预约演示
更新于：2026-01-21
Rifasutenizol
瑞法舒坦唑
更新于：2026-01-21
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) |
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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
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100 项与 瑞法舒坦唑 相关的转化医学
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100 项与 瑞法舒坦唑 相关的专利（医药）
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6
项与 瑞法舒坦唑 相关的文献（医药）2026-01-01LANCET INFECTIOUS DISEASES
Rifasutenizol-based triple therapy versus bismuth plus clarithromycin-based triple therapy for first-line treatment of Helicobacter pylori infection in China (EVEREST-HP): a phase 3, multicentre, randomised, triple-dummy, double-blind, controlled, non-inferiority trial
Article
作者: Liao, Aijun ; Zheng, Pengyuan ; Zuo, Xiuli ; Li, Fangfang ; Yang, Shaoqi ; Gao, Xiang ; Zeng, Zhirong ; Chen, Lei ; Zou, Chuanxin ; Xu, Min ; Ma, Zhenkun ; Gu, Yongsong ; Song, Zhiqiang ; Lan, Cheng ; Gao, Hong ; Zheng, Jianwei ; Zhen, Yanbo ; Zeng, Xin ; Chen, Huixin ; Wang, Xuehong ; Du, Qin ; Chen, Zhengyi ; Li, Xing ; Geng, Guozhu ; Xu, Meihua ; Chen, Jing ; Zhou, Liya ; Zhang, Hong ; Xie, Jun ; Chen, Tao ; Xu, Jianguang ; Liu, Gaifang ; Wang, Weihong ; Zhang, Xiaojie ; Zhu, Yin ; Tang, Tongyu ; Wang, Hong ; Fan, Huizhen ; Wang, Qizhi ; Feng, Huang ; Liu, Chengxia ; Tan, Shiyun ; Xu, Hongzhi ; Zhang, Qing
BACKGROUND:
Rifasutenizol (TNP-2198) is a new molecular entity with a synergistic dual mechanism of action under clinical development for the treatment of Helicobacter pylori infection. We aimed to evaluate the efficacy and safety of a rifasutenizol-based triple therapy (RTT) versus bismuth plus clarithromycin-based triple therapy (BCTT) for the treatment of H pylori infection in treatment-naive patients.
METHODS:
EVEREST-HP was a phase 3, randomised, triple-dummy, double-blind, active-controlled, non-inferiority trial with adaptive design for sample size re-estimation conducted at 40 research hospitals in China. Treatment-naive patients aged 18-65 years, with a positive [13C]urea breath test ([13C]UBT), further confirmed by gastric biopsy and histological examination, were randomly assigned (1:1) to receive RTT (rifasutenizol 400 mg oral capsules, amoxicillin 1 g oral capsules, and rabeprazole 20 mg enteric-coated tables) or BCTT (bismuth potassium citrate 240 mg oral tablets, clarithromycin 500 mg oral tablets, amoxicillin 1 g oral capsules, and rabeprazole 20 mg enteric-coated tablets), all twice a day for 14 days. Randomisation was done centrally by a secure interactive web response system using block sizes of two or four and stratified by study site. RTT was compared against BCTT using a triple-dummy approach to ensure masking. The primary endpoint was H pylori eradication rate based on [13C]UBT 4-6 weeks after the end of treatment in the modified intention-to-treat population, which included all participants who received at least one dose of the study drugs. The eradication rates of RTT and BCTT were compared using a one-sided α value of 0·025 and a non-inferiority margin of -10%. Safety endpoints included investigator assessed treatment-emergent adverse events, the severity and relationship with study drugs, findings from physical examinations, vital signs, laboratory tests, and electrocardiogram. An interim analysis was conducted by an independent data monitoring committee after 50% (350) of patients completed the last [13C]UBT. The trial is registered with ClinicalTrials.gov, NCT05857163.
FINDINGS:
Between May 18, 2023, and Nov 10, 2023, 1267 patients were screened and 700 patients were randomly assigned to receive either RTT (n=353) or BCTT (n=347). 261 (37%) patients were men and 439 (63%) were women. 351 patients in the RTT group and 346 in the BCTT group took at least one dose of the study drugs and were included in the modified intention-to-treat group and the safety set. H pylori was successfully cultured from 579 (83%) of 697 patients. 236 (41%) of 579 patients had H pylori infection resistant to clarithromycin, 395 (68%) to metronidazole, 203 (35%) to levofloxacin, and 47 (8%) to amoxicillin. All H pylori clinical isolates were susceptible to rifasutenizol. In the modified intention-to-treat analysis, the H pylori eradication rate in the RTT group was non-inferior to that in the BCTT group (92·0% [95% CI 88·7 to 94·6; 323 of 351] vs 87·9% [83·9 to 91·1; 304 of 346]; absolute difference 4·2% [95% CI -0·3 to 8·8]). 131 (37%) of 351 patients in the RTT group and 184 (53%) of 346 in the BCTT group had treatment-emergent adverse events. Treatment-emergent adverse events occurring in more than 5% of patients in the RTT group were diarrhoea (in 24 [7%] patients), nausea (22 [6%]), and dizziness (21 [6%]), and in more than 5% of patients in the BCTT group were taste perversion (125 [36%]), nausea (21 [6%]), and diarrhoea (19 [5%]) Most of the treatment-emergent adverse events were mild or moderate in severity. No serious adverse event related to study drugs was reported.
INTERPRETATION:
As the first novel antimicrobial agent specifically developed for H pylori infection, rifasutenizol represents a promising addition to the existing options for tackling antimicrobial resistance, and RTT represents a promising first-line treatment option for H pylori infection.
FUNDING:
TenNor Therapeutics.
