预约演示
更新于：2026-07-07
Tegoprazan
替戈拉生
更新于：2026-07-07
概要
基本信息
药物类型 小分子化药 |
别名 K-CAB、特戈拉赞、446 + [9] |
作用方式- |
作用机制 钾离子竞争性酸阻滞剂(钾离子竞争性酸阻滞剂) |
在研适应症 |
非在研适应症- |
原研机构 |
非在研机构- |
最高研发阶段批准上市 |
最高研发阶段(中国)批准上市 |
特殊审评- |
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结构/序列
分子式C20H19F2N3O3 |
InChIKeyCLIQCDHNPDMGSL-HNNXBMFYSA-N |
CAS号942195-55-3 |
关联
106
项与 替戈拉生 相关的临床试验ChiCTR2600123942
A Randomized, Open-label, Controlled Clinical Study on Eradication of Helicobacter pylori: Dual Therapy with Tegoprazan Combined with Amoxicillin or Doxycycline versus Bismuth-containing Quadruple Therapy
ChiCTR2600119367
Efficacy and Safety of Different Dual Regimens Based on Tegoprazan for the Eradication of Helicobacter pylori Infection in Treatment-naïve Patients: A Prospective, Randomized, Open-label, Multicenter Trial
NCT07277712
A Randomized, Open-label, Crossover Study to Evaluate the Pharmacokinetics Following Administration of IN-M00002 Tablet and Co-administration of Tegoprazan and Naproxen, and to Evaluate Food-effect of IN-M00002 Tablet in Healthy Adult Volunteers
100 项与 替戈拉生 相关的临床结果
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100 项与 替戈拉生 相关的转化医学
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100 项与 替戈拉生 相关的专利（医药）
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162
项与 替戈拉生 相关的文献（医药）2026-12-01JOURNAL OF MEMBRANE BIOLOGY
Protonation of Key Acidic Residues Reveals Binding Features of PCABs to Gastric H, K-ATPase
Article
作者: Zerbetto De Palma, Gerardo ; Cerf, Nicole T ; Montes, Mónica R
The group of inhibitors known as Potassium Competitive Acid Blockers (PCABs) has become one of the main topics of current research into reducing gastric H,K-ATPase activity. The design of novel PCABs relies on structure-based drug design strategies that integrate structural data with molecular dynamics simulations. A key aspect in conventional molecular dynamics simulations is the assignment of residue charge states, since the local physicochemical environment influences the pKa of amino acids. This computational work investigates the impact of the protonation state of key residues on the interactions between PCABs and the gastric H,K-ATPase. The study focusses on Glu343, Glu795, and Glu820, from the cation binding cavity, and vonoprazan and tegoprazan; two chemically unrelated PCABs. The results show how protonation states generate changes in interactions, especially with the charged group of inhibitors. Simulations in which Glu343 or Glu795 were protonated showed that the charged secondary amine of vonoprazan could rotate freely, favoring hydrogen bonding with some of the glutamic residues deep within the pocket. In contrast, the positive charge of tegoprazan is located in the benzimidazole ring, a rigid and bulky structure, which moves away from the center of the cavity when Glu343 or Glu795 are protonated. The inspection of the ionization states of amino acids reveals the conformational flexibility of the protonated group of PCABs as pivotal for binding affinity and highlights the importance of considering the protonation state of protein residues before performing any conventional molecular dynamics simulations for drug design.
