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更新于：2026-03-11
Linaprazan glurate
戊二酸利那拉生酯
更新于：2026-03-11
概要
基本信息
非在研机构 |
最高研发阶段批准上市 |
首次获批日期 中国 (2024-12-01), |
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C26H32N4O5 |
InChIKeyGPHPBXRKAJSSIC-UHFFFAOYSA-N |
CAS号1228559-81-6 |
关联
16
项与 戊二酸利那拉生酯 相关的临床试验NCT07313774
A Randomized, Phase 3, Double-blind, Double-dummy, Active Comparator-controlled Multicenter Clinical Trial to Evaluate the Efficacy and Safety of Linaprazan Glurate Compared to Lansoprazole in Maintenance of Healing in Participants With Healed Erosive Esophagitis (EE) Due to Gastroesophageal Reflux Disease (GERD) of Los Angeles (LA) Grades A to D
The goal of this clinical trial is to investigate how well linaprazan glurate can maintain healed erosive esophagitis (EE) caused by GERD in participants who have participated in a prior healing trial, compared to lansoprazole (an approved treatment for GERD). Researchers will also examine:
* the effect of linaprazan glurate on heartburn symptoms compared to lansoprazole.
* whether linaprazan glurate treatment is safe and tolerable, based on symptoms and procedures such as blood and urine tests, endoscopy, and electrocardiograms (measure the heart's electrical activity). Endoscopy means that the doctor will insert a thin, flexible tube with a camera down the throat to look at each participant's esophagus area and collect small tissue samples (called biopsies).
* the side effects that may happen during treatment with linaprazan glurate.
Participants must be between 18 to 80 years old and have participated in a prior healing trial with healed EE (due to GERD) confirmed by an endoscopy either from the prior healing trial or from the initial period of this trial. Participants cannot participate if they are not healed, had to stop trial treatment because of a side effect in a prior healing trial, or if they have a condition that could make it unsafe.
The study is a randomized, double-blind, active comparator-controlled clinical trial lasting for almost 14 months. Randomized means that participants are assigned by chance (like flipping a coin) to one of the treatment groups and double-blind means neither the participants nor the study team will know which treatment is given. Participants will be placed into one of three groups:
* Linaprazan glurate - High dose
* Linaparazan glurate - Low dose, and
* Lansoprazole - marketed approved dose Everyone will take a total of 2 tablets and 1 capsule orally every day for up to 52 weeks. The tablets and capsule will be separated into a morning dose and an evening dose. Some tablets or capsules will be placebos (look like medicine but contain no active drug).
Participants will complete several questionnaires on an electronic device during treatment. An endoscopy will be performed after 24 weeks of treatment to determine if healing has been maintained. If healing has been maintained, the participant will continue taking trial treatment and another endoscopy will be performed at 52 weeks. If healing has not been maintained at 24 weeks or if the participant has reached 52 weeks, the participant will stop taking trial treatment and return for a follow up visit.
* the effect of linaprazan glurate on heartburn symptoms compared to lansoprazole.
* whether linaprazan glurate treatment is safe and tolerable, based on symptoms and procedures such as blood and urine tests, endoscopy, and electrocardiograms (measure the heart's electrical activity). Endoscopy means that the doctor will insert a thin, flexible tube with a camera down the throat to look at each participant's esophagus area and collect small tissue samples (called biopsies).
* the side effects that may happen during treatment with linaprazan glurate.
Participants must be between 18 to 80 years old and have participated in a prior healing trial with healed EE (due to GERD) confirmed by an endoscopy either from the prior healing trial or from the initial period of this trial. Participants cannot participate if they are not healed, had to stop trial treatment because of a side effect in a prior healing trial, or if they have a condition that could make it unsafe.
The study is a randomized, double-blind, active comparator-controlled clinical trial lasting for almost 14 months. Randomized means that participants are assigned by chance (like flipping a coin) to one of the treatment groups and double-blind means neither the participants nor the study team will know which treatment is given. Participants will be placed into one of three groups:
* Linaprazan glurate - High dose
* Linaparazan glurate - Low dose, and
* Lansoprazole - marketed approved dose Everyone will take a total of 2 tablets and 1 capsule orally every day for up to 52 weeks. The tablets and capsule will be separated into a morning dose and an evening dose. Some tablets or capsules will be placebos (look like medicine but contain no active drug).
