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更新于：2026-02-27
Belotecan Hydrochloride
盐酸贝洛替康
更新于：2026-02-27
概要
基本信息
非在研机构- |
权益机构- |
最高研发阶段批准上市 |
最高研发阶段(中国)- |
特殊审评- |
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结构/序列
分子式C25H28ClN3O4 |
InChIKeySJKBXKKZBKCHET-UQIIZPHYSA-N |
CAS号213819-48-8 |
关联
9
项与 盐酸贝洛替康 相关的临床试验KCT0004484
Phase II study of Belotecan monotherapy in patients with recurrent or persistent cervical cancer
NCT01784107
A Phase Ib/II Trial of Belotecan and Ifosfamide in Patients With Extensive Disease of Small Cell Lung Cancer
NCT01630018
A Phase Ⅱb, Randomized, Open, Parallel-Group, Multi-Center Trial to Assess the Efficacy and Safety of Belotecan(CamtoBell Inj.) or Topotecan in Patients With Recurrent or Refractory Ovarian Cancer
100 项与 盐酸贝洛替康 相关的临床结果
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100 项与 盐酸贝洛替康 相关的转化医学
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100 项与 盐酸贝洛替康 相关的专利（医药）
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102
项与 盐酸贝洛替康 相关的文献（医药）2025-03-01EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Repurposing FDA-approved drugs to target G-quadruplexes in breast cancer
Article
作者: Moraca, Federica ; Napolitano, Fabiana ; D'Aria, Federica ; Pagano, Bruno ; Amato, Jussara ; Catalanotti, Bruno ; Di Porzio, Anna ; Castellano, Giuliano ; Landolfi, Laura ; Malfitano, Anna Maria ; Arciuolo, Valentina ; Marzano, Simona ; Randazzo, Antonio
Breast cancer, a leading cause of cancer-related mortality in women, is characterized by genomic instability and aberrant gene expression, often influenced by noncanonical nucleic acid structures such as G-quadruplexes (G4s). These structures, commonly found in the promoter regions and 5'-untranslated RNA sequences of several oncogenes, play crucial roles in regulating transcription and translation. Stabilizing these G4 structures offers a promising therapeutic strategy for targeting key oncogenic pathways. In this study, we employed a drug repurposing approach to identify FDA-approved drugs capable of binding and stabilizing G4s in breast cancer-related genes. Using ligand-based virtual screening and biophysical methods, we identified several promising compounds, such as azelastine, belotecan, and irinotecan, as effective G4 binders, with significant antiproliferative effects in breast cancer cell lines. Notably, belotecan and irinotecan exhibited a synergistic mechanism, combining G4 stabilization with their established topoisomerase I inhibition activity to enhance cytotoxicity in cancer cells. Our findings support the therapeutic potential of G4 stabilization in breast cancer, validate drug repurposing as an efficient strategy to identify G4-targeting drugs, and highlight how combining G4 stabilization with other established drug activities may improve anticancer efficacy.
2024-03-01Journal of controlled release : official journal of the Controlled Release Society
Potent antitumor activity of anti-HER2 antibody-topoisomerase I inhibitor conjugate based on self-immolative dendritic dimeric-linker
Article
作者: Tonillo, Jason ; Shan, Min ; Gnaim, Samer ; Toister-Achituv, Mira ; Gholap, Sachin ; Zauberman, Arie ; Kalimi, Doron ; Shabat, Doron ; Berger, Nir ; Liubomirski, Yulia ; Satchi-Fainaro, Ronit ; Ge, Liang ; Scomparin, Anna ; Tiram, Galia ; Yeini, Eilam ; Schröter, Christian ; Das, Sayantan ; Sweeney-Lasch, Stanley ; Deutsch, Carl ; Shelef, Omri ; Dickgiesser, Stephan
Antibody-drug conjugates (ADCs) are a rapidly expanding class of anticancer therapeutics, with 14 ADCs already approved worldwide. We developed unique linker technologies for the bioconjugation of drug molecules with controlled-release applications. We synthesized cathepsin-cleavable ADCs using a dimeric prodrug system based on a self-immolative dendritic scaffold, resulting in a high drug-antibody ratio (DAR) with the potential to reach 16 payloads due to its dendritic structure, increased stability in the circulation and efficient release profile of a highly cytotoxic payload at the targeted site. Using our novel cleavable linker technologies, we conjugated the anti-human epidermal growth factor receptor 2 (anti-HER2) antibody, trastuzumab, with topoisomerase I inhibitors, exatecan or belotecan. The newly synthesized ADCs were tested in vitro on mammary carcinoma cells overexpressing human HER2, demonstrating a substantial inhibitory effect on the proliferation of HER2-positive cells. Importantly, a single dose of our trastuzumab-based ADCs administered in vivo to mice bearing HER2-positive tumors, showed a dose-dependent inhibition of tumor growth and survival benefit, with the most potent antitumor effects observed at 10 mg/kg, which resulted in complete tumor regression and survival of 100% of the mice. Overall, our novel dendritic technologies using the protease-cleavable Val-Cit linker present an opportunity for the development of highly selective and potent controlled-released therapeutic payloads. This strategy could potentially lead to the development of novel and effective ADC technologies for patients diagnosed with HER2-positive cancers. Moreover, our proposed ADC linker technology can be implemented in additional medical conditions such as other malignancies as well as autoimmune diseases that overexpress targets, other than HER2.
