预约演示
更新于：2026-10-23
Marizomib
更新于：2026-10-23
概要
基本信息
药物类型 小分子化药 |
别名 Marizomib (USAN/INN)、MRZ、Salinosporamide A + [2] |
作用方式 抑制剂、刺激剂 |
作用机制 蛋白酶体抑制剂、细胞凋亡刺激剂 |
在研适应症 |
非在研适应症 |
最高研发阶段临床3期 |
首次获批日期- |
最高研发阶段(中国)- |
特殊审评孤儿药 (美国)、孤儿药 (欧盟) |
登录后查看时间轴
结构/序列
分子式C15H20ClNO4 |
InChIKeyNGWSFRIPKNWYAO-SHTIJGAHSA-N |
CAS号437742-34-2 |
关联
13
项与 Marizomib 相关的临床试验NCT05050305
A Phase 2 Study With Safety Run-In of Marizomib, Pomalidomide, and Dexamethasone For Relapsed and Refractory Multiple Myeloma and CNS Myeloma
NCT04341311
Phase 1 Trial of Marizomib Alone and in Combination With Panobinostat for Children With Diffuse Intrinsic Pontine Glioma
NCT03727841
Phase II Clinical Trial of Marizomib for Recurrent Low-Grade and Anaplastic Supratentorial, Infratentorial and Spinal Cord Ependymoma
100 项与 Marizomib 相关的临床结果
登录后查看更多信息
100 项与 Marizomib 相关的转化医学
登录后查看更多信息
100 项与 Marizomib 相关的专利（医药）
登录后查看更多信息
353
项与 Marizomib 相关的文献（医药）2026-09-01BIOCHEMICAL PHARMACOLOGY
Nanoparticle-Based delivery of proteasome inhibitors for glioblastoma Therapy: Strategies to overcome Blood-Brain barrier and therapeutic resistance
Review
作者: Ali, Meser M ; Apu, Ehsanul Hoque ; Yadab, Mahesh Kumar ; Rahman, Md Ataur
Glioblastoma (GBM), the most malignant primary brain tumor, has a poor prognosis despite surgical resection, radiation, and temozolomide-based chemotherapy. GBM's strong infiltrativeness, intratumoral heterogeneity, activation of compensatory survival mechanisms, and the tight blood-brain barrier (BBB) prevent medication delivery to tumor regions, causing therapeutic failure. Dysregulation of the ubiquitin-proteasome system (UPS), which regulates proteostasis, apoptosis, cell cycle progression, and stress responses, contributes to glioblastoma progression and therapeutic resistance. Thus, proteasome inhibitors (PIs) such bortezomib (BTZ), carfilzomib, ixazomib, and marizomib are promising treatments. However, low BBB penetration, systemic toxicity, and drug resistance mechanisms have hampered its GBM clinical usefulness. Nanoparticle-based therapeutic delivery technologies improve drug solubility, pharmacokinetics, and brain tumor targeting to address these issues. Liposomes, polymeric nanoparticles, dendrimers, inorganic nanoparticles, and exosome-derived vesicles can improve PI bioavailability and treatment efficacy in preclinical GBM models. Surface functionalization with targeted ligands, peptides, and antibodies improves BBB transport and tumor uptake. Stimuli-responsive nanocarriers and multi-modal nanoparticle systems allow regulated drug release and combinatorial delivery of chemotherapeutics, genetic materials, and radiosensitizers. To improve glioblastoma clinical outcomes with nanomedicine and proteasome inhibition, we also explore translational difficulties and prospects. This review provides the UPS's biological role in GBM, proteasome inhibitors and their limitations, and nanoparticle-enabled delivery techniques to bypass BBB barriers and treatment resistance.
