预约演示
更新于：2025-09-02
Rifasutenizol
瑞法舒坦唑
更新于：2025-09-02
概要
基本信息
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 |
特殊审评快速通道 (美国)、合格传染病产品 (美国) |
登录后查看时间轴
结构/序列
分子式C47H59N7O13 |
InChIKeyAJVPRSDTABRSLD-IAANOTQRSA-N |
CAS号1001314-13-1 |
关联
12
项与 瑞法舒坦唑 相关的临床试验NCT06551623
A Single Center, Open Label, Phase 1 Study in Healthy Participants to Investigate the Drug-Drug Interactions Between TNP-2198 and Midazolam, Clarithromycin
CTR20242839
在健康受试者中评价TNP-2198与咪达唑仑、克拉霉素药物相互作用的单中心、开放、I 期临床研究
NCT05857163
Phase 3 Clinical Trial to Evaluate the Efficacy and Safety of Rifasutenizol (TNP 2198) in Combination With Rabeprazole and Amoxicillin in the Primary Treatment of Participants With H. Pylori Infection
100 项与 瑞法舒坦唑 相关的临床结果
登录后查看更多信息
100 项与 瑞法舒坦唑 相关的转化医学
登录后查看更多信息
100 项与 瑞法舒坦唑 相关的专利（医药）
登录后查看更多信息
4
项与 瑞法舒坦唑 相关的文献（医药）2024-06-01The Lancet. Infectious diseases
Safety, pharmacokinetics, and efficacy of rifasutenizol, a novel dual-targeted antibacterial agent in healthy participants and patients in China with Helicobacter pylori infection: four randomised clinical trials
Article
作者: Liu, Jingrui ; Ma, Zhenkun ; Liu, Yusi ; Wu, Min ; Geng, Guozhu ; Wang, Meng ; Gao, Lei ; Ding, Yanhua ; Wang, Jing ; Li, Xiaojiao ; Lou, Jinfeng ; Chen, Jing ; Zhang, Hong ; Chen, Hong
BACKGROUND:
Due to the rapid development of antimicrobial resistance, the efficacy of most Helicobacter pylori eradication therapies have progressively decreased to an unacceptable level. Rifasutenizol (TNP-2198) is a new molecular entity with a synergistic dual mechanism of action currently under clinical development for the treatment of microaerophilic and anaerobic bacterial infections. We aimed to evaluate the safety, pharmacokinetics, and efficacy of rifasutenizol in healthy Chinese participants and patients with H pylori.
METHODS:
We conducted four clinical trials of rifasutenizol capsules in healthy participants (aged 18-55 years) and patients with asymptomatic H pylori infection (aged 18-65 years) in a clinical trial centre in Jilin province, China. Trial 1 was a phase 1, double-blind, randomised, placebo-controlled, single ascending dose study, in which participants were enrolled into one of seven rifasutenizol dose groups (50 mg, 100 mg, 200 mg, 400 mg, 600 mg, 800 mg, or 1000 mg) and were randomly assigned in a 4:1 ratio to study drug or placebo. Trial 2 was a phase 1, double-blind, randomised, placebo-controlled, multiple ascending dose study, in which patients were enrolled into one of three rifasutenizol dose groups (200 mg, 400 mg, or 600 mg) and were randomly assigned in a 3:1 ratio to study drug or placebo. Trial 3 was a phase 2a, open-label, randomised, multiple-dose, dose-finding study in which patients enrolled into one of four cohorts were randomly assigned in a 1:1:1:1 ratio to a rifasutenizol dual or triple regimen. Trial 4 was a phase 2b, open-label, randomised, multiple-dose, regimen exploration study, in which patients enrolled into one of five cohorts were randomly assigned in a 2:2:1:1:2 ratio to a rifasutenizol dual therapy, triple therapy, or a control cohort. Block randomisation (block size 4 or 8) was used in all four trials. The key primary endpoints for trials 1, 2, and 3 were the tolerability, safety, and pharmacokinetics of rifasutenizol. For trial 4, the primary endpoint was the eradication rate of H pylori. These four trials were registered at ClinicalTrials.gov (NCT06081699, NCT06081712, NCT06076681, and NCT06076694) and chinadrugtrials.org.cn (CTR20190734, CTR20192553, CTR20212050, and CTR20220625) and are completed.