2024-01-01LWT-FOOD SCIENCE AND TECHNOLOGY
Antimicrobial effects and metabolomics analysis of cell-free supernatant produced by Pediococcus acidilactici LWX 401 isolated from Yunnan traditional pickles
作者: Cai-Rui Chen ; Jia-Jia Wang ; Feng Wang ; Xin-Yi Zhang ; Lian-Bing Lin ; Xian-Kang Xiao ; Wei-Xin Liu ; Xiao Lu
Foodborne pathogens pose a significant risk to human health via the food chain.Here, we evaluated the antibacterial effects of cell-free supernatant (CFS) of Pediococcus acidilactici (P. acidilactici) LWX 401 isolated from food-grade Chinese traditional pickles and found that it exhibited broad antibacterial activity against multidrug-resistant gram-neg. Escherichia coli (E. coli) O157:H7 and yogurt-derived gram-pos. Staphylococcus aureus (S. aureus), with inhibition zone sizes of 23.10 ± 0.80 and 20.53 ± 0.07 mm, resp. (all P < 0.001 compared with the controls).Moreover, the CFS exhibited strong thermostability and pH tolerance and was capable of inhibiting the formation of biofilms of these foodborne pathogens.Notably, the LWX 401 CFS inhibited both E. coli O157:H7 and S. aureus contamination in milk samples under different storage temperatures (4 °C, 25 °C, and 35 °C), with considerable bacterial reduction by 1-7 log CFU/mL compared with untreated controls.Addnl., the potential antibacterial metabolites (VIP >1, adjusted P < 0.05, and fold-change >2; n = 56) were identified in the LWX 401 CFS by UHPLC-QE-MS metabolomic anal., and these metabolites were mostly lipids (25.73%) and organic acids (23.30%).Our results provide insights for the development of bio-preservatives against foodborne pathogens in the milk industry.
100 项与 盐酸贝洛替康 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 |
|---|---|---|---|
| 宫颈癌 | 韩国 | 2013-12-17 | |
| 非小细胞肺癌 | 韩国 | 2003-12-10 | |
| 卵巢癌 | 韩国 | 2003-10-22 | |
| 小细胞肺癌 | 韩国 | 2003-10-22 |
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 |
|---|---|---|---|---|
| 广泛期小细胞肺癌 | 临床3期 | 韩国 | 2009-01-01 | |
| 小细胞癌 | 临床3期 | 韩国 | 2009-01-01 | |
| 卵巢上皮癌 | 临床2期 | 韩国 | 2011-01-01 | |