2026-06-01VETERINARY JOURNAL
Overcoming mirtazapine's therapeutic limitations in veterinary practice: Development of a taste - masked orally disintegrating tablet with microsphere-based controlled release
Article
作者: Wu, Zhiyong ; Li, Yifan ; Ma, Wanjin ; Lu, Yitong ; Wang, Shun ; Guo, Yajing
Anorexia is a clinically significant condition in companion animals, particularly cats, that disrupts metabolic homeostasis and impedes recovery from underlying diseases. Mirtazapine (MRZ), a commonly prescribed appetite stimulant in veterinary medicine, has limited clinical utility due to its intense bitterness and suboptimal bioavailability in conventional dosage forms. To address these limitations, we developed a novel drug delivery system integrating microencapsulation technology with an orally disintegrating tablet (ODT) formulation. Using an optimized emulsification-solvent diffusion method, we produced ethyl cellulose-based microspheres exhibiting high encapsulation efficiency (93.19 ± 0.71%), uniform particle size distribution (106.12 ± 1.49 μm), and pH-responsive drug release characteristics. Comprehensive physicochemical characterization confirmed the structural integrity of the microspheres and the absence of detrimental drug-polymer interactions. Furthermore, the ODT formulation exhibited excellent pharmaceutical properties, including rapid disintegration and complete drug release under gastric conditions, and effective masking of MRZ's bitter taste in the oral cavity. In vivo evaluations revealed significantly improved palatability (p < 0.05) and preliminary evidence of appetite stimulation (p < 0.05) compared with conventional formulations, supporting further clinical development. Stability studies indicated robustness under standard storage conditions. This advanced delivery system successfully overcomes the major limitations of current MRZ therapies, offering a promising solution for enhancing treatment compliance and therapeutic outcomes in veterinary practice. Moreover, the developed technology platform provides valuable insights for formulating other challenging active pharmaceutical ingredients requiring taste masking and controlled release.
2026-05-29INVESTIGATIVE OPHTHALMOLOGY & VISUAL SCIENCE
Identification of a Small-Molecule Modulator of Astrocyte Reactivity for Optic Nerve Protection
Article
作者: Pan, Shaohui ; Wu, Wencan ; Jin, Ming ; Zhu, Miyao ; Li, Ziwei ; Li, Ting ; Peng, Haotian ; Wu, Nanxin ; Dai, Qin
Purpose:
Injury of the optic nerve leads to retinal ganglion cells (RGCs) apoptosis and irreversible vision loss, in which reactive astrocytes play a central role. The aim of this study is to modulate pathological reactive astrocytes to reduce the progression of optic nerve degeneration.
Methods:
Given the therapeutic potential of small molecules to modulate astrocyte reactivity, we used a drug-screening platform to identify small molecules, and evaluated their capacity to regulate astrocyte phenotypes and preserve RGCs after optic nerve crush (ONC). The primary astrocytes from neonatal C57BL/6J mouse cortices, A1 astrocytes, are induced by TNF, IL-1α, and C1q (TIC), both of them are confirmed at transcript and protein levels. High-throughput screening using SiPer, a computational screening platform, together with DRUG-seq2, yielding candidate small molecules, whose effects on A1/A2 transitions were assessed by RT-qPCR, RNA sequencing (RNA-seq), Western blotting, and immunofluorescence. In vivo, an ONC model received intravitreal compound delivery. RGC survival and astrocyte phenotypes were evaluated by retinal flat-mounts and immunofluorescence.
Results:
Primary astrocytes exposed to TIC acquired A1 phenotype, characterized by upregulated C3, GBP2, H2-d1, and H2-t23, and induced RGC cytotoxicity. Transcriptomic drug screening identified proteasome inhibition as a potential strategy to suppress pathological reactive astrocytes. Marizomib, a blood-brain barrier (BBB)-permeable proteasome inhibitor, downregulated A1 markers and upregulated A2 neuroprotective genes. In an ONC model, Marizomib reduced GBP2-positive astrocytes and, at a lower dose, a modest increase in RGC survival was observed at 14 days post-ONC.
Conclusions:
We developed a small-scale drug-screening platform and identified Marizomib as a modulator of astrocyte phenotypes. Its therapeutic potential was validated both in vitro and in vivo, providing a new chemical tool to modulate astrocyte reactivity for future therapeutic exploration.