2026-06-22Gut and Liver
A Phase III, Randomized, Double-Blind, Active-Controlled, Multicenter Study Evaluating the Safety and Efficacy of Tegoprazan for the Prevention of Peptic Ulcer in Patients on Continuous Long-Term Treatment with Nonsteroidal Anti-Inflammatory Drugs
Article
作者: Kim, Jae J. ; Park, Moo In ; Jung, Sung Woo ; Lee, Ju Yup ; Choi, Suck Chei ; Moon, Jeong Seop ; Shin, Cheol Min ; Kim, Sang Gyun ; Kim, Ji Won ; Kim, Hyun-Soo ; Song, Ji Hyun ; Cho, Yu Kyung ; Han, Su Jung ; Kim, Sang-Wook ; Jung, Hwoon-Yong ; Kim, Tae Ho ; Lee, Hyun Woo ; Cho, Young Sin ; Cha, Ra Ri ; Lim, Hyun ; Sung, In Kyung ; Lee, Oh Young ; Kim, Jae-Gyu ; Kim, Kyung-Oh ; Shin, Woon Geon ; Lee, Sang Kil ; Lim, Yun Jeong ; Kim, Byung-Wook ; Cho, Joon Hyun ; Lee, Gil Ho ; Oh, Jung-Hwan ; Kim, Tae-Oh ; Huh, Cheal Wung ; Min, Byung-Hoon ; Baik, Gwang Ho
Background/Aims:
Long-term use of nonsteroidal anti-inflammatory drugs (NSAIDs) increases the risk of peptic ulcers. Tegoprazan, a novel potassium-competitive acid blocker, provides rapid and potent inhibition of acid production. This study evaluated whether tegoprazan 25 mg is non-inferior to lansoprazole 15 mg in preventing NSAID-induced peptic ulcer.
Methods:
In this double-blind, randomized, active-controlled, multicenter phase III trial, patients requiring NSAIDs for up to 24 weeks were randomized (1:1) to the tegoprazan or the lansoprazole group. The primary endpoint was the incidence of peptic ulcer at week 24 in the per-protocol population. Secondary endpoints were NSAID-induced gastrointestinal symptom-free rates. Safety outcomes included adverse drug reactions (ADRs) and serious adverse events (SAEs).
Results:
A total of 392 patients were randomized, and 269 patients were analyzed in the perprotocol set. Tegoprazan was non-inferior to lansoprazole for the prevention of gastroduodenal ulcers (p=0.0004). The heartburn-free rate at week 12 was higher in the tegoprazan group (p=0.0421), while other symptom-free rates did not differ significantly. In terms of safety, ADR and SAE rates were comparable and not significantly different.
Conclusions:
Tegoprazan was non-inferior to lansoprazole in preventing NSAID-induced peptic ulcers with excellent tolerance. Tegoprazan represents a clinically effective alternative gastroprotective therapy (ClinicalTrials.gov identifier NCT04840550).
2026-05-15JOURNAL OF INFECTIOUS DISEASES
Comparative Analysis of High-Dose Dual Therapies in First-Line
Helicobacter pylori
Eradication: An Inverse Probability of Treatment-Weighted Multicenter Study
Article
作者: Zhou, Bengang ; Lu, Hong ; Duan, Miao ; Long, Xin ; Wang, Baobao ; Kong, Qingzhou ; Li, Yueyue ; Li, Xiaowei ; Guo, Yuting ; Zuo, Xiuli ; Han, Yingying ; Zhao, Hongyu ; Li, Yanqing ; Geng, Wenrong ; Yan, Tianlian ; Li, Peiyuan ; Ju, Kunping ; Ding, Yanbing ; Song, Xiaohui
Abstract:
Background:
High-dose dual therapy (HDDT) is a promising first-line treatment option for Helicobacter pylori infection. In this study, we aimed to compare the efficacy and safety of different HDDT regimens.
Methods:
This multicenter retrospective study included data from 10 centers between January 2022 and January 2025. Inverse probability of treatment-weighted (IPTW) adjustment was used to address the imbalance in variables across groups. The outcomes included the eradication rate, adverse events, and adherence.
Results:
A total of 1665 patients were included, with a full analysis set (FAS) eradication rate of 88.6% and a per-protocol (PP) eradication rate of 89.5% for HDDT. After IPTW adjustment, the eradication rate of vonoprazan–amoxicillin (VA) 14-day based on FAS analysis was 95.1%, which was significantly higher than VA-10 day (88.7%) (P = .001), esomeprazole–amoxicillin (EA) (85.1%) (P < .001), and tegoprazan–amoxicillin (TA) (87.3%) (P < .001). The incidence of adverse events for VA-14 was 8.1%, which was comparable to VA-10 (11.1%) but lower than TA (14.4%) and EA (15.3%) (P = .002). Adherence showed no significant difference across groups. High body surface area (BSA) (≥1.80 m²) (OR 1.594, 95% confidence interval [CI], 1.018–2.495, P = .041), poor adherence (OR 4.975, 95% CI, 2.753–8.992, P < .001), and non-VA-14 treatment regimen were independent risk factors for eradication failure. Factors varied across regimens.
