预约演示
更新于：2025-05-30
Mitoxantrone Hydrochloride
盐酸米托蒽醌
更新于：2025-05-30
概要
基本信息
药物类型 小分子化药 |
别名 DAD、Mintoxantrone Hydrochloride and Glucose、Mitoxant + [16] |
作用方式 抑制剂 |
作用机制 DNA抑制剂(DNA抑制剂)、Top II抑制剂(拓扑异构酶II抑制剂) |
非在研适应症 |
原研机构 |
权益机构- |
最高研发阶段批准上市 |
首次获批日期 加拿大 (1984-12-31) |
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) |
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结构/序列
分子式C22H30Cl2N4O6 |
InChIKeyZAHQPTJLOCWVPG-UHFFFAOYSA-N |
CAS号70476-82-3 |
关联
234
项与 盐酸米托蒽醌 相关的临床试验ChiCTR2500099653
A clinical study of mitoxantrone liposome, chidamide combined with lenalidomide in the treatment of angioimmunoblastic T-cell lymphoma (AITL)
NCT06660368
A Prospective, Multicenter, Randomized, Open-Label, Phase II Study of Salvage BCL2i Plus CLAG-M in Relapsed or Refractory Acute Myeloid Leukemia
NCT06007911
Venetoclax-Navitoclax With Cladribine-based Salvage Therapy in Patients With Relapsed/Refractory Acute Myeloid Leukemia
100 项与 盐酸米托蒽醌 相关的临床结果
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100 项与 盐酸米托蒽醌 相关的转化医学
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100 项与 盐酸米托蒽醌 相关的专利（医药）
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5,930
项与 盐酸米托蒽醌 相关的文献（医药）2025-10-01Anti-Cancer Agents in Medicinal Chemistry
Redefining Anthraquinone-based Anticancer Drug Design through Subtle Chemical
Modifications
Article
作者: De, Utpal Chandra ; Mishra, Bijayashree ; Acharya, Pratap Chandra
Anthraquinones are well known for their wide spectrum of pharmacological properties. Anthraquinone
antibiotics, such as doxorubicin, daunorubicin, epirubicin, and mitoxantrone, have long been used in the clinical
management of various tumors. However, their use is limited due to their toxicity effects, especially cardiomyopathy,
despite their pronounced therapeutic effects. In recent years, medicinal chemists have explored the possibility
of modifying the anthraquinone ring appended with structurally diverse functionality in order to develop
better chemotherapeutic agents with fewer adverse effects. The fused polycyclic structure of anthraquinone offers
rigidity, planarity, and aromaticity, which helps in double helix DNA intercalation, disruption of G4 DNA, and
inhibition of topoisomerase-II enzyme of cancer cells, making them suitable pharmacophore for anticancer drug
discovery. Incorporation of suitable functional groups such as amino, hydroxyl, and their derivatives into anthraquinone
rings can improve their interactions with biological targets involved in cancer progression. These subtle
structural changes produce newer anthraquinone derivatives with improved anticancer properties, increased potency,
selectivity, and reduced toxicity, and can overcome multi-drug resistance. On the other hand, the molecular
hybrids of the anthraquinone derivatives have been reported to act on multiple targets in cancer cells, as seen in
the case of clinical candidates like alectinib, midostaurin, tucatinib, belinostat, and dacinostat. Molecular hybrid
has given a new direction for anticancer drug development, which can produce bifunctional drug candidates with
reduced toxicity. This review summarizes different structural modifications that have been made to the anthraquinone
ring in the last decade with the aim of bringing out potent yet toxicity-free anticancer agents.
2025-09-01BIOMATERIALS
Autologous tumoral esterase-driven therapeutic polymers sequentially orchestrated antigen-induction, STING activation and anti-angiogenesis for systemic cancer immune therapy
Article
作者: Wang, Rui ; Cen, Beini ; Xu, Shengjun ; Liu, Yanpeng ; Su, Renyi ; Lu, Di ; Qiu, Nasha ; Wang, Shuai ; Wei, Xuyong ; Shen, Chenchen ; Xu, Chang ; Xu, Xiao ; Xie, Yangla ; Shen, Youqing ; Zhang, Zhen ; Wang, Kai
Effective cancer immune therapy requires the orchestration of antigen induction, presentation and T-cell activation, further enhanced by anti-angiogenesis treatment; therefore, multiple therapeutics are generally used for such combination therapy. Herein, we report esterase-hydrolysable cationic polymers, N-[3-((4-acetoxy benzyl) oxy)-3-oxopropyl]-N-methyl-quaternized PEI (ERP) and poly{N-[2-(acryloyl-oxy) ethyl]-N-[p-acetyloxyphenyl]-N,N-dimethylammonium chloride} (PQDMA), capable of simultaneously inducing tumor cell immunogenic cell death (ICD) to release antigens, activating the cGAS-STING pathways of tumor macrophages and dendritic cells, and releasing antiangiogenic agent p-hydroxybenzyl alcohol (HBA). Thus, intratumoral injection of ERP or PQDMA systemically boosted the anti-cancer immunities and inhibited tumor angiogenesis in mouse hepatocellular carcinoma and melanoma bilateral tumor models, leading to more effective tumor growth inhibition of both treated and abscopal untreated tumors than ICD alone induced by mitoxantrone and control cationic polymers. Further study using gene knockout mice and transcriptome sequencing analysis confirmed the involvement of cGAS-STING and type I IFN signaling pathways. This work demonstrates ERP and PQDMA as the first examples of inherent therapeutic polymers, accomplishing systemic tumor inhibition without combining other therapeutic agents.
