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更新于：2026-03-12
Rifaquizinone
利福喹酮
更新于：2026-03-12
概要
基本信息
药物类型 小分子化药 |
别名 利法喹嗪酮、CBR-2092、TNP 2092 + [3] |
作用方式 抑制剂 |
作用机制 Bacterial DNA gyrase 抑制剂(细菌DNA旋转酶 抑制剂)、Bacterial top IV抑制剂(细菌拓扑异构酶IV抑制剂)、RNAP抑制剂(细菌DNA指导的RNA聚合酶复合体抑制剂) |
非在研适应症 |
权益机构- |
最高研发阶段临床3期 |
首次获批日期- |
最高研发阶段(中国)临床3期 |
特殊审评优先审评 (美国)、孤儿药 (美国)、合格传染病产品 (美国)、特殊审批 (中国)、快速通道 (美国) |
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结构/序列
分子式C65H81FN6O15 |
InChIKeyOPZFMLLAJBIKAN-UHFFFAOYSA-N |
CAS号922717-97-3 |
关联
9
项与 利福喹酮 相关的临床试验NCT06889701
A Phase 1/2 Study to Evaluate the Safety, PK and Efficacy of TNP-2092 Administered Via IA Injection in Participants With Early or Acute Hematogenous PJI Requiring or Not Requiring DAIR After TKA, or Requiring Long-term Antibiotic Therapy
NCT06394518
A Phase 1, Single-Center, Randomized, Double-Blind, Placebo-Controlled, Dose-Escalation Clinical Trial to Evaluate the Safety, Tolerability, and Pharmacokinetics of Single-Dose and Multiple-Dose Continuous Intravenous Infusions of TNP-2092 for Injection in Healthy Chinese Participants
NCT05074134
An Open Label Phase 1 Study in Healthy Adult Male Subjects to Investigate the Absorption, Metabolism, and Excretion of [14C]-TNP-2092 Following a Single Intravenous Dose Administration
100 项与 利福喹酮 相关的临床结果
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100 项与 利福喹酮 相关的转化医学
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100 项与 利福喹酮 相关的专利（医药）
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10
项与 利福喹酮 相关的文献（医药）2026-02-01EXPERT OPINION ON INVESTIGATIONAL DRUGS
A randomized, double-blind, placebo-controlled study to evaluate the safety, pharmacokinetics and ammonia-lowering effect of Rifaquizinone, an intestinally restricted investigational drug
Article
作者: Liu, Jingrui ; Ma, Zhenkun ; Lu, Mengdi ; Geng, Guozhu ; Niu, Junqi ; Ai, Changlin ; Ding, Yanhua ; Li, Xiaojiao ; Shi, Chunhua ; Xu, Jia ; Zhang, Hong ; Chen, Jing ; Hu, Yue
BACKGROUND:
Rifaquizinone (RQZ, TNP-2092) is a novel drug for treating hepatic encephalopathy (HE). This study assessed the safety, pharmacokinetics (PK), and efficacy of RQZ capsules in healthy participants and cirrhosis patients with hyperammonemia.
RESEARCH DESIGN AND METHODS:
We conducted three double-blind, randomized, placebo-controlled trials. Trials 1 and 2 enrolled healthy participants, while Trial 3 involved 36 cirrhosis patients with hyperammonemia.
RESULTS:
In healthy participants and liver cirrhosis patients with hyperammonemia, RQZ was safe and well tolerated. Adverse events were generally mild or moderate. Both food and liver cirrhosis disease status increased the exposure of RQZ, which was around 1% of that of the corresponding doses after intravenous administration. The effect in lowering blood ammonia was dose-dependent. The changes from baseline in blood ammonia levels at day 15 were -14.1 and 0.5 μmol/L in 600 mg and placebo cohort. The percentage of achieving normal blood ammonia during treatment were 31.9% and 7.4% in 600 mg and placebo cohort.
CONCLUSIONS:
Although this study enrolled a relatively small cohort of cirrhotic patients with hyperammonemia, RQZ demonstrated an excellent safety profile as an intestinally restricted agent and showed promising potential for lowering blood ammonia and treating hepatic encephalopathy.
