预约演示
更新于：2025-11-15
Radotinib Dihydrochloride
拉多替尼二盐酸盐
更新于：2025-11-15
概要
基本信息
药物类型 小分子化药 |
别名 Radotinib、Radotinib hydrochloride、Supect + [4] |
作用方式 抑制剂、拮抗剂 |
作用机制 Bcr-Abl抑制剂(bcr-abl酪氨酸激酶抑制剂)、PDGFR拮抗剂(血小板衍生生长因子受体拮抗剂) |
在研适应症 |
非在研适应症- |
非在研机构- |
权益机构- |
最高研发阶段批准上市 |
首次获批日期 韩国 (2012-01-05), |
最高研发阶段(中国)申请上市 |
特殊审评- |
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结构/序列
分子式C27H23Cl2F3N8O |
InChIKeyGEWCZTBAWRSKBX-UHFFFAOYSA-N |
CAS号926037-85-6 |
关联
9
项与 拉多替尼二盐酸盐 相关的临床试验NCT06665412
A Single-arm, Open-label, Multicenter, Investigator-led Observational Study to Evaluate the Efficacy and Safety of Dose Reduction of Radotinib as a First-line Treatment in Patients With Newly Diagnosed Chronic Phase Ph+ Chronic Myeloid Leukemia.
NCT06461078
A Randomized, Open-label, Single-dose, Two-way Crossover Clinical Trial to Investigate the Effects of Food on the Pharmacokinetics and Safety of Orally Administered Radotinib in Healthy Adults
NCT04691661
A Randomized Double-blind Placebo-controlled Multicentre Study to Assess Safety, Tolerability, Pharmacokinetics and Efficacy of Radotinib in Parkinson's Disease
100 项与 拉多替尼二盐酸盐 相关的临床结果
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100 项与 拉多替尼二盐酸盐 相关的转化医学
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100 项与 拉多替尼二盐酸盐 相关的专利（医药）
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81
项与 拉多替尼二盐酸盐 相关的文献（医药）2025-12-01Drug Metabolism and Pharmacokinetics
Tyrosine kinase inhibitors, nilotinib and radotinib, suppress both catalytic function and mRNA expression of human cytochrome P450 2J2 and 2C8
Article
作者: Yamazaki, Hiroshi ; Katoh, Miki ; Kojima, Ayaka ; Nadai, Masayuki
Cytochrome P450 (P450 or CYP) 2J2, which metabolizes exogenous medicines and endogenous arachidonic acid to 14,15-epoxyeicosatrienoic acid (14,15-EET), is expressed in various organs and cancer cells. Additionally, CYP2C8 catalyzes the synthesis of 14,15-EET, a vasodilator that promotes cancer cell proliferation. However, the effect of tyrosine kinase inhibitors (TKIs) used in leukemia treatment on CYP2J2 and CYP2C8 remains unclear. This study investigated the effects of 16 TKIs used for leukemia treatment on recombinant CYP2J2-and CYP2C8-mediated processes. Among the TKIs, nilotinib and radotinib strongly inhibited CYP2J2-dependent astemizole O-demethylation and rivaroxaban hydroxylation, and CYP2C8-mediated paclitaxel 6α-hydroxylation (<20 %), with competitive inhibition constants of 0.41 and 0.22 μM, respectively (for astemizole O-demethylation). Nilotinib and radotinib suppressed CYP2J2-and CYP2C8-catalyzed arachidonic acid epoxidation and decreased their mRNA expression in Huh-7 cells (possibly via the peroxisome proliferator-activated receptor α pathway). Given that their inhibition constants are lower than their reported plasma concentrations, both may substantially suppress CYP2J2 and CYP2C8 functional enzyme levels and enzymatic activities in clinical settings. This suppression could potentially alter vasodilation by affecting 14,15-EET production, influencing CYP2J2 and CYP2C8-mediated drug-disease (conditions) and drug-drug interactions.
2025-09-22Journal of biomolecular structure & dynamics
Hematopoietic cell kinase as a nexus for drug repurposing: implications for cancer and HIV therapy
Article
作者: Almoyad, Mohammad Ali Abdullah ; Alsayari, Abdulrhman ; Wahab, Shadma ; Chandra, Subhash
Hematopoietic cell kinase (HCK) has emerged as a potential target for therapeutic intervention in cancer and HIV infection because of its critical role in critical signaling pathways. Repurposing FDA-approved drugs offers an efficient strategy to identify new treatment options. Here, we address the need for novel therapies in cancer and HIV by investigating the potential of repurposed drugs against HCK. Our goal was to identify promising drug candidates with high binding affinities and specific interactions within the HCK binding pocket. We employed an integrated computational approach combining molecular docking and extensive molecular dynamics (MD) simulations. Initially, we analyzed the binding affinities and interaction patterns of a library of FDA-approved drugs sourced from DrugBank. After careful analysis, we focused on two compounds, Nilotinib and Radotinib, which exhibit exceptional binding affinities and specificity to the HCK binding pocket, including the active site. Additionally, we assessed the pharmacological properties of Nilotinib and Radotinib, making them attractive candidates for further drug development. Extensive all-atom MD simulations spanning 200 nanoseconds (ns) elucidated the conformational dynamics and stability of the HCK-Nilotinib and HCK-Radotinib complexes. These simulations demonstrate the robustness of these complexes over extended timescales. Our findings highlighted the potential of Nilotinib and Radotinib as promising candidates against HCK that offer valuable insights into their binding mechanisms. This computational approach provides a comprehensive understanding of drug interactions with HCK and sets the stage for future experimental validation and drug development endeavors.
