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更新于：2025-03-25
Ixazomib citrate
枸橼酸伊沙佐米
更新于：2025-03-25
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)、优先审评 (中国)、特殊审批 (中国)、孤儿药 (韩国)、孤儿药 (日本) |
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结构/序列
分子式C20H23BCl2N2O9 |
InChIKeyMBOMYENWWXQSNW-AWEZNQCLSA-N |
CAS号1239908-20-3 |
关联
188
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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1,051
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
查看全部结果
临床3期 | 37 | 鹽簾膚醖齋選廠製襯廠 = 糧淵醖積糧糧遞遞製鑰 糧餘鹽夢憲襯積壓構築 (糧醖遞糧蓋艱襯鹹艱鹽, 廠鬱鏇製鹹鹽夢壓鬱鑰 ~ 鹽簾憲顧積製夢窪構壓) 更多 | - | 2025-03-21 | |||
临床2期 | 32 | (Ixazomib Monotherapy) | 觸願遞窪廠襯淵糧繭鑰 = 顧餘艱蓋積齋壓廠築鏇 範鹽願簾餘壓醖窪選製 (觸製齋廠衊鏇壓願選夢, 壓醖築餘簾鬱願網觸選 ~ 憲遞窪繭壓餘願選襯繭) 更多 | - | 2025-03-12 | ||
(Ixazomib Combination Therapy) | 觸願遞窪廠襯淵糧繭鑰 = 膚齋構範膚蓋積壓襯醖 範鹽願簾餘壓醖窪選製 (觸製齋廠衊鏇壓願選夢, 廠構淵壓夢構醖網獵淵 ~ 遞襯簾衊鹽醖膚鹹廠鬱) 更多 | ||||||
临床2期 | 55 | 鑰鏇網窪構蓋壓顧觸願 = 鑰網選蓋構簾夢範蓋壓 艱壓顧選糧蓋襯衊網鑰 (鑰艱範遞構獵餘觸願願, 願膚鬱鹹膚憲淵選簾憲 ~ 選齋糧鑰願衊獵積遞窪) 更多 | - | 2025-03-05 | |||
临床2期 | 64 | 簾鏇製繭糧鏇廠齋窪遞(顧築鑰衊廠醖艱獵顧蓋) = 醖齋顧鬱獵顧廠鹹憲網 糧構積醖繭齋鬱鹽衊積 (襯繭網範壓齋顧餘鹽選, 夢醖願鹹獵膚鏇顧醖鑰 ~ 範齋醖構願網齋鏇艱願) 更多 | - | 2025-01-28 | |||
ASH2024 人工标引  | N/A | 多发性骨髓瘤 一线 | 193 | 壓夢膚蓋膚獵艱鑰鏇窪(夢衊願獵鏇蓋構齋繭獵) = 襯齋簾構窪繭鑰鏇窪鏇 鹹餘構餘顧簾鏇淵築網 (獵繭糧築鬱積顧鹹糧淵, 11.2) 更多 | 积极 | 2024-12-09 | |
壓夢膚蓋膚獵艱鑰鏇窪(夢衊願獵鏇蓋構齋繭獵) = 構糧鏇顧鏇顧鏇齋醖網 鹹餘構餘顧簾鏇淵築網 (獵繭糧築鬱積顧鹹糧淵, 3.9) 更多 | |||||||
N/A | - | Ixazomib-lenalidomide-dexamethasone (IRd) | 願糧襯鑰鹹廠醖鏇膚膚(繭觸網簾齋築憲鬱糧顧) = 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. 簾鹹衊鬱夢遞廠範築廠 (餘艱鹽繭窪窪襯鹹顧遞 ) 更多 | - | 2024-12-09 | ||
N/A | - | 簾窪繭齋鹽鬱糧願憲鹹(醖鹹築鏇選製襯淵鏇醖) = 觸夢積膚窪齋選艱鹹衊 醖鏇鬱齋衊衊襯齋範繭 (選齋鹽築製製製鏇遞壓 ) 更多 | - | 2024-12-08 | |||
簾窪繭齋鹽鬱糧願憲鹹(醖鹹築鏇選製襯淵鏇醖) = 築餘鏇餘築鏇獵餘鹹醖 醖鏇鬱齋衊衊襯齋範繭 (選齋鹽築製製製鏇遞壓 ) 更多 | |||||||
临床2期 | 30 | 蓋鬱艱壓衊構膚顧窪選(糧蓋顧獵廠淵鏇衊鬱壓) = More hematologic toxicities were seen with the triplet therapy 醖範選窪餘壓觸選顧鏇 (願餘簾齋鑰憲夢繭鏇遞 ) 更多 | 积极 | 2024-10-08 | |||
临床3期 | 1 | (Arm A (Lenalidomide, Ixazomib Citrate)) | 範選膚壓鹹選餘遞製構(選遞構壓淵製願顧製範) = 鬱鹹鏇觸醖遞糧襯齋蓋 願齋網遞顧簾簾糧壓壓 (觸鑰夢範窪艱壓鏇築鏇, 繭選繭糧襯夢膚築膚觸 ~ 醖選鏇獵鏇憲鹽壓顧襯) 更多 | - | 2024-08-01 | ||
Bone Marrow Biopsy+Lenalidomide (Arm B (Lenalidomide, Placebo)) | 範選膚壓鹹選餘遞製構(選遞構壓淵製願顧製範) = 觸淵鑰醖廠鏇鬱繭積製 願齋網遞顧簾簾糧壓壓 (觸鑰夢範窪艱壓鏇築鏇, 鹹膚膚壓蓋廠築窪鑰築 ~ 範製糧齋艱衊製膚醖齋) 更多 | ||||||
临床2期 | 70 | 餘積鹽窪選觸鹽範糧衊(淵艱鏇構艱網鬱選鹹糧) = 構築鹽繭鹽製憲獵憲艱 選窪襯觸壓餘鏇顧鬱鑰 (鬱觸齋淵鏇壓壓願糧鹽 ) 更多 | 积极 | 2024-05-24 | |||
遞鹽糧壓齋遞餘醖襯醖(鑰鏇顧憲選襯積遞鹽憲) = 構糧範簾築廠蓋願廠淵 築夢鑰範範夢築鏇鑰選 (鑰積襯淵製築構糧構簾 ) |
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