FINDINGS:
Between May 9, 2019, and Sept 14, 2022, 78 healthy participants (trial 1: n=10 per cohort in a 4:1 rifasutenizol:placebo ratio; and an additional eight for the food-effect cohort) and 168 patients with asymptomatic H pylori infection (trial 2: n=16 per cohort in a 3:1 rifasutenizol:placebo ratio; trial 3: n=10 per cohort; trial 4: n=10 or n=20 per cohort) were enrolled in the four clinical trials. Single doses of rifasutenizol (50-1000 mg) and multiple doses of rifasutenizol (200 mg to 600 mg, twice a day), either as monotherapy or co-administered with rabeprazole and amoxicillin, showed favourable safety and tolerability profiles. Most adverse events were mild, and no serious adverse events were reported. Rifasutenizol demonstrated a linear pharmacokinetic profile over the dose range of 50-800 mg, and there were no apparent pharmacokinetic interactions between rifasutenizol and the co-administrated drugs. Food intake slightly elevated the area under the plasma concentration-time curve (AUC) of rifasutenizol, and the geometric mean of AUC from time 0 to the last timepoint with a quantifiable concentration (AUC0-t) and AUC from time 0 to infinity (AUC0-∞) in the fed state were 1·334 and 1·396 times of those in the fasted state, respectively. There was mild accumulation after continuous administration of rifasutenizol, and the Rac(AUC) of rifasutenizol 400 mg in the dual and triple regiments in trial 3 were 1·37 and 1·49, respectively. In trial 3, the eradication rates of H pylori with 200 mg, 400 mg, or 600 mg of rifasutenizol in combination with rabeprazole, twice a day for 14 days, were 0% (95% CI 0-31), 30% (7-65), and 40% (12-74), respectively, identifying rifasutenizol 400 mg as the effective dose. In trial 4, H pylori eradication rates with the triple regimen in cohort A (400 mg rifasutenizol, 20 mg rabeprazole sodium, and 1 g amoxicillin) twice a day for 14 days was 95% (95% CI 74-100), and triple therapy (600 mg rifasutenizol, 20 mg rabeprazole sodium, and 1 g amoxicillin) three times a day for 7 days was 100% (69-100).
INTERPRETATION:
Rifasutenizol monotherapy and combination therapy was generally safe and well tolerated in healthy participants and patients with H pylori infection. A triple regimen of 400 mg rifasutenizol capsules, 20 mg rabeprazole sodium enteric-coated tablets, and 1 g amoxicillin capsules twice a day for 14 days showed promising efficacy as a new treatment regimen for H pylori infection.
FUNDING:
TenNor Therapeutics and National Natural Science Foundation of China.
TRANSLATION:
For the Chinese translation of the abstract see Supplementary Materials section.
2022-05-01CURRENT MEDICINAL CHEMISTRY2区 · 医学
A Comparative Insight on the Newly Emerging Rifamycins: Rifametane, Rifalazil, TNP-2092 and TNP-2198
2区 · 医学
Review
作者: Nazli, Adila ; He, Yun ; Xu, Huacheng ; Wang, Zhi-Peng ; He, David L
Abstract::
Rifamycins are considered a milestone for tuberculosis (TB) treatment because of their proficient sterilizing ability. Currently, available TB treatments are complicated and need a long duration, which ultimately leads to failure of patient compliance. Some new rifamycin derivatives, i.e., rifametane, TNP-2092 (rifamycin-quinolizinonehybrid), and TNP-2198 (rifamycin-nitromidazole hybrid) are under clinical trials, which are attempting to overcome the problems associated with TB treatment. The undertaken review is intended to compare the pharmacokinetics, pharmacodynamics and safety profiles of these rifamycins, including rifalazil, another derivative terminated in phase II trials, and already approved rifamycins. The emerging resistance of microbes is an imperative consideration associated with antibiotics. Resistance development potential of microbial strains against rifamycins and an overview of chemistry, as well as structure-activity relationship (SAR) of rifamycins, are briefly described. Moreover, issues associated with rifamycins are discussed as well. We expect that newly emerging rifamycins shall appear as potential tools for TB treatment in the near future.
2022-03-24Journal of medicinal chemistry1区 · 医学
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens
1区 · 医学
Article
作者: Wang, Huan ; Ma, Zhenkun ; Molodtsov, Vadim ; Ding, Charles ; He, Shijie ; Liu, Yu ; Yuan, Ying ; Weiss, William J. ; Zhuang, Zhijun ; Xu, Xiangyi ; Nguyen, Phung ; Lin, Wei ; Duncan, Leonard ; Pulse, Mark ; Lynch, Anthony Simon ; Robertson, Gregory T. ; Ebright, Richard H. ; Doyle, Timothy ; Chen, Jing
TNP-2198, a stable conjugate of a rifamycin pharmacophore and a nitroimidazole pharmacophore, has been designed, synthesized, and evaluated as a novel dual-targeted antibacterial agent for the treatment of microaerophilic and anaerobic bacterial infections. TNP-2198 exhibits greater activity than a 1:1 molar mixture of the parent drugs and exhibits activity against strains resistant to both rifamycins and nitroimidazoles. A crystal structure of TNP-2198 bound to a Mycobacterium tuberculosis RNA polymerase transcription initiation complex reveals that the rifamycin portion of TNP-2198 binds to the rifamycin binding site on RNAP and the nitroimidazole portion of TNP-2198 interacts directly with the DNA template-strand in the RNAP active-center cleft, forming a hydrogen bond with a base of the DNA template strand. TNP-2198 is currently in Phase 2 clinical development for the treatment of Helicobacter pylori infection, Clostridioides difficile infection, and bacterial vaginosis.
