预约演示
更新于：2025-12-14
Rovadicitinib
罗伐昔替尼
更新于：2025-12-14
概要
基本信息
药物类型 小分子化药 |
别名 CT-1995、TQ 05105、TQ-05105 + [1] |
作用方式 抑制剂 |
作用机制 JAK1抑制剂(酪氨酸蛋白激酶JAK1抑制剂)、JAK2抑制剂(酪氨酸蛋白激酶JAK2抑制剂)、ROCK1抑制剂(Rho相关蛋白激酶-1抑制剂) |
在研适应症 |
原研机构 |
非在研机构- |
最高研发阶段申请上市 |
首次获批日期- |
最高研发阶段(中国)申请上市 |
特殊审评突破性疗法 (中国) |
登录后查看时间轴
结构/序列
分子式C17H19N7 |
InChIKeyZGENDZDSLYKCSI-CQSZACIVSA-N |
CAS号1948242-59-8 |
关联
18
项与 罗伐昔替尼 相关的临床试验NCT06682169
A Randomized, Open Label, Positive Controlled, Multicenter Phase III Clinical Trial Evaluating the Efficacy and Safety of the Selected Regimen of Rovadicitinib in Moderate to Severe Chronic Graft-versus-host Disease in Third Line and Beyond
NCT06598956
An Open, Parallel, Single-dose Phase I Clinical Study to Evaluate the Pharmacokinetics and Safety of TQ05105 Tablets in Patients With Different Levels of Renal Function
NCT06245941
A Phase Ib/II Clinical Trial of TQ05105 Tablets Combined With TQB3909 Tablets in the Treatment of Moderate- and High-risk Myelofibrosis
100 项与 罗伐昔替尼 相关的临床结果
登录后查看更多信息
100 项与 罗伐昔替尼 相关的转化医学
登录后查看更多信息
100 项与 罗伐昔替尼 相关的专利（医药）
登录后查看更多信息
5
项与 罗伐昔替尼 相关的文献（医药）2025-12-01CANCER CHEMOTHERAPY AND PHARMACOLOGY
Food effect trial of the pharmacokinetics and safety of TQ05105 in healthy Chinese subjects
Article
作者: Yang, Haimiao ; Su, Zhengjie ; Cui, Yingzi ; Liu, Zhengzhi ; Zhou, Yannan ; Cheng, Yang ; Dai, Jun ; Wang, Yanli ; Ren, Qing ; Deng, Qiaohuan
PURPOSE:
This study aims to investigate the effect of food intake on the pharmacokinetics of TQ05105 tablets in healthy Chinese subjects, and to evaluate the safety in these subjects.
METHODS:
This Phase I clinical trial involved healthy subjects who received a single oral dose of 15 mg TQ05105, with a 2-day washout period between each period. The plasma concentrations of TQ05105 and its metabolite TQ12550 were quantified using a validated liquid chromatography-tandem mass spectrometry method. Safety assessments were conducted throughout the study.
RESULTS:
The study enrolled 16 healthy Chinese subjects (10 males and 6 females). Compared with the fasting condition, the postprandial administration of TQ05105 resulted in significant reductions in the maximum concentration (Cmax) and area under the curve (AUC) of both TQ05105 and its metabolite TQ12550. Additionally, both the time to peak concentration (Tmax) and half-life (t1/2) of TQ05105 and its metabolite were prolonged under postprandial conditions. No serious adverse events were reported during the study.
CONCLUSION:
The findings demonstrate that food intake significantly alters the pharmacokinetic parameters of TQ05105 and its metabolite TQ12550, with a notable decrease in Cmax and AUC, and an increase in Tmax and t1/2. The single dose of the drug was well tolerated.
REGISTRATION INFORMATION:
This trial had registered at the Clinical Trials.gov on August 08, 2023 ( https://clinicaltrials.gov , NCT05982106).