2024-06-14The Journal of infectious diseases
The Efficacy and Safety of an Intra-articular Dual-Acting Antibacterial Agent (TNP-2092) for Implant Infection–Associated Methicillin-Resistant Staphylococcus aureus
Article
作者: Dai, Tianyu ; Wang, Huan ; Zhang, Fan ; Chen, Liaobin ; Wen, Yinxian ; Ma, Chi ; Wang, Hui ; Ma, Zhenkun
Abstract:
Owing to the presence of microbial biofilm on the implant, the eradication of biofilm-associated infections poses a challenge for antibiotic therapies. The study aimed to investigate the efficacy and safety of the novel antibiotic agent TNP-2092 in the context of implant infections. In vivo, rats with periprosthetic joint infection (PJI) treated with antibiotics showed an increase in body weight and decrease in swelling, temperature, and width of knee, compared with the control group. Meanwhile, inflammatory markers in synovium and serum were decreased in the TNP-2092 group, consistent with the pathological results. Moreover, TNP-2092 was effective in eliminating bacteria and disruption biofilm formation, and further alleviated the abnormal bone absorption and reactive bone changes around the prosthesis. In conclusion, intra-articular injection of TNP-2092 is safe and effective in treating knee PJI in a rat model. The study provides a foundation for the future utilization of TNP-2092 in the management of implant-related infections.
2020-07-01Diagnostic microbiology and infectious disease4区 · 医学
In vitro activity of TNP-2092 against periprosthetic joint infection–associated staphylococci
4区 · 医学
Article
作者: Schmidt-Malan, Suzannah M ; Ma, Zhenkun ; Patel, Robin ; Yuan, Ying ; He, Shijie ; Fisher, Cody R
Staphylococci are the most common causes of periprosthetic joint infection (PJI). TNP-2092 is an investigational hybrid drug composed of rifamycin and quinolizinone pharmacophores conjugated via a covalent linker. We determined minimum inhibitory concentration (MIC), minimum bactericidal concentration (MBC), and minimum biofilm bactericidal concentration (MBBC) values of TNP-2092 against 80 PJI-associated Staphylococcus aureus and Staphylococcus epidermidis isolates compared to ciprofloxacin and rifampin alone and in combination, alongside daptomycin and vancomycin. TNP-2092 exhibited the following activity against S. aureus: MIC50/MIC90, ≤0.0075/0.015 μg/mL; MBC50/MBC90, 0.5/4 μg/mL; and MBBC50/MBBC90, 0.5/2 μg/mL, and the following activity against S. epidermidis: MIC50/MIC90, ≤0.0075/0.015 μg/mL; MBC50/MBC90, 0.015/0.125 μg/mL; and MBBC50/MBBC90, 0.06/0.25 μg/mL. TNP-2092 MIC, MBC, and MBBC values were >8 μg/mL for 1 isolate, while MIC values were ≤0.25 μg/mL and MBC and MBBC values were ≤4 μg/mL for all other isolates. Results of this study show that TNP-2092 has promising in vitro activity against PJI-associated staphylococci.
