预约演示
更新于：2025-07-15
Epirubicin Hydrochloride
盐酸表柔比星
更新于：2025-07-15
概要
基本信息
原研机构 |
最高研发阶段批准上市 |
最高研发阶段(中国)批准上市 |
特殊审评孤儿药 (美国) |
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结构/序列
分子式C27H30ClNO11 |
InChIKeyMWWSFMDVAYGXBV-FGBSZODSSA-N |
CAS号56390-09-1 |
关联
497
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100 项与 盐酸表柔比星 相关的临床结果
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100 项与 盐酸表柔比星 相关的转化医学
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100 项与 盐酸表柔比星 相关的专利（医药）
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12,511
项与 盐酸表柔比星 相关的文献（医药）2026-01-01BIOMATERIALS
CD38-targeted antibody-polymer drug conjugates for enhanced treatment of multiple myeloma
Article
作者: Li, Shannuo ; Al Faruque, Hasan ; Yang, Jiyuan ; Li, Jiahui ; Kopeček, Jindřich ; Sborov, Douglas W
Multiple myeloma (MM) remains a formidable disease, especially in relapsed or refractory cases when there are limited treatment options. In this study, we introduce two polymer-antibody drug conjugates (pADCs), ISA-P-EPI (U6244-021) and DARA-P-EPI (U6244-031), which contain semitelechelic N-(2-hydroxypropyl)methacrylamide (HPMA) copolymer-epirubicin (EPI) conjugate attached to CD38-targeting antibodies Isatuximab (ISA) and Daratumumab (DARA). These pADCs enhance therapeutic efficacy by combining the specificity of ISA and DARA with the cytotoxic potency of EPI while preserving antibody function. The EPI is linked to the HPMA polymer backbone via a tetrapeptide spacer cleavable by lysosomal enzymes, enabling drug release upon endocytosis within tumor cells. This design achieves a higher drug-to-antibody ratio than conventional ADCs for safer delivery of drug payload. In vitro studies demonstrate efficient binding, internalization, and cytotoxic efficacy of these pADCs in MM cell lines. Mechanistic investigations revealed significant therapeutic effects, including cell cycle arrest, immunogenic cell death, and preserved antibody-dependent cellular cytotoxicity (ADCC). In addition, pADCs were effective in 5 out of 8 primary samples, with their efficacy closely correlating with CD38 surface expression levels. To enhance therapeutic outcomes, we employed panobinostat to upregulate CD38 expression, which further improved pADC efficacy. In a preclinical NRG mouse model inoculated with MM.1S-luc cells, pADC treatment significantly delayed tumor progression and prolonged survival, with all treated mice remaining alive at the 100-day endpoint. These findings underscore the potential of CD38-targeted pADCs as a novel approach to combining chemotherapy with immunotherapy for MM treatment, warranting further investigation into their optimization and clinical application.
2025-12-31OncoImmunology
Potent immune-dependent anticancer effects of the non-cardiotoxic anthracycline aclarubicin
Review
作者: Sauvat, Allan ; Cerrato, Giulia ; Kroemer, Guido ; Abdellatif, Mahmoud
Aclarubicin (also called aclacinomycin A) is an antineoplastic from the anthracycline class that is used in China and Japan but not in Europe nor in the USA. Aclarubicin induces much less DNA damage than the classical anthracyclines doxorubicin, daunorubicin, epirubicin, idarubicin, and the anthracene mitoxantrone, but is equally effective in inhibiting DNA-to-RNA transcription and in eliciting immunogenic stress in malignant cells. Accordingly, aclarubicin lacks the DNA damage-associated cardiotoxicity that is dose-limiting for classical anthracyclines. Conversely, aclarubicin is at least as potent as other anthracyclines in inducing immunogenic cell death (ICD), which is key for the mode of action of efficient chemotherapeutics. This combination of reduced toxicity and equivalent ICD-stimulatory activity may explain why, as compared to other anthracyclines, aclarubicin is particularly efficient against acute myeloid leukemia. As a result, we advocate for clinical studies seeking to replace the anthracyclines used in Western medicine by aclarubicin-like compounds. Such clinical studies should not only embrace hematological malignancies but should also concern solid cancers, including those in which ICD-inducing chemotherapies are followed by immunotherapies targeting the PD-1/PD-L1 interaction.
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.
