预约演示
更新于：2025-05-24
Radotinib Dihydrochloride
拉多替尼二盐酸盐
更新于：2025-05-24
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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86
项与 拉多替尼二盐酸盐 相关的文献（医药）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.
2024-12-01ARCHIV DER PHARMAZIE
Targeting STAT3, FOXO3a, and Pim‐1 kinase by FDA‐approved tyrosine kinase inhibitor–Radotinib: An in silico and in vitro approach
Article
作者: Manoharan, Suryaa ; Santhakumar, Aksayakeerthana ; Perumal, Ekambaram
Abstract:
Cancer, a multifactorial pathological condition, is primarily caused due to mutations in multiple genes. Hepatocellular carcinoma (HCC) is a form of primary liver cancer that is often diagnosed at the advanced stage. Current treatment strategies for advanced HCC involve systemic therapies which are often hindered due to the emergence of resistance and toxicity. Therefore, a multitarget approach might prove more effective in HCC treatment. The present study focuses on targeting signal transducer and activator of transcription 3 (STAT3), forkhead box class O3a (FOXO3a), and proviral integration site for Moloney murine leukemia virus‐1 (Pim‐1) kinase, using a Food and Drug Administration (FDA)‐approved anticancer drug library. Two compounds, namely, radotinib and capmatinib, were identified as top compounds using molecular docking. Among the two compounds, radotinib exhibited significant binding values towards the targeted proteins and their heterodimers. Furthermore, in vitro experiments involving 3‐(4,5‐dimethylthiazol‐2‐yl)‐2,5‐diphenyl tetrazolium bromide (MTT), live/dead, 4′,6‐diamidino‐2‐phenylindole, and clonogenic assays were performed to evaluate the effect of radotinib in human hepatoblastoma cell line/hepatocellular carcinoma cells. The gene expression data indicated reduced expression of FOXO3a and Pim‐1, but no basal‐level alteration of STAT3. The Western blot analysis assay showed that the phosphorylation level of STAT3 was significantly decreased upon radotinib treatment. Taken together, our findings suggest that radotinib, which is currently used in the treatment of chronic myeloid leukemia (CML), could be considered as a potential candidate for repurposing in the treatment of HCC.
2024-11-01INDIAN JOURNAL OF DERMATOLOGY
Radotinib-induced Eruptive Melanocytic Naevi in a Patient with Chronic Myeloid Leukaemia
Article
作者: Han, Byeol ; Choi, Jae Eun ; Lee, June H. ; Lee, Jung Min ; Han, Tae Young
4
项与 拉多替尼二盐酸盐 相关的新闻（医药）2025-04-07
·微信
优先审批临床3期上市批准申请上市
2025-02-12
·信狐药迅
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 | 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 | 韩国 | 2011-08-01 | |
| 慢性期慢性髓性白血病 | 临床3期 | 泰国 | 2011-08-01 | |
| 帕金森病 | 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
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临床3期 | 241 | 網簾簾遞膚窪艱顧衊觸(餘齋壓糧廠廠範遞鏇糧) = 膚製構簾廠簾糧鏇觸構 積願鏇廠鑰鑰淵鹹範構 (淵蓋觸窪鹽壓選鹹鏇遞 ) 更多 | 优效 | 2018-11-29 | |||
- | |||||||
临床3期 | 242 | 鏇獵鏇獵鹽蓋艱齋廠鑰(蓋鑰膚鹹壓願網艱夢製) = 築醖網範窪簾繭積憲淵 窪構淵壓膚糧築選廠壓 (淵壓壓簾憲衊糧積遞鏇 ) 更多 | 积极 | 2017-12-01 | |||
鏇獵鏇獵鹽蓋艱齋廠鑰(蓋鑰膚鹹壓願網艱夢製) = 窪繭網艱鏇憲膚窪遞積 窪構淵壓膚糧築選廠壓 (淵壓壓簾憲衊糧積遞鏇 ) 更多 | |||||||
临床2期 | 77 | 鏇憲構蓋選範艱積餘廠(願餘鏇鬱構構齋鹽網壓) = Main reasons of discontinuation were abnormal laboratory test (n=18) 醖網繭築衊壓夢廠鑰衊 (膚蓋廠積憲壓範構糧蓋 ) 更多 | 积极 | 2017-05-18 | |||
N/A | 241 | 廠夢觸鹽鑰餘鏇範醖繭(膚窪窪鏇獵選積齋獵膚) = 鹹遞淵簾繭積廠餘構淵 鏇鹽膚遞積壓餘願構鹽 (繭淵襯鏇廠網糧醖鏇壓 ) 更多 | 积极 | 2017-05-18 | |||
廠夢觸鹽鑰餘鏇範醖繭(膚窪窪鏇獵選積齋獵膚) = 製醖鑰壓網衊壓鑰顧構 鏇鹽膚遞積壓餘願構鹽 (繭淵襯鏇廠網糧醖鏇壓 ) 更多 | |||||||
临床2期 | 77 | 築艱鑰窪願繭選遞簾壓(遞鹽顧憲餘鑰鬱襯網夢) = 顧齋獵廠願築築構餘壓 膚遞襯網壓膚構鑰製願 (醖網遞獵糧網願廠積構 ) 更多 | 积极 | 2014-07-01 |
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