Participants will complete several questionnaires on an electronic device during treatment. An endoscopy will be performed after 24 weeks of treatment to determine if healing has been maintained. If healing has been maintained, the participant will continue taking trial treatment and another endoscopy will be performed at 52 weeks. If healing has not been maintained at 24 weeks or if the participant has reached 52 weeks, the participant will stop taking trial treatment and return for a follow up visit.
开始日期2026-03-01 |
申办/合作机构 |
CTR20254718
多中心、随机、双盲双模拟、阳性药平行对照的Ⅲ期临床研究评价X842胶囊用于十二指肠溃疡患者的有效性和安全性
主要目的：评价X842胶囊每日1次50mg连续给药4到6周对十二指肠溃疡的内镜下溃疡愈合的有效性，以验证X842胶囊在6周内的内镜下溃疡愈合受试者比例非劣效于兰索拉唑肠溶胶囊；
次要目的：与兰索拉唑肠溶胶囊相比，评价X842胶囊改善十二指肠溃疡受试者的临床症状（上腹疼痛、胃烧灼感、反酸、恶心、呕吐、嗳气和腹胀）的有效性；与兰索拉唑肠溶胶囊相比，评价X842胶囊治疗十二指肠溃疡的安全性；观察X842胶囊用于十二指肠溃疡患者后血清胃泌素的治疗前后变化情况。
开始日期2025-12-17 |
申办/合作机构 上海生诺医药科技有限公司 [+1] |
CTIS2024-518194-34-00
An open, single arm, single-center, Phase 1 trial investigating the effect of 7-days-repeated administration of linaprazan glurate on the pharmacokinetics of repeated doses of an approved antibiotic in healthy participants
开始日期2025-11-11 |
申办/合作机构 |
100 项与 戊二酸利那拉生酯 相关的临床结果
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100 项与 戊二酸利那拉生酯 相关的转化医学
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100 项与 戊二酸利那拉生酯 相关的专利（医药）
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8
项与 戊二酸利那拉生酯 相关的文献（医药）2025-05-01·ALIMENTARY PHARMACOLOGY & THERAPEUTICS
Clinical Trial: Dose‐Finding Study of Linaprazan Glurate, A Novel Potassium‐Competitive Acid Blocker, Versus Lansoprazole for the Treatment of Erosive Oesophagitis
Article
作者: Unge, Peter ; Andersson, Kjell ; Popadiyn, Ivan ; Yektaei, Elham ; Rosenholm, Maria ; Vaezi, Michael ; Sharma, Prateek ; Larsson, Kajsa ; Armstrong, David ; Rosztóczy, Andras
ABSTRACT:
Background:
Linaprazan glurate, a potassium‐competitive acid blocker, is in development for the treatment of erosive oesophagitis and other acid‐related diseases.
Aim:
To evaluate the 4‐week healing rate and safety of four linaprazan glurate dosing regimens in patients with erosive oesophagitis.
Methods:
This double‐blind, dose‐finding study compared linaprazan glurate to lansoprazole. We included patients with endoscopically confirmed erosive oesophagitis (validated by a central review board) if they had Los Angeles (LA) grade C/D or LA grade A/B with partial response to at least 8 weeks of proton pump inhibitor therapy. Patients were randomised to 4 weeks of linaprazan glurate (25, 50, 75 or 100 mg twice daily) or lansoprazole (30 mg once daily), followed by 4 weeks of open‐label lansoprazole.
Results:
Of 248 patients randomised, central review confirmed erosive oesophagitis in 182 at screening endoscopy. Across all doses, linaprazan glurate achieved a 4‐week healing rate of 71.1% in intention‐to‐treat (ITT) analysis and 80.9% in per protocol (PP) analysis. In comparison, lansoprazole achieved healing rates of 60.6% (ITT) and 59.1% (PPS). The best performing linaprazan glurate dosing group outperformed lansoprazole by 28% in patients with LA grade A/B with partial PPI response and by more than 50% in patients with LA grade C/D.
