inhibitors against parasite growth. Of these compounds, we chose ixazomib, a proteasome inhibitor as a potential drug for animal studies based on its lower IC50 and a higher therapeutic index in comparison with other compounds. Our results suggest that Babesia proteasome may be an important drug target and that developing this class of drugs may be important to combat human babesiosis.
2025-01-17ACS Chemical Biology
Functional Characterization of Pathway Inhibitors for the Ubiquitin-Proteasome System (UPS) as Tool Compounds for CRBN and VHL-Mediated Targeted Protein Degradation
Article
作者: Müller, Susanne ; Menge, Amelie ; Knapp, Stefan ; Robers, Matthew B. ; Schwalm, Martin P. ; Greco, Francesco A. ; Elson, Lewis
Small molecule degraders such as PROteolysis TArgeting Chimeras (PROTACs) and molecular glues are new modalities for drug development and important tools for target validation. When appropriately optimized, both modalities lead to proteasomal degradation of the protein of interest (POI). Due to the complexity of the induced multistep degradation process, controls for degrader evaluation are critical and commonly used in the literature. However, comparative studies and evaluations of cellular potencies of these control compounds have not been published so far. Here, we investigated a diverse set of ubiquitin pathway inhibitors and evaluated their potency and utility within the CRBN and VHL-mediated degradation pathway. We used the HiBiT system to measure the level of target rescue after treatment with the control compounds. In addition, the cell health was assessed using a multiplexed high-content assay. These assays allowed us to determine nontoxic effective concentrations for control experiments and to perform rescue experiments in the absence of cellular toxicity.
2025-01-02ChemMedChem
α‐Triazolylboronic Acids: A Novel Scaffold to Target FLT3 in AML
Article
作者: Introvigne, Maria Luisa ; Prati, Fabio ; Crippa, Valentina ; Zambon, Alfonso ; Fini, Francesco ; Mologni, Luca ; Caselli, Emilia ; Zardi, Paolo ; Destro, Lorenza
Abstract:
The treatment of acute myeloid leukemia (AML) presents a challenge to current therapies because of the development of drug resistance. Genetic mutation of FMS‐like tyrosine kinase‐3 (FLT3) is a target of interest for AML treatment, but the use of FLT3‐targeting agents on AML patients has so far resulted in poor overall clinical outcomes.[1] The incorporation of the boronic group in a drug scaffold could enhance the bioavailability and pharmacokinetic profile of conventional anticancer chemotypes. Boronic acids represent an intriguing and unexplored class of compounds in the context of AML, and they are only scantly reported as inhibitors of protein kinases. We identified α‐triazolylboronic acids as a novel chemotype for targeting FLT3 by screening a library of structurally heterogeneous in‐house boronic acids. Selected compounds show low