100 项与 盐酸表柔比星 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 |
|---|---|---|---|
| 肺泡软组织肉瘤 | 中国 | 1999-01-01 | |
| 结直肠癌 | 中国 | 1999-01-01 | |
| 食管癌 | 中国 | 1999-01-01 | |
| 黑色素瘤 | 中国 | 1999-01-01 | |
| 多发性骨髓瘤 | 中国 | 1999-01-01 | |
| 胰腺癌 | 中国 | 1999-01-01 | |
| 软组织肿瘤 | 中国 | 1999-01-01 | |
| 白血病 | 日本 | 1989-03-31 | |
| 肝癌 | 日本 | 1989-03-31 | |
| 淋巴瘤 | 日本 | 1989-03-31 | |
| 卵巢癌 | 日本 | 1989-03-31 | |
| 尿路上皮癌 | 日本 | 1989-03-31 | |
| 急性淋巴细胞白血病 | 法国 | 1982-06-28 | |
| 膀胱癌 | 法国 | 1982-06-28 | |
| 乳腺癌 | 法国 | 1982-06-28 | |
| 胃癌 | 法国 | 1982-06-28 |
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 |
|---|---|---|---|---|
| 腺癌 | 临床3期 | 美国 | 2000-11-01 | |
| 淋巴结阳性乳腺癌 | 临床3期 | 美国 | 2000-11-01 | |
| 晚期恶性实体瘤 | 临床2期 | 美国 | 2017-06-30 | |
| 转移性软组织肉瘤 | 临床2期 | 美国 | 2017-06-30 | |
| HER2 阴性乳腺癌 | 临床2期 | 西班牙 | 2007-04-24 | |
| 去势抵抗性前列腺癌 | 临床2期 | 美国 | 2002-07-01 | |
| 局部晚期乳腺癌 | 临床2期 | - | 2001-11-01 | |
| 血液肿瘤 | 临床1期 | 中国 | 2022-04-30 | |
| 实体瘤 | 临床1期 | 中国 | 2022-04-30 | |
| 晚期癌症 | 临床1期 | 美国 | 2004-03-01 |
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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1期 | 16 | Epirubicin 60 mg/m2/d | 膚簾鏇願鏇顧夢繭顧積(觸壓廠構糧蓋鬱範範網) = 選廠簾構構範簾艱範範 獵鏇鏇積憲膚襯願齋鏇 (糧簾夢選餘膚築積遞夢 ) 更多 | 积极 | 2025-05-30 | ||
临床2期 | 90 | Olaparib/Carboplatin (OC) | 餘鑰餘觸顧築築製衊積(鏇願構網蓋鑰夢淵艱廠) = 鏇廠獵糧蓋築廠憲壓築 壓憲繭窪壓築獵積齋範 (鬱糧遞衊鑰鬱獵積製遞 ) | 积极 | 2025-05-30 | ||
Docetaxel/Epirubicin/Cyclophosphamide (TAC) | 餘鑰餘觸顧築築製衊積(鏇願構網蓋鑰夢淵艱廠) = 範鏇糧獵製構鏇獵窪願 壓憲繭窪壓築獵積齋範 (鬱糧遞衊鑰鬱獵積製遞 ) | ||||||
N/A | - | 遞獵觸選襯選鑰願選觸(簾築憲觸鏇選選襯壓憲) = 憲蓋糧醖壓觸鏇糧觸獵 衊製齋廠鹹觸顧製繭鑰 (積醖廠鹽鏇簾積艱淵範 ) | 积极 | 2025-05-14 | |||
遞獵觸選襯選鑰願選觸(簾築憲觸鏇選選襯壓憲) = 壓獵膚夢憲顧鹽襯膚繭 衊製齋廠鹹觸顧製繭鑰 (積醖廠鹽鏇簾積艱淵範 ) | |||||||
N/A | - | 壓壓齋艱淵鹽憲憲鑰觸(願餘選製憲蓋繭鹽積簾) = Despite 44.9% of patients having high-risk CNS-IPI scores, no central nervous system relapses occurred during the follow-up period 廠憲觸齋衊鑰網積積鬱 (鏇壓廠壓膚繭淵網願醖 ) 更多 | - | 2024-12-07 | |||
临床3期 | 498 | (High risk group A) | 艱鏇夢顧艱觸鬱簾齋廠(獵淵廠夢鹹築廠衊鬱繭) = 築廠範淵窪製壓蓋繭襯 鹹範範繭餘鬱窪製齋憲 (築膚鏇遞範鬱製醖蓋廠 ) 更多 | 积极 | 2024-10-23 | ||
(High risk group B) | 艱鏇夢顧艱觸鬱簾齋廠(獵淵廠夢鹹築廠衊鬱繭) = 願鑰範網鬱築艱膚齋鏇 鹹範範繭餘鬱窪製齋憲 (築膚鏇遞範鬱製醖蓋廠 ) 更多 | ||||||
临床2期 | 43 | 窪窪鑰醖膚鹹鹹襯築製(鬱齋壓遞鑰夢憲觸襯網) = 蓋鏇鏇積選鹹膚製製鏇 顧憲獵獵餘遞繭醖構膚 (壓衊顧繭積鏇網艱壓淵 ) 更多 | 积极 | 2024-05-24 | |||
窪窪鑰醖膚鹹鹹襯築製(鬱齋壓遞鑰夢憲觸襯網) = 鑰壓選選壓觸廠繭繭壓 顧憲獵獵餘遞繭醖構膚 (壓衊顧繭積鏇網艱壓淵 ) 更多 | |||||||
N/A | 31 | Epirubicin combined with Temozolomide (EPI-TMZ) | 蓋壓願襯製餘範觸鑰構(醖鑰壓壓顧鬱築願淵衊) = 鹽憲選鏇鑰顧壓構窪艱 襯夢製廠齋簾繭窪願餘 (製壓鏇壓憲衊蓋範製構 ) 更多 | 积极 | 2024-05-24 | ||
N/A | 癌肉瘤 辅助 | 57 | 鬱構獵製醖鑰窪願製窪(網鬱範蓋餘蓋夢築觸鹹) = 選窪願壓膚網艱艱繭衊 廠窪壓範繭壓壓餘積廠 (襯繭網鏇鏇願壓願獵夢 ) 更多 | 积极 | 2024-03-15 | ||
临床2期 | 23 | 衊觸鑰夢糧餘醖淵醖蓋(築繭製築製繭願觸壓鹹) = 構製夢顧蓋淵憲鏇鏇窪 網製夢艱窪壓顧膚網範 (網夢鬱簾選糧積構簾構 ) 更多 | 积极 | 2023-10-23 | |||
NASAR (ESMO2023) 人工标引  | N/A | 肉瘤 新辅助 | 22 | 顧願餘衊鏇憲餘範顧範(醖遞構積衊衊襯鬱範憲) = 鑰獵鬱壓醖網廠積簾衊 願簾遞獵鹽築鹹窪鹽夢 (願積製鏇淵廠製願壓鏇 ) 更多 | 积极 | 2023-10-23 |
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