100 项与 Marizomib 相关的药物交易
登录后查看更多信息
研发状态
10 条进展最快的记录, 后查看更多信息
登录
| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 复发性胶质母细胞瘤 | 临床3期 | 美国 | 2018-07-26 | |
| 复发性胶质母细胞瘤 | 临床3期 | 奥地利 | 2018-07-26 | |
| 复发性胶质母细胞瘤 | 临床3期 | 比利时 | 2018-07-26 | |
| 复发性胶质母细胞瘤 | 临床3期 | 加拿大 | 2018-07-26 | |
| 复发性胶质母细胞瘤 | 临床3期 | 丹麦 | 2018-07-26 | |
| 复发性胶质母细胞瘤 | 临床3期 | 法国 | 2018-07-26 | |
| 复发性胶质母细胞瘤 | 临床3期 | 德国 | 2018-07-26 | |
| 复发性胶质母细胞瘤 | 临床3期 | 荷兰 | 2018-07-26 | |
| 复发性胶质母细胞瘤 | 临床3期 | 挪威 | 2018-07-26 | |
| 复发性胶质母细胞瘤 | 临床3期 | 西班牙 | 2018-07-26 |
登录后查看更多信息
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 | 749 | (Experimental Arm) | 餘鏇製遞膚製構簾襯夢(網壓鬱網衊醖膚繭糧範) = 淵製憲衊觸壓積襯鏇餘 襯鏇選憲廠網淵艱壓餘 (壓鹽醖遞襯鬱鏇簾網範, 齋鬱糧淵繭夢窪廠選鹹 ~ 窪餘顧獵醖構鏇膚衊衊) 更多 | - | 2024-01-31 | ||
radiotherapy+Temozolomide (Standard Arm) | 餘鏇製遞膚製構簾襯夢(網壓鬱網衊醖膚繭糧範) = 壓壓簾顧網鏇構鹽鹹衊 襯鏇選憲廠網淵艱壓餘 (壓鹽醖遞襯鬱鏇簾網範, 糧獵糧鹹築築繭願憲淵 ~ 衊廠鏇簾衊淵蓋鑰網獵) 更多 | ||||||
临床1期 | 4 | Marizomib alone | 淵範糧鹽鏇積繭淵蓋網(鹹遞鬱遞壓遞蓋憲顧遞) = Adverse events were related to disease/tumor progression or considered mild (grade 1 headache, emesis, diarrhea, fatigue, lymphopenia, thrombocytopenia) with the exception of sinus tachycardia and dyspnea (grade 2) (n=1) 築繭窪鑰壓範餘憲積選 (觸膚醖壓獵鬱選繭窪觸 ) | 积极 | 2023-09-08 | ||
临床3期 | 749 | 鏇鹽獵廠鑰構繭醖憲醖(築鹽糧選膚憲鏇鹽淵遞) = 選糧簾糧窪範繭淵鏇鹽 鏇網觸襯餘範選製獵夢 (顧網蓋顧蓋築觸艱選憲 ) 更多 | 不佳 | 2021-05-28 | |||
鏇鹽獵廠鑰構繭醖憲醖(築鹽糧選膚憲鏇鹽淵遞) = 糧鏇選簾選遞觸築繭齋 鏇網觸襯餘範選製獵夢 (顧網蓋顧蓋築觸艱選憲 ) 更多 | |||||||
临床1期 | 胶质母细胞瘤 一线 | 66 | 鏇廠廠築獵壓簾夢淵顧(製襯鏇窪醖觸齋淵餘襯) = 壓鬱窪繭襯鬱壓築衊夢 網網鏇構憲窪憲鏇鹽觸 (顧醖齋網鏇餘夢糧醖鹹 ) 更多 | 积极 | 2019-06-02 | ||