Conclusions:
Linaprazan glurate demonstrated high 4‐week healing rates compared to lansoprazole, with a good safety profile, supporting its further development.
Trial Registration:
ClinicalTrials.gov: NCT05055128; EudraCT: 2020‐003319‐91
2024-11-01·Current gastroenterology reports
Potassium-competitive Acid Blockers: Current Clinical Use and Future Developments
Review
作者: Scarpignato, Carmelo ; Hunt, Richard H
Abstract:
Purpose of the Review:
Acid suppression with proton pump inhibitors (PPIs) represents the standard of care in the treatment of acid-related diseases. However, despite their effectiveness, PPIs display some intrinsic limitations, which underlie the unmet clinical needs that have been identified over the past decades. The aims of this review are to summarize the current status and future development of the new class of antisecretory drugs (potassium-competitive acid blockers, P-CABs) that have recently been introduced into medical practice.
Recent Findings:
Over the past decades, clinical needs unmet by the current acid suppressants have been recognized, especially in the management of patients with GERD, Helicobacter pylori infection and NSAID-related peptic ulcer. The failure to address these needs is mainly due to their inability to achieve a consistent acid suppression in all patients and, particularly, to control nighttime acidity. It was then realized that an extended duration of acid suppression would exert additional benefits. The available data with P-CABs show that they are able to address these unmet clinical needs.
Summary:
Four different P-CABs (vonoprazan, tegoprazan, fexuprazan and keverprazan) are currently available. However, only two of them are approved outside Asia. Vonoprazan is available in North, Central and South America while tegoprazan is marketed only in Latin American countries. Two other compounds (namely linazapran glurate and zestaprazan) are presently under clinical development. While clinical trials on GERD have been performed with all P-CABs, only vonoprazan and tegoprazan have been investigated as components of Helicobacter pylori eradication regimens. The available data show that—in the above two clinical indications—P-CABs provide similar or better efficacy in comparison with PPIs. Their safety in the short-term overlaps that of PPIs, but data from long-term treatment are needed.
2024-05-01·Journal of pharmaceutical and biomedical analysis
Absorption, distribution, metabolism and excretion of linaprazan glurate in rats
Article
作者: Jin Xiu ; Ying Yang ; Donghui Liu ; Ming Lu ; Chen Yang ; Xingxing Diao ; Xinyue Zhang ; Yali Yuan ; Yuandong Zheng ; Pingsheng Hu
Linaprazan (AZD0865, TX07) is one of potassium-competitive acid blockers. However, linaprazan is rapidly excreted from the body, shortening its acid inhibition property. Linaprazan glurate (X842) is a prodrug of linaprazan with a prolonged inhibitory effect on gastric acid secretion. Linaprazan glurate has entered clinical trials, but few studies have reported its metabolism in non-clinical and clinical settings. In this study, we studied the pharmacokinetics, tissue distribution, mass balance, and metabolism of linaprazan glurate in rats after a single oral dose of 2.4 mg/kg (100 µCi/kg) [14C]linaprazan glurate. The results demonstrated that linaprazan glurate was mainly excreted via feces in rats with 70.48% of the dose over 168 h. The plasma AUC0-∞ of linaprazan glurate in female rats was 2 times higher than that in male rats. Drug-related substances were mainly concentrated in the stomach, eyes, liver, small intestine, and large intestine after administration. In blood, drug-related substances were mostly distributed into plasma instead of hemocytes. In total, 13 metabolites were detected in rat plasma, urine, feces, and bile. M150 (2,6-dimethylbenzoic acid) was the predominant metabolite in plasma, accounting for 80.65% and 67.65% of AUC0-24h in male and female rats, respectively. Based on the structures, linaprazan glurate was mainly hydrolyzed into linaprazan, followed by a series of oxidation, dehydrogenation, and glucuronidation in rats. Besides, CES2 is the main metabolic enzyme involved in the hydrolysis of linaprazan glurate to linaprazan.