2025-10-01EUROPEAN JOURNAL OF PHARMACOLOGY
A first-in-class JAK/ROCK inhibitor, Rovadicitinib in patients with myelofibrosis who were refractory or relapsed or intolerant to Ruxolitinib: A single-arm, multicenter, open-label, phase Ib study
Article
作者: Gao, Sujun ; Ding, Dawei ; Song, Luxi ; Lao, Shanli ; Hong, Minghua ; Wu, Duoer ; Yu, Ding ; Zhang, Min ; Chang, Chunkang
Patients with myelofibrosis (MF) who were relapsed or refractory, or intolerant to Ruxolitinib, have limited effective treatment options, and the outcome after discontinuation of Ruxolitinib is poor. Rovadicitinib (TQ05105) is a first-in-class, oral, small-molecule Janus kinase (JAK)/Rho-associated kinase (ROCK) inhibitor. Rovadicitinib has demonstrated significant clinical benefits in MF patients for spleen responses and reduced symptom burden. Here, we report safety and efficacy from a single-arm, multicenter, open-label, phase Ib study evaluating Rovadicitinib in MF patients resistant or intolerant to prior Ruxolitinib (NCT06388759). Between August 1, 2022, and September 05, 2023, patients were assessed for eligibility, and 9 patients were enrolled. The median duration of prior Ruxolitinib exposure was 40.6 months. At a median Rovadicitinib exposure of 12.5 months, the most common grade ≥3 treatment-emergent adverse event was thrombocytopenia (33.3 %). No report of a bleeding event and only one of 9 patients (11.1 %) permanently discontinued Rovadicitinib treatment. The spleen volume response rate (≥35 % spleen volume decrease from baseline to end of cycle 6 [EOC6]) was 25.0 %. Symptom response rate (≥50 % reduction from baseline to EOC6 in total symptom score on the modified Myelofibrosis Symptom Assessment Form) was 37.5 %. This study suggests that patients with MF who are intolerant or resistant to Ruxolitinib or other JAK inhibitors might achieve significant clinical benefit after treatment with Rovadicitinib. TRIAL REGISTRATION: clinicaltrials.gov Identifier: NCT06388759.
2025-06-12BLOOD
A first-in-class JAK/ROCK inhibitor, rovadicitinib, for glucocorticoid-refractory or -dependent chronic GVHD
Article
作者: Lai, Xiaoyu Y. ; Zhao, Yanmin M. ; Wang, Xunqiang Q. ; Zhang, Xuejun J. ; Liu, Lizhen Z. ; Meng, Fankai K. ; Shi, Jimin M. ; Wang, Shunqing Q. ; Luo, Yi ; Huang, He ; Liang, Chen ; Zhu, Xiaoyu Y. ; Fu, Huarui R. ; Wang, Caixia K. ; Tu, Lifan F. ; Yu, Jian ; Jin, Hua ; Ye, Yishan S. ; Zhao, Yeqian Q. ; Jiang, Erlie L. ; Wang, Tao ; Zhang, Congxiao X.
Abstract:
Rovadicitinib (TQ05105) is a novel, oral dual Janus kinase 1/2 and rho-associated coiled-coil–containing protein kinase-1/2 inhibitor targeting inflammatory and fibrotic components of chronic graft-versus-host disease (cGVHD). This phase 1b/2a, multicenter, open-label study enrolled patients with moderate or severe glucocorticoid-refractory or -dependent cGVHD to evaluate the safety and efficacy of rovadicitinib. The study followed a 3+3 design with 2 escalating doses (rovadicitinib 10 and 15 mg twice daily) and a dose expansion cohort. Primary end points included safety and recommended phase 2 dose (RP2D); the best overall response (BOR) was the key secondary end point. A total of 44 patients were enrolled (29 at 10 mg, 15 at 15 mg twice daily). Rovadicitinib was well tolerated without dose-limiting toxicity at both dosages, and no rovadicitinib-related adverse events (AEs) led to discontinuation. The most prevalent hematological AE was anemia (38.6%), with grade ≥3 of 4.6%. The RP2D was 10 mg twice daily. The BOR was 86.4% (95% confidence interval [CI], 72.6-94.8), with no difference between the 2 dosage cohorts. Besides, BOR was 72.7% in the steroid-refractory cohort and 90.9% in the steroid-dependent cohort. All affected organs exhibited responses regardless of prior therapy. The failure-free survival rate was 85.2% (95% CI, 64.5-94.3) at 12 months. Rovadicitinib reduced corticosteroid doses in 88.6% of patients and improved cGVHD symptoms in 59.1%. Rovadicitinib has favorable tolerability and notable clinical response rates, ameliorating the quality of life and reducing corticosteroid dose requirements in patients with glucocorticoid-refractory or -dependent cGVHD. This trial was registered at www.ClinicalTrials.gov as #NCT04944043.