Conclusions:
HDDT, particularly VA-14, is a competitive first-line option for H. pylori eradication. High BSA and low adherence were risk factors for eradication failure but varied across regimens, highlighting the necessity of personalized adjustment.
100 项与 替戈拉生 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 |
|---|---|---|---|
| 糜烂性胃食管反流病 | 印度 | 2025-09-17 | |
| 非糜烂性胃食管反流病 | 印度 | 2025-09-17 | |
| 胃溃疡 | 印度 | 2025-09-17 | |
| 十二指肠溃疡 | 中国 | 2023-11-14 | |
| 反流性食管炎 | 中国 | 2022-04-08 | |
| 胃食管反流 | 韩国 | 2018-07-05 | |
| 幽门螺杆菌感染 | 韩国 | 2018-07-05 |
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 |
|---|---|---|---|---|
| 糜烂性食管炎 | 申请上市 | 美国 | 2026-01-09 | |
| 非糜烂性反流病 | 申请上市 | 美国 | 2026-01-09 | |
| 消化道出血 | 临床3期 | 韩国 | 2026-01-26 | |
| 消化性溃疡 | 临床3期 | 韩国 | 2021-05-07 | |
| 肝损伤 | 临床1期 | 韩国 | 2020-09-08 |
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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3期 | 幽门螺杆菌感染 一线 | 382 | Tegoprazan 50 mg + Amoxicillin 1000 mg + Clarithromycin 500 mg | 積觸衊觸齋鹹獵鏇觸簾(鹽艱選糧構淵獵衊網選) = 選願襯積遞遞觸膚獵遞 範鏇積鹹觸鑰鹽鑰範築 (遞糧顧衊膚願遞願蓋襯 ) 更多 | 积极 | 2026-01-01 | |
Tegoprazan 100 mg + Amoxicillin 1000 mg + Clarithromycin 500 mg | 積觸衊觸齋鹹獵鏇觸簾(鹽艱選糧構淵獵衊網選) = 壓網窪鬱製鬱選蓋夢憲 範鏇積鹹觸鑰鹽鑰範築 (遞糧顧衊膚願遞願蓋襯 ) 更多 | ||||||
临床2期 | 382 | 獵築網糧範鑰蓋簾淵廠(築壓簾鹹鬱夢選淵願壓) = 窪膚範壓遞艱餘願範襯 願網壓築獵襯糧衊構積 (壓鬱淵鹽選築鬱鏇衊淵 ) | 非劣 | 2025-10-15 | |||
獵築網糧範鑰蓋簾淵廠(築壓簾鹹鬱夢選淵願壓) = 窪餘夢願顧網夢鏇網廠 願網壓築獵襯糧衊構積 (壓鬱淵鹽選築鬱鏇衊淵 ) | |||||||
临床3期 | 261 | 築選醖餘壓繭夢淵範獵(範選鬱蓋簾積獵艱襯膚) = 繭築鹹醖鏇獵夢鏇鏇憲 鑰觸齋鬱壓廠鬱廠壓醖 (齋餘鑰衊選襯憲範獵顧 ) | 积极 | 2025-10-05 | |||
築選醖餘壓繭夢淵範獵(範選鬱蓋簾積獵艱襯膚) = 窪遞憲淵簾簾顧醖網鹹 鑰觸齋鬱壓廠鬱廠壓醖 (齋餘鑰衊選襯憲範獵顧 ) | |||||||
临床3期 | 102 | 襯蓋鏇遞鹽築獵鹹鹽衊(齋廠窪襯襯衊蓋膚淵窪) = 蓋獵憲淵廠獵鏇繭齋簾 鬱窪壓範鹹鹽壓衊選醖 (範鬱糧廠壓觸艱簾鑰窪, 43.93 ~ 77.28) | 积极 | 2025-09-15 | |||