100 项与 利福喹酮 相关的药物交易
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外链
| KEGG | Wiki | ATC | Drug Bank |
|---|---|---|---|
| - | - | - |
研发状态
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 |
|---|---|---|---|---|
| 皮肤和皮肤结构感染 | 临床3期 | 中国 | 2022-02-26 | |
| 幼年性息肉 | 临床2期 | 中国 | 2025-04-03 | |
| 假体关节感染 | 临床2期 | 中国 | 2025-04-01 | |
| 假体关节感染 | 临床2期 | 中国 | 2025-04-01 | |
| 腹泻型肠易激综合征 | 临床2期 | 中国 | 2021-09-09 | |
| 高氨血症 | 临床2期 | 中国 | 2020-08-27 | |
| 肝硬化 | 临床2期 | 中国 | 2020-08-27 | |
| 丹毒 | 临床2期 | 美国 | 2019-04-20 | |
| 肝性脑病 | 临床2期 | 中国 | - | |
| 幽门螺杆菌感染 | 临床1期 | 中国 | 2016-11-02 |
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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1期 | 58 | (TNP-2092 Capsules 100mg (Fasting)) | 廠衊製餘遞壓鏇遞鏇餘 = 鹹艱範製餘簾網選鬱醖 繭膚構鑰構衊鹽構窪積 (獵積鹽範窪鑰鑰觸觸窪, 網鹽膚齋積憲網獵網製 ~ 壓觸鹽蓋鹽夢鹽窪繭醖) 更多 | - | 2025-04-25 | ||
(TNP-2092 Capsules 200mg (Fasting)) | 廠衊製餘遞壓鏇遞鏇餘 = 蓋窪網範齋糧選鏇鏇襯 繭膚構鑰構衊鹽構窪積 (獵積鹽範窪鑰鑰觸觸窪, 鹽鬱築鏇襯獵願範鹽糧 ~ 艱襯鹽鹹膚膚廠壓廠艱) 更多 | ||||||
临床1期 | 40 | (TNP-2092 Capsules 100 mg) | 築糧夢餘夢網鹽鹹窪簾 = 繭廠壓醖鹽鬱鑰鑰選選 願廠廠廠膚淵淵願鏇齋 (鬱艱廠觸構網鬱簾淵壓, 繭網壓鏇艱衊膚夢選壓 ~ 願鏇鹽齋範淵醖獵鏇襯) 更多 | - | 2025-01-29 | ||
(TNP-2092 Capsules 300 mg) | 築糧夢餘夢網鹽鹹窪簾 = 廠構範製遞窪艱窪膚積 願廠廠廠膚淵淵願鏇齋 (鬱艱廠觸構網鬱簾淵壓, 膚壓願艱醖築製構範蓋 ~ 觸餘窪廠選鏇憲衊製構) 更多 | ||||||
临床1/2期 | 36 | (TNP-2092 Capsules 100mg Twice Daily(BID)) | 鹽顧憲網構壓繭襯夢夢 = 鏇膚憲築窪醖廠鬱醖齋 膚廠齋壓範構築鹹獵簾 (簾醖夢選憲蓋鏇範獵遞, 簾淵積網糧衊壓窪鏇憲 ~ 願範鹹願鑰襯獵積網蓋) 更多 | - | 2024-05-10 | ||
(TNP-2092 Capsules 300mg BID) | 鹽顧憲網構壓繭襯夢夢 = 獵範齋夢遞蓋鹽鹽廠糧 膚廠齋壓範構築鹹獵簾 (簾醖夢選憲蓋鏇範獵遞, 鑰餘餘構簾鏇範顧鏇窪 ~ 餘鑰廠壓簾蓋顧鏇顧餘) 更多 | ||||||
临床2期 | 120 | (TNP-2092) | 夢膚齋淵餘憲獵範齋鬱 = 顧鬱觸壓顧簾鑰膚憲艱 窪繭選構網壓繭獵齋膚 (憲齋積壓鹽鹹網繭遞範, 鏇夢夢糧淵範蓋鏇壓廠 ~ 獵壓獵積衊鹽製糧遞範) 更多 | - | 2023-12-01 | ||
(Vancomycin) | 夢膚齋淵餘憲獵範齋鬱 = 顧鹽構齋夢築衊顧獵壓 窪繭選構網壓繭獵齋膚 (憲齋積壓鹽鹹網繭遞範, 遞願網鬱鬱鏇淵膚餘繭 ~ 製願構繭範範齋廠糧築) 更多 | ||||||
临床2期 | - | 鬱獵鹽繭願齋鏇艱鏇壓(繭築遞鏇獵壓鬱簾鬱齋) = 鹽淵顧鹽鏇遞築鏇築積 餘顧窪壓糧餘淵構齋淵 (鑰願醖願繭鑰艱衊蓋鬱 ) 更多 | 积极 | 2019-11-11 | |||
鬱獵鹽繭願齋鏇艱鏇壓(繭築遞鏇獵壓鬱簾鬱齋) = 網觸壓壓鑰蓋願衊築鹹 餘顧窪壓糧餘淵構齋淵 (鑰願醖願繭鑰艱衊蓋鬱 ) 更多 |
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