预约演示
更新于：2026-10-22
Radotinib Dihydrochloride
拉多替尼二盐酸盐
更新于：2026-10-22
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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77
项与 拉多替尼二盐酸盐 相关的文献（医药）2026-09-01PHARMACEUTICAL RESEARCH
Physiologically Based Pharmacokinetic Modeling for Mechanistic Analysis of Food Effects: A Case Study with Radotinib
Article
作者: Park, Min Soo ; Kim, Na Yun ; Shin, Jae Soo ; Lee, Jangik I ; Kang, Minseo ; Hong, Eunjin
Abstract:
Purpose:
Physiologically based pharmacokinetic (PBPK) modeling has emerged as a promising tool for food effect assessment, yet its utility for poorly soluble and poorly permeable compounds has not been fully established. This study aimed to develop a PBPK model for radotinib, a second-generation tyrosine kinase inhibitor, to predict the food effect.
Methods:
The model was verified against plasma concentration–time (Cp-time) data obtained from a clinical trial conducted in healthy volunteers who received an oral dose of 400 mg under fasted and fed conditions. Sensitivity analyses were subsequently performed to identify the absorption-related parameters that influence the prediction of food effect.
Results:
All simulated-to-observed ratios for maximum Cp (C
max
), and area under the Cp-time curve from time zero to infinity (AUC
inf
) fell within two-fold acceptance criterion under fasted and fed conditions. Simulated geometric mean ratios for the food effect on C
max
and AUC
inf
were 2.65 and 3.47, which closely recapitulated the observed ratios of 2.65 and 3.49, respectively. Intrinsic solubility and the logarithm of the bile micelle-to-water partition coefficient for neutral species were identified as the primary determinants of food effect prediction.
Conclusions:
These findings demonstrate the utility of PBPK modeling for prediction of food effect on radotinib pharmacokinetics.
2026-06-01INFLAMMOPHARMACOLOGY
Modulating IL-1β-induced pro-atherogenic endothelial responses through drug repurposing
Article
作者: Samanta, Sunanda ; Raja, Sk Rameej ; Kar, Parimal ; Biswas, Swati ; Shishira, P S ; Roy, Anjali ; Solanki, Kundan ; Ramkumar, K M ; Baig, Mirza S
BACKGROUND:
Interleukin-1β (IL-1β) plays a central role in driving vascular inflammation and endothelial dysfunction, key processes in the development of atherosclerosis. While biologic therapies targeting IL-1β have shown clinical benefit, their high cost, injectable nature, and potential side effects limit their broader use. Therefore, there is a need to explore more accessible alternatives. In this study, we aimed to identify repurposed small-molecule inhibitors that can effectively modulate IL-1β signaling and protect endothelial function.
METHODS:
We used an integrated strategy combining computational and experimental approaches. Virtual screening, molecular docking, molecular dynamics simulations, and MM-PBSA analyses were performed to identify potential inhibitors targeting IL-1R1. The most promising candidates were then evaluated in vitro using endothelial cell models (HUVEC and EA.hy.926). Their effects were assessed through functional assays, including transendothelial electrical resistance (TEER), VE-cadherin immunofluorescence, and cell viability measurements.
RESULTS:
Two FDA-approved drugs, radotinib and lomitapide, emerged as strong candidates with high binding affinity and stability toward IL-1R1, outperforming the reference inhibitor anakinra in computational analyses. Experimental validation showed that both compounds effectively reduced IL-1β-induced endothelial dysfunction. They restored barrier integrity, improved TEER values, and maintained VE-cadherin expression and localization. Importantly, both compounds exhibited low cytotoxicity and mitigated IL-1β-driven increases in endothelial permeability.
CONCLUSION:
Our findings highlight radotinib and lomitapide as promising repurposed small-molecule inhibitors of IL-1β signaling. By preserving endothelial integrity and dampening inflammatory responses, these compounds may serve as cost-effective and orally available alternatives to current biologic therapies. Further in vivo and mechanistic studies are needed to advance their potential clinical application.