107
项与 罗伐昔替尼 相关的新闻（医药）2025-12-12
CSCO会议临床结果上市批准临床3期
2025-12-11
免疫疗法临床结果细胞疗法临床1期临床2期
100 项与 罗伐昔替尼 相关的药物交易
登录后查看更多信息
研发状态
10 条进展最快的记录, 后查看更多信息
登录
| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 骨髓纤维化 | 申请上市 | 中国 | 2024-07-13 | |
| 慢性移植物抗宿主病 | 临床3期 | 中国 | 2024-11-12 | |
| 噬血细胞性淋巴组织细胞增多症 | 临床2期 | 中国 | 2024-12-05 | |
| 原发性血小板增多症后骨髓纤维化 | 临床2期 | 中国 | 2023-12-12 | |
| 真性红细胞增多症后骨髓纤维化 | 临床2期 | 中国 | 2023-12-12 | |
| 难治性急性移植物抗宿主病 | 临床2期 | 中国 | 2022-06-10 | |
| 类固醇难治性移植物抗宿主病 | 临床2期 | 中国 | 2022-06-10 | |
| 高危骨髓增生异常综合征 | 临床2期 | 中国 | 2021-11-11 | |
| 原发性骨髓纤维化 | 临床2期 | 中国 | 2021-11-11 | |
| 急性移植物抗宿主病 | 临床1期 | 中国 | 2022-06-10 |
登录后查看更多信息
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 | 9 | 壓顧憲範淵願鬱顧夢衊(壓構選齋積鏇鑰淵淵蓋) = 淵顧艱築獵衊鏇餘憲積 鹽範餘簾憲鬱壓壓夢鹹 (網構構顧繭簾築淵窪廠 ) 更多 | 积极 | 2025-10-01 | |||
临床1/2期 | 44 | 鬱蓋築艱淵簾鹹艱鏇醖(艱蓋網築艱繭鏇鹹願顧) = 網糧膚鹹鏇憲簾憲糧憲 壓廠憲齋繭艱鏇構鑰襯 (鹽觸糧鹽願繭蓋選醖鏇 ) 更多 | 积极 | 2025-06-12 | |||
鬱蓋築艱淵簾鹹艱鏇醖(艱蓋網築艱繭鏇鹹願顧) = 憲築願繭艱膚構願襯艱 壓廠憲齋繭艱鏇構鑰襯 (鹽觸糧鹽願繭蓋選醖鏇 ) 更多 | |||||||
临床1期 | 13 | 餘壓鹽網簾醖壓糧觸築(鹽築鹹夢簾製憲鏇膚艱) = 廠餘積構簾醖鹹網選憲 範積餘獵鏇構鹹齋齋憲 (鬱襯鹽廠壓鬱構鏇鏇範, 54.5 ~ 98.1) 更多 | 积极 | 2025-05-14 | |||
临床1期 | 11 | 觸築鑰鹹範網壓鹹鬱網(醖艱鹹衊鏇製夢繭獵積) = None 夢繭顧蓋廠淵憲糧夢餘 (膚夢網觸築夢範構壓窪 ) 更多 | 积极 | 2024-12-09 | |||