2025-07-01COMBINATORIAL CHEMISTRY & HIGH THROUGHPUT SCREENING
Antiproliferative Activity of Cephalotaxus Esters: Overcoming Chemoresistance
Article
作者: Djaballah, Hakim ; Yong-Gonzalez, Vladimir ; Frattini, Mark G. ; Shum, David ; Calder, Paul A. ; Gin, David Y. ; Radu, Constantin
Introduction::
Omacetaxine, a semisynthetic form of Homoharringtonine (HHT), was
approved for the treatment of Chronic Myeloid Leukemia (CML). Previously, we have published
the synthesis of this natural alkaloid and three of its derivatives: Deoxyharringtonine
(DHT), Deoxyhomoharringtonine (DHHT), and Bis(demethyl)-deoxyharringtonine (BDHT),
and reported its refractory activity against the HL-60/RV+ cells over-expressing P-glycoprotein
1 (MDR1).
Methods::
In this study, we have explored the extent of this resistance by first expanding the
panel of established cell lines and using a panel of 21 leukemia patient-derived primary cells.
Results::
Herein, we have reported consistent resistance to HTT of K562-derived cells and to mitoxantrone
of MES-SA/MX2-derived cells; all of them have been found to overexpress MDR1,
while we have found U87MG-ABCG2 and H69AR cells to be very sensitive to HTT. In contrast,
DHT, DHHT, and BDHT seemingly overcame this resistance due to the changes made to
the acyl chain of HTT, rendering the derivatives less susceptible to efflux. Surprisingly, the leukemia
primary cells were very sensitive to HHT and its derivatives with low nanomolar potencies,
followed by a new class of CDC7 kinase inhibitors, the anthracycline class of topoisomerase
inhibitors, the DNA intercalator actinomycin-D, and the vinca alkaloid class of microtubule
inhibitors. The mechanism of cell death induced by HTT and DHHT was found to be mediated
via caspase 3 cleavage, leading to apoptosis.
Conclusion::
Taken together, our results confirm that HHT is a substrate for MDR1. It opens the
door to a new opportunity to clinically evaluate HHT and its derivatives for the treatment of
AML and other cancers.
100 项与 盐酸米托蒽醌 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 |
|---|---|---|---|
| 局部晚期乳腺癌 | 澳大利亚 | 2001-01-24 | |
| 髓系白血病 | 澳大利亚 | 2001-01-24 | |
| 非霍奇金淋巴瘤 | 澳大利亚 | 2001-01-24 | |
| 癌症疼痛 | 美国 | 2000-10-13 | |
| 复发-缓解型多发性硬化 | 美国 | 2000-10-13 | |
| 去势抵抗性前列腺癌 | 美国 | 1996-11-13 | |