81
项与 戊二酸利那拉生酯 相关的新闻（医药）2026-03-07
在消化科门诊，有两类场景几乎每天都在上演：患者捂着胸口抱怨“反酸烧心好几年，换了好几种药，白天能压一压，一到半夜就呛醒，整宿睡不着”；临床医生面对难治性病例无奈感慨“PPI用了不少，可部分患者就是效果不佳，还总担心长期用药的安全问题”。
酸相关疾病（胃食管反流病、反流性食管炎、消化性溃疡等）作为消化科常见病、多发病，不仅严重影响患者生活质量，也给临床诊疗带来诸多挑战。今日，河北省利那拉生上市会顺利举办，同步开展酸相关疾病诊疗学术交流，省内消化、药学领域专家齐聚，梳理诊疗规范、解读药物进展，为临床合理用药提供了清晰指引。本文结合本次上市会核心学术内容、国内外权威指南共识及网络公开学术资料，系统化整理酸相关疾病诊疗干货，深化专业知识点，兼顾易懂性与专业性，仅供医疗卫生专业人士个人学习使用，具体临床诊疗请以指南及医嘱为准。
【免责声明】
本文内容整理自河北省利那拉生上市会学术交流内容、国内外官方发布的指南共识、多中心临床研究结果及网络公开学术资料，仅供医疗卫生专业人士个人学习交流使用，不构成任何临床诊疗建议，非专业人士请勿随意试药、自行用药。本文相关内容若涉及侵权，请联系作者及时删除，感谢理解与支持。一、直击临床痛点：酸相关疾病，不止“反酸烧心”那么简单
很多人以为酸相关疾病就是“胃酸多、反酸烧心”，实则不然——它是胃酸/胃蛋白酶分泌异常引发的一系列消化道疾病的统称，核心涵盖胃食管反流病（GERD）、反流性食管炎（RE）、消化性溃疡，还包括幽门螺杆菌（Hp）感染、非静脉曲张性上消化道出血、功能性消化不良等，是消化科最核心的常见病、多发病，且诊疗过程中仍有诸多未被满足的临床需求。1. 流行特征+疾病负担：发病率攀升，危害远超想象
近30年，我国胃食管反流病（GERD）患病率持续上升，涨幅达60%，成人反流性食管炎（RE）患病率达5.4%，其中中重度RE患者超420万，且患病群体逐渐年轻化。这种疾病的危害，远不止“反酸烧心”的不适：
隐蔽性强，易误诊漏诊：超半数患者不以反酸烧心为首发症状，反而表现为慢性咳嗽、咽部异物感、非心源性胸痛，常常辗转呼吸科、耳鼻喉科、心内科，耽误诊疗时机；
并发症风险高：长期未规范控制，可能出现食管狭窄、巴雷特食管，甚至食管腺癌发病风险升高，还可能引发复发性肺炎、支气管扩张等肺部相关问题，严重影响患者长期健康；
医疗负担较重：从全球数据来看，美国每年GERD相关医疗支出超240亿美元，英国年相关支出达7.6亿英镑，其中难治性患者医疗成本较普通患者翻倍，合并食管外症状的患者医疗支出也明显增加，给个人、家庭及医疗系统带来一定压力。2. 临床诊疗难点：传统PPI的“短板”，困扰医患双方
质子泵抑制剂（PPI）作为酸相关疾病治疗的经典药物，临床应用数十年，在控制症状、促进黏膜愈合方面发挥了重要作用，尤其是国家集采政策实施后，PPI价格大幅下降，大幅提升了药物可及性，让更多普通患者能负担得起基础治疗。但在临床实践中，其局限性也较为突出，成为医患双方共同面临的困扰：
起效慢，急性发作难快速缓解：PPI需3-5天才能达到稳态抑酸效果，多项研究显示，仅30%的患者在首剂PPI后实现全天症状完全缓解，对于反酸烧心急性发作、急诊就诊的患者，难以快速控制症状，影响患者就医体验。
控酸不持久，夜间酸突破高发：PPI半衰期较短，仅能抑制活化状态的质子泵，对夜间静息状态的质子泵作用有限，夜间酸突破发生率较高——这也是很多患者“白天还好，半夜呛醒”的核心原因，不仅严重影响睡眠，还可能增加反流相关并发症风险。