100 项与 瑞法舒坦唑 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 |
|---|---|---|---|---|
| 幽门螺杆菌感染 | 申请上市 | 中国 | 2025-08-22 | |
| 幽门螺杆菌感染 | 申请上市 | 中国 | 2025-08-22 | |
| 厌氧菌感染 | 临床3期 | 中国 | 2023-05-06 | |
| 细菌性阴道炎 | 临床3期 | 中国 | 2023-05-06 | |
| 艰难梭菌腹泻 | 临床3期 | 中国 | 2023-05-06 | |
| 消化系统感染 | 临床3期 | 中国 | 2023-05-06 | |
| 梭菌感染 | 临床1期 | 中国 | 2021-09-16 | |
| 腹泻 | 临床1期 | 中国 | 2021-09-16 | |
| 艰难梭菌感染 | 临床前 | 美国 | 2022-02-17 | |
| 艰难梭菌感染 | 临床前 | 中国 | 2022-02-17 |
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3期 | 700 | Clarithromycin placebo tablets+Rifasutenizol capsules+Amoxicillin Capsules+Rabeprazole sodium enteric-coated tablets (Test Group) | 構築製築願鹽簾顧糧鏇 = 選憲範積齋範衊蓋簾窪 襯願憲鏇艱齋簾願繭鑰 (鏇範襯觸醖顧齋壓壓壓, 簾積醖衊醖鏇襯鏇顧齋 ~ 夢獵網選艱繭鹽齋艱鹽) 更多 | - | 2025-08-17 | ||
Rifasutenizol placebo capsules+Amoxicillin Capsules+Clarithromycin tablets+Rabeprazole sodium enteric-coated tablets+Bismuth potassium citrate capsules (Control Group) | 構築製築願鹽簾顧糧鏇 = 衊積糧窪鬱遞鹹衊獵衊 襯願憲鏇艱齋簾願繭鑰 (鏇範襯觸醖顧齋壓壓壓, 廠獵餘網膚構築膚壓淵 ~ 膚鬱鑰艱觸夢願餘艱觸) 更多 | ||||||
临床3期 | 700 | TNP-2198三联方案 | 觸膚蓋壓積顧鹹簾餘夢(壓夢遞壓遞艱鹹獵壓蓋) = 鬱醖醖顧鹹夢製鬱窪醖 繭顧壓夢範憲糧繭網齋 (鬱築齋範網鏇觸構廠艱 ) 达到 更多 | 积极 | 2024-11-18 | ||
铋剂四联方案 | 觸膚蓋壓積顧鹹簾餘夢(壓夢遞壓遞艱鹹獵壓蓋) = 廠鑰齋鑰膚範願夢選艱 繭顧壓夢範憲糧繭網齋 (鬱築齋範網鏇觸構廠艱 ) 达到 更多 | ||||||
临床1/2期 | - | 鏇顧餘衊遞窪鹽構製醖(遞鏇夢艱願製餘構鏇鏇) = 網餘簾觸齋淵鹹齋膚膚 顧醖築範壓鹽顧範蓋構 (夢蓋蓋鹹襯齋窪製構鏇, 7 ~ 65) | - | 2024-02-01 | |||
鏇顧餘衊遞窪鹽構製醖(遞鏇夢艱願製餘構鏇鏇) = 築構鑰膚鏇遞繭艱範網 顧醖築範壓鹽顧範蓋構 (夢蓋蓋鹹襯齋窪製構鏇, 12 ~ 74) | |||||||
临床2期 | 80 | (Group A) | 網繭築醖繭憲構觸選夢 = 觸觸艱範糧壓繭艱淵鏇 糧淵顧鬱襯遞獵範簾鏇 (鹹鹽蓋憲淵製築蓋鬱繭, 窪鑰選繭繭醖餘築網廠 ~ 繭鹹繭顧積襯餘獵積窪) 更多 | - | 2023-12-12 | ||
(Group B) | 網繭築醖繭憲構觸選夢 = 餘顧蓋鹹遞鹽鏇艱網鬱 糧淵顧鬱襯遞獵範簾鏇 (鹹鹽蓋憲淵製築蓋鬱繭, 網獵襯範襯糧構衊艱憲 ~ 襯壓獵憲糧壓齋築壓衊) 更多 | ||||||
临床1/2期 | 40 | (Group A) | 遞蓋襯窪蓋衊築鏇簾簾 = 製壓鹹製壓積鹽糧網顧 糧蓋積廠網廠鏇餘鏇糧 (鏇艱醖簾選窪餘廠築觸, 顧遞遞鑰壓積鬱鹽獵餘 ~ 鑰鹽積鹽網鹽構範繭獵) 更多 | - | 2023-11-22 | ||
(Group B) | 遞蓋襯窪蓋衊築鏇簾簾 = 廠網選淵壓築衊壓鹽淵 糧蓋積廠網廠鏇餘鏇糧 (鏇艱醖簾選窪餘廠築觸, 餘鑰淵獵製簾齋襯積鏇 ~ 製鬱範獵遞齋鹹憲獵窪) 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
Eureka LS:
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