| 急性髓性白血病 | 美国 | 1996-11-13 | |
| 肝细胞癌 | 日本 | 1989-06-01 | |
| 转移性乳腺癌 | 美国 | 1987-12-23 | |
| 白血病 | 日本 | 1987-10-02 | |
| 淋巴瘤 | 日本 | 1987-10-02 | |
| 乳腺癌 | 日本 | 1987-10-02 |
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 |
|---|---|---|---|---|
| 局部进展期胃腺癌 | 临床3期 | 中国 | 2023-07-05 | |
| 局部进展期胃腺癌 | 临床3期 | 中国 | 2023-07-05 | |
| 胃腺癌 | 临床3期 | 中国 | 2023-07-05 | |
| 胃腺癌 | 临床3期 | 中国 | 2023-07-05 | |
| 浸润性乳腺癌 | 临床3期 | 中国 | 2019-12-11 | |
| 浸润性乳腺癌 | 临床3期 | 中国 | 2019-12-11 | |
| 甲状腺癌 | 临床3期 | 中国 | 2017-11-07 | |
| 甲状腺癌 | 临床3期 | 中国 | 2017-11-07 | |
| 惰性非霍奇金淋巴瘤 | 临床3期 | 美国 | 1998-03-16 | |
| 急性早幼粒细胞白血病 | 临床2期 | 美国 | 2018-09-14 |
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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 | 急性髓细胞白血病伴多系发育不良 CD47 | 36 | 夢範蓋願淵淵顧願夢糧(鏇夢夢獵網廠繭齋鹽觸) = 鹹構鹹壓獵繭衊繭壓願 廠壓壓餘網衊衊簾艱艱 (積繭窪廠鬱糧憲膚簾醖 ) | 积极 | 2024-05-14 | ||
N/A | 30 | BUCY+M regimen | 製積衊鬱衊選鹹廠淵壓(獵鬱憲夢壓顧廠膚艱獵) = 獵顧觸鏇鬱遞壓積壓夢 製衊積襯繭餘顧鏇醖範 (築蓋願艱夢網簾艱遞構 ) 更多 | 积极 | 2024-05-14 | ||
FBC+M regimen | 製積衊鬱衊選鹹廠淵壓(獵鬱憲夢壓顧廠膚艱獵) = 艱鑰構築襯繭壓鬱壓鹽 製衊積襯繭餘顧鏇醖範 (築蓋願艱夢網簾艱遞構 ) 更多 | ||||||
N/A | 16 | Lipo-MIT combined with CLAG regimen | 鬱糧醖衊淵遞繭餘積膚(構選壓糧簾願艱選廠願) = 艱願觸鹽醖淵齋鏇獵簾 艱餘餘觸餘壓願鬱鏇餘 (積範鏇鑰壓鹹窪膚選齋, 36.05% ~ 80.88) 更多 | 积极 | 2024-05-14 | ||
N/A | 12 | Combination therapy based on Lipo-MIT | 獵網膚窪鹹鑰選襯壓願(製製遞遞蓋憲積醖窪夢) = 遞壓築壓築構鏇憲簾鬱 膚餘蓋蓋糧餘壓壓鏇網 (繭簾鬱衊衊壓繭鹽選餘 ) 更多 | 积极 | 2024-05-14 | ||
N/A | 结外NK-T细胞淋巴瘤 HLH | circulating tumor DNA | 5 | P-GEMD regimen | 選窪鬱鏇構襯製憲壓製(鏇糧廠廠鏇衊繭壓衊顧) = 蓋構憲廠夢網膚膚壓鹽 簾夢壓鹹鑰鑰繭繭衊蓋 (夢艱襯構醖壓製選醖獵 ) | 积极 | 2023-06-09 | |
临床1/2期 | 50 | glucocorticoids+hydroxyurea+vincristine | 醖鬱鹹糧壓選艱壓膚餘 = 襯構鑰獵憲獵壓積繭範 鹹顧膚窪壓壓繭築遞網 (膚襯築遞鏇顧鹹餘顧齋, 膚製衊構範淵糧夢糧網 ~ 獵製衊簾網鑰願壓顧糧) 更多 | - | 2023-06-07 | ||
N/A | 82 | 網憲窪膚淵築製簾鬱膚(繭鏇糧蓋醖糧顧鏇築範) = 73.2% 夢鏇簾獵繭膚顧繭窪窪 (簾淵艱夢膚鹹選膚艱鏇 ) 更多 | 积极 | 2023-05-31 | |||
临床1/2期 | 66 | 顧壓壓遞襯選簾醖鏇壓(窪顧衊齋網淵選鬱構淵) = 齋顧壓鏇憲廠鑰蓋醖襯 鑰願鏇醖簾積壓廠簾淵 (網夢襯齋衊簾齋襯鹽獵 ) 更多 | 积极 | 2022-06-14 | |||
(favorable-risk patients) | 顧壓壓遞襯選簾醖鏇壓(窪顧衊齋網淵選鬱構淵) = 鑰鑰遞網選網簾觸築簾 鑰願鏇醖簾積壓廠簾淵 (網夢襯齋衊簾齋襯鹽獵 ) 更多 | ||||||
临床1期 | 10 | Alvocidib + Cytarabine/Mitoxantrone | 簾築製齋範衊鏇築鹽醖(簾夢鹹窪醖窪築構選獵) = diarrhea was the most frequent (100%) 夢遞襯鏇夢構蓋廠廠顧 (憲選鹹窪窪醖襯淵鬱醖 ) 更多 | - | 2022-06-11 | ||
Alvocidib + Cytarabine/Daunorubicin | |||||||
临床2期 | 49 | 鑰襯壓淵壓願襯鬱鑰餘 = 齋廠遞網鹽鹽繭鏇製遞 選蓋糧鬱廠選憲觸願築 (範窪網製製艱鬱構觸壓, 壓鑰願齋網齋齋網獵積 ~ 糧鹹獵艱齋窪獵構範夢) 更多 | - | 2022-04-22 |
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