受饮食、基因影响大，个体差异明显：PPI需餐前30分钟空腹服用才能发挥最佳效果，但临床调研显示，仅42.3%的患者能严格遵守服药要求，上班族、作息不规律人群漏服率极高；同时，PPI主要经CYP2C19代谢，我国超40%人群存在该基因多态性，这类人群服用后疗效可能下降，个体差异较为显著。
长期用药有安全隐患，依从性有待提升：长期大剂量使用PPI，可能增加肠道菌群紊乱、感染风险升高、营养吸收障碍、骨质疏松等不良反应发生风险，同时存在高胃泌素血症风险；部分患者因担心副作用自行停药，导致病情反复，反而增加了后续治疗成本。二、药物迭代升级：P-CAB登场，弥补传统治疗短板
针对传统PPI的临床局限性，抑酸药物研发持续推进，钾离子竞争性酸阻滞剂（P-CAB）的问世，为酸相关疾病治疗提供了新的选择，其作用机制与临床价值已得到国内外指南的权威认可，成为临床诊疗的重要补充。1. 核心差异：P-CAB vs PPI，到底强在哪？
很多临床医生和患者会问，P-CAB和我们常用的PPI，本质区别是什么？用通俗的话来说，两者的核心差异的是“作用靶点和适用条件”，我们用一张简单的对比，帮大家快速理解：
PPI：只能“对付”活化状态的质子泵，还需要酸性环境才能被激活，就像“只在胃酸分泌时才能发挥作用”，抑酸效果有局限；
P-CAB：既能“对付”活化状态的质子泵，也能结合静止状态的质子泵，无论酸性还是中性环境，都能稳定发挥作用，相当于“全天候守护”，能全维度阻断胃酸分泌。
也正是这一机制优势，P-CAB完美弥补了PPI的短板：无需胃酸活化、不受进食影响（不用严格卡着餐前30分钟服用）、不受CYP2C19基因多态性干扰（不同体质患者疗效更稳定），且半衰期更长，抑酸效果更持久，能有效解决夜间酸突破、服药依从性差等临床痛点。2. 指南共识明确推荐：P-CAB的临床定位
目前，P-CAB的临床价值已得到全球权威指南的认可，成为酸相关疾病治疗的重要选择，结合国内外指南，核心推荐意见整理如下（精准提炼，便于临床参考）：
2024年《美国胃肠病协会关于P-CAB纳入临床实践的更新》：每日两次PPI治疗失败、有明确酸相关反流证据的患者，可选用P-CAB；重度RE（LA-C/D级）患者急性期及维持愈合治疗，可选用P-CAB。
2023年《中国胃食管反流病诊疗规范》：PPI和P-CAB均为GERD初始治疗和维持治疗的首选药物；难治性GERD患者，优先优化PPI使用，或换用P-CAB治疗。
2022年《中国胃食管反流病多学科诊疗共识》：PPI和P-CAB均为GERD治疗的首选药物，可缓解大部分患者症状与并发症；P-CAB可与PPI相互替代，填补传统治疗短板，其临床应用已得到亚洲多国指南一致推荐。三、河北新药上市：利那拉生（酯键P-CAB）学术全解析
本次河北省上市会推出的利那拉生，属于酯键P-CAB类药物，是我国自主研发的1.1类创新药，其作用机制、药代动力学特征及临床数据，在本次上市会中由省内专家进行了系统解读，结合网络公开的指南及研究资料，我们进行系统化梳理，兼顾专业性与易懂性，供临床参考。1. 药物核心特点：机制独特，优势突出（临床重点关注）
利那拉生的核心优势，源于其独特的酯键结构设计，结合药代动力学特征，主要体现在以下4点，精准匹配临床痛点：
起效快：药物达峰时间约1.25小时，首次给药即可快速达到血药浓度峰值，相较于部分传统PPI，能更快缓解反酸烧心症状，适合症状急性发作的患者；
服药便捷：无需餐前空腹服用，不受高脂饮食等进食因素影响，上班族、作息不规律人群无需刻意记服药时间，能大幅提升患者用药依从性；
抑酸持久：半衰期约8.68小时，可实现24小时持续平稳抑酸，能有效覆盖夜间胃酸分泌高峰，从根源上减少夜间酸突破，解决患者“夜间呛醒”的困扰；
