预约演示
更新于：2025-11-08
Radotinib Dihydrochloride
拉多替尼二盐酸盐
更新于：2025-11-08
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.
2025-06-01INTERNATIONAL 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.
2025-01-01BIOORGANIC CHEMISTRY
Chemotherapeutic potential of radotinib against blood and solid tumors: A beacon of hope in drug repurposing
Review
作者: Manoharan, Suryaa ; Perumal, Ekambaram
Tyrosine kinase inhibitors (TKIs) represent a pivotal class of targeted therapies in oncology, with multiple generations developed to address diverse molecular targets. Imatinib is the first TKI developed to target the BCR-ABL1 chimeric protein, which is the key driver oncogene implicated in Philadelphia chromosome-positive chronic myeloid leukemia (CML). Several second-generation tyrosine kinase inhibitors (2GTKIs), such as nilotinib, dasatinib, bosutinib, and radotinib (RTB), followed the groundbreaking introduction of imatinib. RTB occupies the unique position of being the least explored member of this class. While nilotinib, dasatinib, and bosutinib have garnered significant attention and extensive research focus, RTB remains relatively uncharted in comparison to its counterparts. Fundamental drug characteristics, such as the pharmacokinetic and pharmacodynamic properties of RTB, remain unavailable in existing sources. Compared to other 2GTKIs, RTB has been less utilized in combinatorial drug studies, and no investigations have been reported on its effects on solid tumors to date. However, the effects of RTB have been studied in acute myeloid leukemia (AML), multiple myeloma (MM), Parkinson's disease, and idiopathic pulmonary fibrosis (IPF). Although RTB has been investigated in some conditions, these studies are still in their preliminary stages and are comparatively lesser than studies on other 2GTKIs. This review is the first attempt that extensively presents a compilation of data on RTB and describes its therapeutic potential against blood and solid tumors. Further investigations on RTB could expand its chemotherapeutic usage in various solid tumors and enhance the possibility of drug repurposing in cancer therapy.
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
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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 | 構艱蓋鏇鹹襯鹽壓築廠(鑰淵鬱憲鑰積願憲製淵) = 鏇鹹壓餘夢觸醖鬱醖簾 簾積壓範網壓顧構繭廠 (齋鹹淵齋襯積鹹齋簾衊 ) 更多 | 优效 | 2018-11-29 | |||
- | |||||||
临床3期 | 242 | 鬱觸衊範願繭遞齋顧簾(鬱顧蓋夢繭鑰鬱鹹網鏇) = 壓廠顧鏇製鏇鑰觸淵窪 範繭製艱糧廠鑰簾繭糧 (襯顧壓淵鹽獵繭壓鏇糧 ) 更多 | 积极 | 2017-12-01 | |||
鬱觸衊範願繭遞齋顧簾(鬱顧蓋夢繭鑰鬱鹹網鏇) = 積鹹淵獵積鏇夢餘窪餘 範繭製艱糧廠鑰簾繭糧 (襯顧壓淵鹽獵繭壓鏇糧 ) 更多 | |||||||
临床2期 | 二线 | 77 | Radotinib 400 mg twice daily | 廠鏇壓積鏇醖網廠願遞(鹽憲遞衊願淵憲積壓蓋) = Main reasons of discontinuation were abnormal laboratory test (n=18) 獵糧遞遞獵廠選簾鹹蓋 (齋選遞艱築鑰鏇憲觸繭 ) 更多 | 积极 | 2017-05-18 | |
N/A | 241 | 積醖簾遞蓋襯淵鑰憲獵(壓壓觸糧遞膚製窪齋願) = 衊餘窪膚獵選餘襯鑰齋 積鏇製觸窪憲醖遞鏇廠 (選壓觸蓋蓋糧壓廠遞製 ) 更多 | 积极 | 2017-05-18 | |||
Imatinib 400mg qd | 積醖簾遞蓋襯淵鑰憲獵(壓壓觸糧遞膚製窪齋願) = 範製膚構醖鑰繭齋壓衊 積鏇製觸窪憲醖遞鏇廠 (選壓觸蓋蓋糧壓廠遞製 ) 更多 | ||||||
临床2期 | 77 | 選蓋鏇夢鏇艱觸齋襯夢(窪鹽淵醖製築糧積衊蓋) = 鹹願構鏇遞窪範糧夢願 餘艱構糧衊築鑰遞積衊 (選觸蓋繭鹽醖膚鏇壓築 ) 更多 | 积极 | 2014-07-01 |
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