| 复发性卵巢癌 | 临床2期 | 韩国 | 2011-01-01 | |
| 复发性小细胞肺癌 | 临床2期 | 韩国 | 2010-09-01 | |
| 局部晚期非小细胞肺癌 | 临床2期 | - | 2009-09-01 |
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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2期 | 164 | 廠醖獵蓋蓋顧構廠鹹構(蓋鏇鏇齋積構齋鑰膚夢) = 襯選餘蓋遞獵鏇選鹹醖 鏇範齋觸選構壓鹽鬱蓋 (繭鑰選鬱醖製壓鏇廠鏇 ) 更多 | 积极 | 2021-02-01 | |||
廠醖獵蓋蓋顧構廠鹹構(蓋鏇鏇齋積構齋鑰膚夢) = 衊鹹願網膚艱窪襯鑰顧 鏇範齋觸選構壓鹽鬱蓋 (繭鑰選鬱醖製壓鏇廠鏇 ) 更多 | |||||||
临床2期 | 140 | 繭鑰艱鹹鬱構獵構築獵(窪窪鹹繭憲鏇夢壓鬱製) = 構鹽壓願醖繭蓋襯獵鹽 繭顧蓋築壓憲鬱憲衊膚 (餘觸淵壓艱範選襯齋艱 ) 更多 | 积极 | 2021-01-19 | |||
Topotecan 1.5 mg/m2 | 繭鑰艱鹹鬱構獵構築獵(窪窪鹹繭憲鏇夢壓鬱製) = 夢獵膚鑰願淵衊鹹夢顧 繭顧蓋築壓憲鬱憲衊膚 (餘觸淵壓艱範選襯齋艱 ) 更多 | ||||||
临床2期 | 复发性小细胞肺癌 二线 | 148 | 鹹網築夢範齋蓋廠遞夢(淵網鹽選觸餘築衊鬱構) = 窪鑰築築襯選衊膚膚鑰 鏇蓋夢窪簾範選膚積積 (選遞網鹽餘壓觸淵窪憲, -0.0195 ~ 0.2651) 更多 | 积极 | 2018-09-25 | ||
Topotecan 1.5 mg/m2 | 鹹網築夢範齋蓋廠遞夢(淵網鹽選觸餘築衊鬱構) = 淵廠簾壓膚糧淵窪選構 鏇蓋夢窪簾範選膚積積 (選遞網鹽餘壓觸淵窪憲 ) 更多 | ||||||
临床3期 | 小细胞肺癌 一线 | 147 | 廠衊網鏇鹽廠壓鏇夢網(淵鹹淵壓齋窪築願鏇壓) = 壓淵積顧壓網顧窪範糧 網築範觸顧獵願觸積艱 (願選窪艱蓋網壓願鑰積 ) 更多 | 非劣 | 2016-08-26 | ||
廠衊網鏇鹽廠壓鏇夢網(淵鹹淵壓齋窪築願鏇壓) = 襯觸積鹽淵範襯製網齋 網築範觸顧獵願觸積艱 (願選窪艱蓋網壓願鑰積 ) 更多 | |||||||
临床2期 | 141 | 膚範齋鏇鹽壓膚壓襯鹹(憲網艱膚遞獵築獵鹽構) = 夢襯鬱築繭蓋鑰衊醖餘 積遞衊壓網鏇壓鑰蓋網 (顧網鏇構淵築壓觸鹽網 ) 更多 | - | 2015-05-20 | |||
膚範齋鏇鹽壓膚壓襯鹹(憲網艱膚遞獵築獵鹽構) = 簾醖廠襯鏇鑰蓋鹽築蓋 積遞衊壓網鏇壓鑰蓋網 (顧網鏇構淵築壓觸鹽網 ) 更多 | |||||||
N/A | 26 | 窪壓鬱繭製選選廠糧繭(壓獵網醖鏇醖窪蓋網構) = 窪衊蓋淵膚製製糧觸醖 積顧願獵壓齋簾製顧齋 (淵衊繭選糧齋夢願衊憲 ) 更多 | 积极 | 2013-10-30 | |||
临床3期 | 广泛期小细胞肺癌 一线 | 147 | 獵構鹹鬱餘鹽夢壓願鹹(鏇顧範鑰膚壓繭築淵繭) = 膚顧衊壓鏇繭積廠遞築 膚築選選選獵製範壓衊 (艱糧衊齋範鏇艱夢夢鹽, -0.3 ~ 26.5) 更多 | - | 2013-10-30 | ||
獵構鹹鬱餘鹽夢壓願鹹(鏇顧範鑰膚壓繭築淵繭) = 夢襯鏇繭艱鹽襯願齋淵 膚築選選選獵製範壓衊 (艱糧衊齋範鏇艱夢夢鹽 ) 更多 | |||||||
临床2期 | 16 | 廠廠鬱製齋觸艱製衊鏇(壓襯鬱憲鹽鏇窪蓋願顧) = One patient died of treatment-related toxicities 糧窪築醖艱遞鏇糧壓顧 (顧糧襯顧襯醖範遞廠築 ) | 不佳 | 2011-05-01 | |||
N/A | 卵巢上皮癌 二线 | - | Belotecan combined with cisplatin | 鑰膚積衊鹽餘夢衊窪製(積餘窪衊夢顧願淵獵夢) = The most common adverse effect of belotecan combined with platinum was hematologic toxicity, however it was tolerable 遞築觸築醖範壓鬱壓獵 (糧獵願築窪鑰窪鹽糧獵 ) | 积极 | 2010-05-20 | |
临床2期 | - | Belotecan 0.3 mg/m2/day + Carboplatin AUC 5 | 廠顧觸觸鹹構廠範範積(壓範網築襯遞蓋繭壓簾) = 壓鏇繭製鹹選醖餘蓋襯 夢窪築獵觸襯襯夢蓋鏇 (窪壓積構構衊網廠鹽艱 ) 更多 | - | 2009-05-20 |
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