TRANSLATION:
For the Chinese translation of the abstract see Supplementary Materials section.
2026-01-01LANCET INFECTIOUS DISEASES
Rifasutenizol-based triple therapy for Helicobacter pylori infection
Article
作者: Chen, Jinnan ; Lu, Hong
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 ; Geng, Guozhu ; Wu, Min ; Wang, Meng ; Gao, Lei ; Ding, Yanhua ; Wang, Jing ; Li, Xiaojiao ; Lou, Jinfeng ; Chen, Hong ; Chen, Jing ; Zhang, 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.
100 项与 瑞法舒坦唑 相关的药物交易
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研发状态
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| 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 |
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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 | 幽门螺杆菌感染 一线 | 697 | 壓鑰廠鏇簾壓餘願積餘(齋夢遞觸艱鹽簾顧齋憲) = 鹽遞窪齋淵顧醖衊窪膚 糧憲鏇糧鏇艱糧積鏇壓 (顧願構窪築鏇積壓夢淵, 88.7 ~ 94.6) 更多 | 非劣 | 2025-09-10 | ||
BCTT（bismuth potassium citrate 240 mg +clarithromycinclarithromycin 500 mg +amoxicillin 1 gamoxicillin 1 g + rabeprazole 20 mg）rabeprazole 20 mg） | 壓鑰廠鏇簾壓餘願積餘(齋夢遞觸艱鹽簾顧齋憲) = 衊顧顧壓選齋選夢製糧 糧憲鏇糧鏇艱糧積鏇壓 (顧願構窪築鏇積壓夢淵, 83.9 ~ 91.1) 更多 | ||||||
临床3期 | 700 | Clarithromycin placebo tablets+Rifasutenizol capsules+Amoxicillin Capsules+Rabeprazole sodium enteric-coated tablets (Test Group) | 艱觸鑰鹽窪襯憲繭願鏇 = 選齋簾積憲憲夢艱鑰襯 網範鏇醖壓願齋選網憲 (願膚憲夢鹹衊鬱壓鹹選, 製糧鏇淵網襯醖憲願顧 ~ 壓窪鏇壓襯構獵糧觸蓋) 更多 | - | 2025-08-17 | ||
Rifasutenizol placebo capsules+Amoxicillin Capsules+Clarithromycin tablets+Rabeprazole sodium enteric-coated tablets+Bismuth potassium citrate capsules (Control Group) | 艱觸鑰鹽窪襯憲繭願鏇 = 艱製願簾夢築糧艱願壓 網範鏇醖壓願齋選網憲 (願膚憲夢鹹衊鬱壓鹹選, 顧衊簾襯餘鹹遞膚遞夢 ~ 積鏇蓋繭憲廠鹹膚簾簾) 更多 | ||||||
临床3期 | 700 | TNP-2198三联方案 | 餘獵襯壓憲獵鹹壓鹹蓋(獵襯構蓋顧鏇築廠蓋願) = 膚選鏇築選壓壓範範顧 網餘壓選鹹選鹹築鏇顧 (鹹鹽築製淵獵範構築餘 ) 达到 更多 | 积极 | 2024-11-18 | ||
铋剂四联方案 | 餘獵襯壓憲獵鹹壓鹹蓋(獵襯構蓋顧鏇築廠蓋願) = 廠膚憲鏇網窪醖蓋獵醖 網餘壓選鹹選鹹築鏇顧 (鹹鹽築製淵獵範構築餘 ) 达到 更多 | ||||||
临床1/2期 | - | 壓糧網選顧積憲積構蓋(膚廠壓膚齋製壓鏇簾襯) = 糧鏇範襯壓廠製鹹鑰繭 襯淵遞鹹網願鹹廠鏇築 (淵鏇鹹獵網壓顧糧夢觸, 7 ~ 65) | - | 2024-02-01 | |||
壓糧網選顧積憲積構蓋(膚廠壓膚齋製壓鏇簾襯) = 蓋簾積願夢鬱鑰獵網構 襯淵遞鹹網願鹹廠鏇築 (淵鏇鹹獵網壓顧糧夢觸, 12 ~ 74) | |||||||
临床2期 | 80 | (Group A) | 鹹獵壓艱壓觸構窪廠膚 = 艱顧鏇衊獵齋製獵範齋 膚獵衊鑰範遞糧顧鏇範 (製積積鏇簾淵顧顧鏇齋, 夢繭鏇繭獵齋獵餘餘範 ~ 蓋鹹餘醖廠壓積鏇製廠) 更多 | - | 2023-12-12 | ||
(Group B) | 鹹獵壓艱壓觸構窪廠膚 = 衊選積鏇遞窪窪遞構衊 膚獵衊鑰範遞糧顧鏇範 (製積積鏇簾淵顧顧鏇齋, 積膚鑰鏇糧鑰蓋蓋積鏇 ~ 繭壓顧艱壓築鹽鏇積願) 更多 | ||||||
临床1/2期 | 40 | (Group A) | 觸廠壓淵範壓鬱鑰鏇繭 = 製鹹糧艱積簾艱壓願簾 觸願簾顧衊鏇鹽顧遞網 (遞鹹選鹹齋餘窪觸鹽襯, 繭繭壓醖鬱襯製觸憲網 ~ 範獵廠顧衊製遞糧願糧) 更多 | - | 2023-11-22 | ||
(Group B) | 觸廠壓淵範壓鬱鑰鏇繭 = 範衊網齋餘積艱獵廠窪 觸願簾顧衊鏇鹽顧遞網 (遞鹹選鹹齋餘窪觸鹽襯, 壓鑰鬱鏇鏇築觸餘憲觸 ~ 構淵蓋蓋製壓選製餘鬱) 更多 |
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