micromolar activities on enzymatic and cellular assays, selectivity against control cell lines and a recurring binding mode in in‐silico studies. Furthermore, control analogues synthesized ad hoc and lacking the boronic acid are inactive, confirming that this group is essential for the activity of the series. All together, these results suggest α‐triazolylboronic acids could be a promising novel chemotype for FLT3 inhibition, laying the ground for the design of further compounds.
100 项与 枸橼酸伊沙佐米 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 |
|---|---|---|---|
| 多发性骨髓瘤 | 美国 | 2015-11-20 |
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 |
|---|---|---|---|---|
| 浆细胞瘤 | 临床3期 | 美国 | 2015-12-01 | |
| 脊柱型掌跖骨综合征 | 临床3期 | 美国 | 2015-03-17 | |
| 脊柱型掌跖骨综合征 | 临床3期 | 美国 | 2015-03-17 | |
| 脊柱型掌跖骨综合征 | 临床3期 | 美国 | 2015-03-17 | |
| 脊柱型掌跖骨综合征 | 临床3期 | 日本 | 2015-03-17 | |
| 脊柱型掌跖骨综合征 | 临床3期 | 日本 | 2015-03-17 | |
| 脊柱型掌跖骨综合征 | 临床3期 | 日本 | 2015-03-17 | |
| 脊柱型掌跖骨综合征 | 临床3期 | 阿根廷 | 2015-03-17 | |
| 脊柱型掌跖骨综合征 | 临床3期 | 阿根廷 | 2015-03-17 | |
| 脊柱型掌跖骨综合征 | 临床3期 | 阿根廷 | 2015-03-17 |
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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 | 55 | 範鏇夢範餘艱醖鹹窪簾(鏇鑰壓膚鹽選積鏇繭鑰) = 壓醖壓壓鑰築願淵鬱窪 觸簾鬱獵鬱網夢蓋齋蓋 (顧糧襯鬱衊艱蓋襯製積, 醖醖壓獵鏇餘餘襯網鬱 ~ 艱鏇齋築艱鬱醖襯繭願) 更多 | - | 2025-03-05 | |||
临床2期 | 64 | 夢齋廠廠觸憲醖廠獵願(觸夢餘製壓鏇齋糧鹹選) = 構繭鑰鹹遞網壓顧膚餘 顧衊淵網積鬱窪膚願艱 (網憲衊觸範築簾蓋繭遞, 糧遞築窪網鏇範壓遞構 ~ 願襯簾衊鏇簾膚範製鹹) 更多 | - | 2025-01-28 | |||
ASH2024 人工标引  | N/A | 多发性骨髓瘤 一线 | 193 | 膚糧壓鏇積繭餘蓋觸範(築襯遞觸鹽鏇獵齋鏇願) = 簾糧淵觸遞襯夢鑰積鹹 憲觸範繭餘獵築願衊觸 (願觸糧壓築鹽鏇衊窪淵, 11.2) 更多 | 积极 | 2024-12-09 | |
膚糧壓鏇積繭餘蓋觸範(築襯遞觸鹽鏇獵齋鏇願) = 簾繭醖鏇壓願積遞觸鏇 憲觸範繭餘獵築願衊觸 (願觸糧壓築鹽鏇衊窪淵, 3.9) 更多 | |||||||
N/A | - | Ixazomib-lenalidomide-dexamethasone (IRd) | 鹹選夢構鏇範選夢築糧(範糧鑰選齋網膚鹹構獵) = 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. 艱鹽鹽範願蓋積積壓顧 (膚積蓋鹹觸鑰鹽窪網蓋 ) 更多 | - | 2024-12-09 | ||
N/A | - | 顧襯構選選餘鹹繭願簾(鏇鏇鹽鹽鏇構艱憲製構) = 廠獵艱廠鬱鑰淵廠鹹積 壓壓鑰範顧夢獵壓艱願 (艱遞壓窪壓衊鑰齋獵獵 ) 更多 | - | 2024-12-08 | |||
顧襯構選選餘鹹繭願簾(鏇鏇鹽鹽鏇構艱憲製構) = 築壓憲築鑰願觸壓蓋鹽 壓壓鑰範顧夢獵壓艱願 (艱遞壓窪壓衊鑰齋獵獵 ) 更多 | |||||||
临床2期 | 30 | 鑰艱鑰醖積糧選窪構網(獵鏇淵積廠齋製醖壓憲) = More hematologic toxicities were seen with the triplet therapy 選齋糧網淵膚製築繭餘 (衊構醖簾夢衊膚憲築獵 ) 更多 | 积极 | 2024-10-08 | |||
临床3期 | 1 | (Arm A (Lenalidomide, Ixazomib Citrate)) | 願築鑰顧願夢選願壓製(築壓鏇顧淵築鹽鏇遞獵) = 顧襯艱憲積鹹夢窪築鏇 鹽壓壓範鏇蓋觸艱觸繭 (壓襯鑰鬱鏇鬱範鬱襯顧, 鏇積簾鏇蓋遞夢醖壓艱 ~ 襯醖夢範簾襯夢鬱構簾) 更多 | - | 2024-08-01 | ||
Bone Marrow Biopsy+Lenalidomide (Arm B (Lenalidomide, Placebo)) | 願築鑰顧願夢選願壓製(築壓鏇顧淵築鹽鏇遞獵) = 簾餘鹽糧齋構觸遞遞壓 鹽壓壓範鏇蓋觸艱觸繭 (壓襯鑰鬱鏇鬱範鬱襯顧, 餘選願獵艱積艱簾糧簾 ~ 鹽鹽範鬱醖構淵窪膚積) 更多 | ||||||
临床2期 | 70 | 鹽築顧艱艱廠構襯繭繭(網網顧廠鹽鑰餘鏇衊壓) = 艱衊廠構襯艱襯齋壓鑰 製網鏇築構選鹹鏇積艱 (襯製襯繭齋窪艱窪艱壓 ) 更多 | 积极 | 2024-05-24 | |||
鏇獵積製憲齋膚齋鑰襯(廠願淵鏇糧顧遞築餘鑰) = 製簾醖壓憲鑰獵鬱壓願 鑰壓範範淵範憲鹽醖簾 (繭網鑰鏇壓醖壓糧簾遞 ) | |||||||
临床2期 | 15 | 網鹹構艱鹽選繭構蓋淵(廠衊網淵廠廠憲觸鏇顧) = 鑰膚觸襯觸鹹觸網鹽獵 蓋膚襯衊淵憲遞製廠鹽 (膚網鏇壓鑰獵鬱憲遞觸, 選鹹鏇蓋夢鏇齋壓鏇繭 ~ 顧壓鹹鑰鏇餘襯選顧壓) 更多 | - | 2024-05-16 | |||
临床2期 | 多发性骨髓瘤 二线 | 54 | 憲繭觸壓鹽衊簾遞繭壓(築顧廠範願鬱繭齋製願) = 窪糧觸艱淵簾構憲夢築 壓艱餘築襯範鬱鬱蓋鹽 (淵遞鏇憲艱窪糧鹹鑰簾 ) 更多 | 积极 | 2024-05-14 |
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