临床1期 | - | Marizomib (MRZ) with Temozolomide (TMZ) and Radiotherapy (RT) | 選願鬱蓋餘淵鑰鹹鏇餘(獵醖憲醖選膚衊糧顧築) = 3 (ataxia/diarrhea; ataxia/confusion; ataxia/fatigue) in concomitant and 2 (delirium/ataxia; ataxia/fatigue) in adjuvant cohorts at 1.0 mg/m2 壓願網衊餘襯鑰壓獵鹽 (築艱遞觸繭齋艱蓋範夢 ) 更多 | 积极 | 2018-11-05 | ||
临床1期 | 38 | 鹹鬱鬱蓋鬱鹽顧窪膚構(齋衊膚醖鹽餘窪鏇蓋夢) = 憲衊夢遞艱簾淵淵齋艱 淵壓構築範壓齋鹹醖糧 (鑰願淵夢膚壓遞簾構獵 ) 更多 | 积极 | 2018-01-01 | |||
临床1/2期 | 复发性胶质母细胞瘤 unmethylated MGMT | methylated MGMT | 36 | Marizomib (MRZ) + Bevacizumab (BEV) | 鹽鬱願衊築壓範襯衊衊(築衊鹽壓糧醖鏇衊膚廠) = 鑰廠鹹憲遞鬱鏇膚顧簾 餘網獵網醖鏇繭繭膚網 (醖鑰夢願壓構夢膚鹽觸 ) | 积极 | 2017-11-06 | |
临床2期 | 15 | 鬱糧壓鹽壓鏇網糧廠製 = 鹽簾獵觸淵鑰膚製鏇構 築顧獵廠醖齋餘繭築鹽 (製蓋願築觸顧衊繭獵獵, 醖醖醖憲餘艱鹽築範鏇 ~ 艱淵憲積鹽網蓋遞壓觸) 更多 | - | 2017-09-13 | |||
临床1期 | 胶质瘤 MGMT status | 36 | Marizomib (MRZ) 0.55 mg/m2 | 繭廠繭齋鬱夢膚醖廠蓋(衊鏇簾觸艱繭鬱願夢壓) = One pt (cohort 1) had DLT (fatigue) 構鏇夢簾觸壓蓋願選糧 (衊簾製衊鏇鹹窪鹹膚艱 ) 更多 | 积极 | 2016-11-07 | |
Marizomib (MRZ) 0.7 mg/m2 | |||||||
临床1期 | 86 | (patients with relapsed and/or refractory multiple myeloma (RRMM) and other hematologic malignancies) | 鬱鏇壓蓋膚範壓夢淵淵(齋選築鹹窪壓窪襯網夢) = The Schedule A recommended phase II dose was 0.7 mg/m(2) over 10 minutes; Schedule B was 0.5 mg/m(2) over 2 hours. 壓膚簾範範網壓窪築餘 (淵醖壓鹹簾齋廠蓋廠構 ) 更多 | 积极 | 2016-09-15 | ||
登录后查看更多信息
转化医学
使用我们的转化医学数据加速您的研究。
登录
或
药物交易
使用我们的药物交易数据加速您的研究。
登录
或
核心专利
使用我们的核心专利数据促进您的研究。
登录
或
临床分析
紧跟全球注册中心的最新临床试验。
登录
或
批准
利用最新的监管批准信息加速您的研究。
登录
或
特殊审评
只需点击几下即可了解关键药物信息。
登录
或
提出任何生物医药研究问题
让每一步生物医药决策都精准制胜
基于十亿级生物数据与全球情报的精准 AI，赋能早期药物发现
立即开始免费试用!
智慧芽新药情报库是智慧芽专为生命科学人士构建的基于AI的创新药情报平台，助您全方位提升您的研发与决策效率。
立即接入生物医药数据包
智慧芽新药库数据也通过智慧芽开放平台，以MCP或API服务形式对外开放。立即使用我们的MCP服务定制您的LLM智能体。
生物序列数据库
生物药研发创新
免费使用
化学结构数据库
小分子化药研发创新
免费使用