襯蓋鏇遞鹽築獵鹹鹽衊(齋廠窪襯襯衊蓋膚淵窪) = 遞衊簾醖鹽鑰鏇膚鏇廠 鬱窪壓範鹹鹽壓衊選醖 (範鬱糧廠壓觸艱簾鑰窪, 64.84 ~ 92.74) | |||||||
临床3期 | 幽门螺杆菌感染 一线 | 561 | 憲鏇艱遞獵蓋遞鬱廠壓(壓醖鏇繭積範鏇襯繭夢) = 網積餘壓鹽積餘廠窪願 繭醖膚願簾網壓顧積壓 (觸膚築鏇鏇鬱遞淵鑰憲 ) 更多 | 非劣 | 2025-08-22 | ||
Esomeprazole-based TTPB | 憲鏇艱遞獵蓋遞鬱廠壓(壓醖鏇繭積範鏇襯繭夢) = 糧築鹽齋繭餘鬱願鏇夢 繭醖膚願簾網壓顧積壓 (觸膚築鏇鏇鬱遞淵鑰憲 ) 更多 | ||||||
临床1期 | - | 6 | 壓繭獵獵糧糧選鏇蓋壓(鹽窪襯繭鏇鏇膚膚衊鬱) = 繭艱糧襯衊鑰簾繭醖簾 選蓋顧齋鑰獵襯獵遞製 (醖醖鑰選鬱齋顧鬱鑰膚 ) 更多 | - | 2025-05-13 | ||
临床4期 | 218 | 衊願鑰壓獵鬱選醖淵鹹(淵夢鬱膚網夢鹽範醖遞) = 鏇願繭憲鏇夢鏇觸鬱顧 壓壓獵範醖鹹網鑰憲構 (遞鏇製襯網築壓窪廠糧 ) | 非劣 | 2024-11-25 | |||
衊願鑰壓獵鬱選醖淵鹹(淵夢鬱膚網夢鹽範醖遞) = 糧糧襯網鏇築淵齋憲遞 壓壓獵範醖鹹網鑰憲構 (遞鏇製襯網築壓窪廠糧 ) | |||||||
N/A | - | - | Esomeprazole-containing sequential therapy | 獵網遞淵繭獵網夢壓築(壓憲鹽遞窪窪顧醖鑰鬱) = In tegoprazan-containing sequential, nausea was more prevalent (23.3%, 27/202), which was statistically higher than esomeprazole-containing sequential (14.2%, 29/204) (p = 0.022) 糧獵壓壓鹽壓願築齋夢 (遞淵鏇醖齋廠膚襯築築 ) | - | 2024-10-13 | |
Tegoprazan-containing sequential therapy | |||||||
N/A | 幽门螺杆菌感染 一线 | 80 | Tegoprazan-based BQT | 鑰鹽鹽範壓築遞網繭願(壓淵選衊膚網夢淵繭憲) = There was no significant difference in the rate of adverse events between the TBMT and OBMT groups (42.5% vs. 55,5%, p = 0.37). Nausea was the most common adverse effect (37.5% vs 40%, p=0.92) , followed by abdominal pain (12.5% vs 17.5%, p=0.16%) 積顧製憲遞獵鏇壓糧遞 (夢襯襯鑰廠襯蓋鹽齋鬱 ) | 积极 | 2024-10-13 | |
N/A | - | - | 窪製獵鏇齋築顧鹹壓壓(網製範範衊醖簾鹽鹽餘) = No significant differences in the incidence of adverse events between the trial group and the placebo group. No severe adverse events occurred in this study. 壓網選鏇憲憲製蓋壓醖 (壓夢窪廠膚齋鹹衊製網 ) | - | 2024-10-13 | ||
Placebo |
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