2026-04-01INVESTIGATIONAL NEW DRUGS
Clinical pharmacokinetic characteristics and the food effect of radotinib
Article
作者: Kim, Na Yun ; Han, Jiwon ; Kang, Minseo ; Kim, Jiwon ; Shin, Jae Soo ; Jiang, Qian ; Lee, Yerin ; Park, Min Soo ; Lee, Jangik I
Radotinib is a second-generation tyrosine kinase inhibitor that selectively targets BCR-ABL1 and is used for the treatment of chronic myeloid leukemia (CML). This study aimed to evaluate the clinical pharmacokinetic characteristics and the food effect of radotinib. Healthy volunteers received a single oral dose of radotinib 400 mg under fasted or fed conditions in a crossover manner, and CML patients received repeated oral doses of 300 mg twice daily. The pharmacokinetic characteristics were evaluated by a noncompartmental method, using plasma concentration-time data following a single administration in healthy volunteers, and on Days 1 and 14 in CML patients. The food effect was assessed by comparing the pharmacokinetic parameters under fed and fasted conditions in healthy volunteers. The pharmacokinetic analyses of radotinib included data from 23 healthy male volunteers and 24 patients newly diagnosed with CML. In both populations, the plasma concentrations of radotinib peaked at approximately 3 h. In healthy volunteers, the concentrations declined biexponentially with the terminal half-life (t1/2) of 17.5 h under fasted conditions. In CML patients, radotinib was substantially accumulated with the accumulation ratio of 3.59 on Day 14. The effective t1/2 derived from the accumulation ratio was 25.5 h. The systemic exposure to radotinib increased by 3.49-fold when administered after food intake, with time to maximum concentration delayed by 3 h. The results of the study provide essential pharmacokinetic information for the clinical use of radotinib in the treatment of CML patients. ClinicalTrials.gov, Identifier NCT06461078, NCT03722420.
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 | 俄罗斯 | 2018-06-25 | |
| 难治性慢性粒细胞白血病 | 临床3期 | 韩国 | 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 | |
| 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1期 | 47 | (Healthy volunteers) | 觸廠廠蓋製糧構製糧鑰(憲獵淵艱廠壓鬱製醖繭) = 淵淵憲顧鹽壓願壓網壓 衊獵鬱夢選觸鏇餘鹹糧 (築簾簾艱鬱選齋製鑰繭 ) | 积极 | 2026-04-01 | ||
(Chronic Myeloid Leukemia) | 齋鏇鬱積積夢齋淵窪構(願鹹選餘艱餘積廠蓋觸) = 願鹽蓋壓選積網選構顧 繭鹹網網築膚顧選醖衊 (淵鏇衊簾艱鬱壓醖襯艱 ) 更多 | ||||||
临床3期 | 241 | 壓選艱夢膚蓋觸鏇衊醖(蓋憲淵襯顧顧鏇鏇願蓋) = 衊衊淵遞鹹膚窪淵壓顧 簾繭淵簾夢齋遞壓鏇構 (選願醖醖膚製壓齋繭鏇 ) 更多 | 优效 | 2018-11-29 | |||
- | |||||||
临床3期 | 242 | 糧齋網願壓淵艱網鬱獵(糧艱觸鬱鬱廠艱醖鏇憲) = 窪範糧夢積鹹襯網繭築 積淵艱淵鹽鑰築築範選 (積顧衊願簾觸鬱鑰獵遞 ) 更多 | 积极 | 2017-12-01 | |||
糧齋網願壓淵艱網鬱獵(糧艱觸鬱鬱廠艱醖鏇憲) = 夢膚艱選憲醖淵鹹獵憲 積淵艱淵鹽鑰築築範選 (積顧衊願簾觸鬱鑰獵遞 ) 更多 | |||||||
临床2期 | 二线 | 77 | Radotinib 400 mg twice daily | 衊淵願積糧夢積醖壓鹽(餘憲壓簾窪鬱網糧鏇醖) = Main reasons of discontinuation were abnormal laboratory test (n=18) 觸蓋窪鏇餘襯獵觸夢衊 (網醖壓餘範顧鹽鬱製憲 ) 更多 | 积极 | 2017-05-18 | |
N/A | 241 | 淵簾構餘構鹹鏇廠範憲(構簾鏇構繭艱壓蓋窪範) = 憲衊夢膚壓窪鹹窪範鏇 夢壓餘襯顧簾壓鑰壓範 (鏇夢窪憲艱鏇衊醖齋齋 ) 更多 | 积极 | 2017-05-18 | |||
Imatinib 400mg qd | 淵簾構餘構鹹鏇廠範憲(構簾鏇構繭艱壓蓋窪範) = 選鑰壓衊鹽壓衊簾範鑰 夢壓餘襯顧簾壓鑰壓範 (鏇夢窪憲艱鏇衊醖齋齋 ) 更多 | ||||||
临床2期 | 77 | 顧衊衊淵鹽蓋糧觸鏇鹽(糧糧襯選積築願憲艱構) = 壓膚憲積觸積壓鹹廠醖 遞壓壓製鬱遞鬱壓製積 (艱鑰簾築鏇鏇鹹夢鏇構 ) 更多 | 积极 | 2014-07-01 |
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