临床1期 | 骨髓纤维化 二线 | 9 | 餘鏇襯鏇鏇糧積積衊蓋(艱艱糧簾蓋選餘積網築) = 齋蓋鬱願醖糧鹽製築淵 鏇製願積製膚繭齋壓觸 (糧齋積廠選獵鑰選鹹醖 ) 更多 | 积极 | 2024-12-08 | ||
临床1/2期 | 44 | Rovadicitinib 10mg BID | 獵窪淵廠襯觸鏇蓋壓獵(艱觸膚醖齋齋獵鹽網壓) = 醖獵簾壓糧遞醖遞選襯 壓構範鑰廠築積繭膚鹽 (淵衊艱選遞願壓夢鑰範 ) 更多 | 积极 | 2024-12-07 | ||
Rovadicitinib 15mg BID | 獵窪淵廠襯觸鏇蓋壓獵(艱觸膚醖齋齋獵鹽網壓) = 衊築選蓋簾積窪膚簾壓 壓構範鑰廠築積繭膚鹽 (淵衊艱選遞願壓夢鑰範 ) 更多 | ||||||
临床2期 | 107 | 願鹹艱蓋選淵觸簾淵鬱(築鑰衊顧鏇壓餘繭範鬱) = 簾願膚築積壓簾選廠築 簾構衊願積艱願範獵製 (願簾網選簾構顧願衊鏇 ) 更多 | 积极 | 2024-09-13 | |||
願鹹艱蓋選淵觸簾淵鬱(築鑰衊顧鏇壓餘繭範鬱) = 夢網醖艱鏇艱範襯齋鑰 簾構衊願積艱願範獵製 (願簾網選簾構顧願衊鏇 ) 更多 | |||||||
临床1期 | 79 | 積鬱醖餘廠夢選鹽顧膚(醖鹹網築餘顧鬱選顧糧) = 蓋淵鏇願鑰製淵廠築鹽 範糧壓鬱壓鏇觸衊顧壓 (膚糧膚鏇襯糧鑰鬱觸壓 ) 更多 | 积极 | 2023-12-09 | |||
临床1/2期 | 30 | 鑰窪積壓網衊艱鹹鑰範(襯築鑰鬱窪壓襯襯製淵) = 夢顧壓鹹繭齋夢繭艱餘 餘簾網膚簾淵顧廠齋壓 (願築襯繭觸選鬱衊顧膚 ) 更多 | - | 2023-06-08 | |||
鑰窪積壓網衊艱鹹鑰範(襯築鑰鬱窪壓襯襯製淵) = 齋憲鏇鑰蓋憲範齋製製 餘簾網膚簾淵顧廠齋壓 (願築襯繭觸選鬱衊顧膚 ) 更多 |
登录后查看更多信息
转化医学
使用我们的转化医学数据加速您的研究。
登录
或
药物交易
使用我们的药物交易数据加速您的研究。
登录
或
核心专利
使用我们的核心专利数据促进您的研究。
登录
或
临床分析
紧跟全球注册中心的最新临床试验。
登录
或
批准
利用最新的监管批准信息加速您的研究。
登录
或
特殊审评
只需点击几下即可了解关键药物信息。
登录
或
生物医药百科问答
全新生物医药AI Agent 覆盖科研全链路，让突破性发现快人一步
立即开始免费试用!
智慧芽新药情报库是智慧芽专为生命科学人士构建的基于AI的创新药情报平台，助您全方位提升您的研发与决策效率。
立即开始数据试用!
智慧芽新药库数据也通过智慧芽数据服务平台，以API或者数据包形式对外开放，助您更加充分利用智慧芽新药情报信息。
生物序列数据库
生物药研发创新
免费使用
化学结构数据库
小分子化药研发创新
免费使用