2025-06-01INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
Subtractive proteomics unravel the potency of D-alanine-D-alanine ligase as the drug target for Burkholderia pseudomallei
Article
作者: Hazra, Ditipriya ; Rahman, Shakilur ; Ganguly, Manisha ; Roychowdhury, Amlan ; Das, Amit Kumar ; Bhattacharya, Ayush ; Jana, Prerona
Melioidosis, also known as Whitmore's disease, is caused by the deadly pathogen Burkholderia pseudomallei and remains a significant global health concern, particularly in South Asia. The disease is contracted through exposure to contaminated soil, water, air, and food. Infected individuals often present with abscesses in internal organs such as the lungs, spleen, and liver, and in soft tissues, with severe cases leading to septic shock and acute pneumonia. The rising incidence and mortality rates, coupled with B. pseudomallei's ability to form biofilms and develop resistance to antibiotics like cephalosporins, make treatment increasingly challenging. This highlights the urgent need for novel therapeutic approaches. D-Alanine-D-Alanine ligase (Ddl), a crucial enzyme involved in the final stage of bacterial cell wall synthesis, which protects the pathogen from the hostile cellular environment of the host. While many bacteria have two isoforms of this enzyme, B. pseudomallei possesses only the DdlB isoform, presenting a significant vulnerability. Our study represents the first successful attempt to target DdlB through a combination of molecular docking and molecular dynamics simulations. These investigations provide strong evidence that Conivaptan acts as an effective inhibitor of DdlB, offering a novel therapeutic approach for combating melioidosis.
4
项与 拉多替尼二盐酸盐 相关的新闻（医药）2025-04-07
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2025-02-12
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2025-01-27
·医药观澜
siRNA临床3期突破性疗法临床结果上市批准
100 项与 拉多替尼二盐酸盐 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 |
|---|---|---|---|
| 费城染色体阳性慢性粒细胞白血病 | 韩国 | 2012-01-05 |
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 |
|---|---|---|---|---|
| 难治性慢性粒细胞白血病 | 临床3期 | 美国 | 2018-06-25 | |
| 难治性慢性粒细胞白血病 | 临床3期 | 俄罗斯 | 2018-06-25 | |
| 难治性慢性粒细胞白血病 | 临床3期 | 土耳其 | 2018-06-25 | |
| 难治性慢性粒细胞白血病 | 临床3期 | 乌克兰 | 2018-06-25 | |
| 慢性期慢性髓性白血病 | 临床3期 | 美国 | 2011-08-01 | |
| 慢性期慢性髓性白血病 | 临床3期 | 印尼 | 2011-08-01 | |
| 慢性期慢性髓性白血病 | 临床3期 | 菲律宾 | 2011-08-01 | |
| 慢性期慢性髓性白血病 | 临床3期 | 泰国 | 2011-08-01 | |
| 婴儿帕金森病-肌张力障碍 | 临床2期 | 法国 | 2021-09-09 |
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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 | 241 | 網齋簾齋鑰餘衊構憲齋(衊淵蓋齋衊鹽齋顧鏇觸) = 鬱鹽網齋獵獵淵膚網齋 範醖網齋鹹蓋餘鏇築蓋 (獵鹽選衊鏇鏇衊構醖淵 ) 更多 | 优效 | 2018-11-29 | |||
- | |||||||
临床3期 | 242 | 襯築簾積網遞選構憲齋(鏇廠糧齋積獵鏇製廠衊) = 膚窪鏇襯憲艱範願糧糧 廠齋膚鬱廠鏇觸積簾觸 (壓襯觸遞壓鑰遞鏇願艱 ) 更多 | 积极 | 2017-12-01 | |||
襯築簾積網遞選構憲齋(鏇廠糧齋積獵鏇製廠衊) = 簾襯膚積鬱鑰觸顧範鹽 廠齋膚鬱廠鏇觸積簾觸 (壓襯觸遞壓鑰遞鏇願艱 ) 更多 | |||||||
临床2期 | 二线 | 77 | Radotinib 400 mg twice daily | 繭選膚鬱鏇遞廠蓋積蓋(願鏇餘鹽顧網鏇範願鏇) = Main reasons of discontinuation were abnormal laboratory test (n=18) 鹹獵廠網醖淵淵糧觸觸 (網鑰憲觸願願淵構壓廠 ) 更多 | 积极 | 2017-05-18 | |
N/A | 241 | 艱蓋積範蓋網構廠窪醖(積簾獵簾願鏇願鹹齋遞) = 鏇鑰齋壓積鹽餘鹹鏇願 網壓積齋醖願齋製網憲 (鹽淵積糧範獵鬱遞構憲 ) 更多 | 积极 | 2017-05-18 | |||
Imatinib 400mg qd | 艱蓋積範蓋網構廠窪醖(積簾獵簾願鏇願鹹齋遞) = 選淵範範壓獵選選觸築 網壓積齋醖願齋製網憲 (鹽淵積糧範獵鬱遞構憲 ) 更多 | ||||||
临床2期 | 77 | 觸獵憲顧網顧襯蓋鏇壓(簾鹹憲膚壓憲範獵蓋膚) = 夢壓獵窪構網顧鏇艱艱 選夢糧簾艱蓋夢鏇壓憲 (憲夢衊觸糧窪憲網築繭 ) 更多 | 积极 | 2014-07-01 |
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