安全性更优：独特的酯键结构，让药物进入体内后逐步水解、缓慢释放活性成分，避免血药浓度峰值过高，能有效减轻肝脏代谢负担，降低肝损伤风险。2. 临床研究数据：科学客观，明确临床价值
结合中国III期、国际II期多中心临床研究数据，利那拉生的疗效与安全性均得到验证，核心数据整理如下：
抑酸效果稳定：24h胃内pH≥4的时间占比（HTR）达71±4%，波动幅度小，可稳定维持在RE黏膜愈合所需的pH≥4 HTR 75%左右的标准，能有效促进食管黏膜愈合；
黏膜愈合率高：中国III期数据显示，RE患者接受利那拉生治疗8周，黏膜愈合率达94%，非劣于经典PPI兰索拉唑；国际II期数据显示，针对LA-C/D级重度RE患者，利那拉生治疗4周黏膜愈合率达70%，优于兰索拉唑（37.5%），在中重度黏膜损伤患者中表现更突出；
安全性可控：中国III期数据显示，利那拉生肝功能异常发生率仅1.1%，显著低于部分PPI及同类P-CAB药物；肝胆系统相关不良反应整体发生率较低，其中γ-谷氨酰转移酶（GGT）升高发生率7.42%，丙氨酸氨基转移酶（ALT）升高发生率1.8%，天门冬氨酸氨基转移酶（AST）升高发生率1.4%，均低于兰索拉唑；
适用人群广泛：药物相互作用较少，主要经CYP3A4代谢，对于合并心脑血管疾病、需联用阿司匹林、氯吡格雷等药物的人群，安全性更有优势；轻中度肝肾功能不全患者，无需调整用药剂量，临床适用场景更广泛。
【简明处方核心信息】
通用名称：戊二酸利那拉生酯胶囊
规格：50mg
获批适应症：反流性食管炎
用法用量：口服，空腹服用。成人每日1次，每次50mg，连续治疗8周。
禁忌：对本品任何成份过敏者禁用；正在服用阿扎那韦、奈非那韦或者利匹韦林的患者禁用。四、临床精准用药：利那拉生优先适用人群（结合会议学术分享）
结合本次上市会专家分享的临床经验及相关研究数据，利那拉生并非“万能药”，而是针对特定人群具有显著优势，临床需结合患者病情精准选择，以下5类人群可优先考虑，为临床决策提供参考：1. 中重度反流性食管炎（LA-C/D级）患者
此类患者食管黏膜损伤严重，传统PPI黏膜愈合率有限，病情易反复，甚至可能进展为食管狭窄、巴雷特食管。利那拉生在重度RE患者的黏膜愈合方面表现更优，能更快修复破损黏膜，降低并发症发生风险。2. 难治性GERD、PPI治疗效果不佳的患者
对于标准剂量PPI治疗8周症状仍无缓解，或停药后快速复发的难治性患者，核心问题多为PPI抑酸强度不足、受基因多态性影响疗效。利那拉生不受CYP2C19基因多态性干扰，抑酸作用更稳定，可作为此类患者的重要治疗选择。3. 夜间酸突破突出、严重影响睡眠的患者
夜间反流不仅严重影响患者睡眠质量，还可能增加喉头痉挛、气道窒息等风险。利那拉生半衰期较长，可实现24小时平稳抑酸，能有效覆盖夜间胃酸分泌高峰，从根源上解决夜间酸突破问题。4. 老年、多药联用、轻中度肝肾功能不全的特殊人群
老年患者常合并高血压、冠心病等多种基础病，需长期联用多种药物，肝肾功能存在生理性减退，对用药安全性和便捷性要求较高。利那拉生药物相互作用少，肝损风险较低，轻中度肝肾功能不全无需调整剂量，一天一次服药更便捷，更适合此类人群。5. 作息不规律、用药依从性差的中青年患者
上班族、作息不规律的中青年人群，难以严格遵守PPI餐前30分钟空腹服用的要求，漏服、错服是导致病情反复的核心原因。利那拉生不受进食影响，服药便捷，且起效较快，能大幅提升此类患者的用药依从性，帮助实现病情长期稳定控制。
会议专家同时指出，基于其抑酸作用特点，利那拉生在幽门螺杆菌根除、消化性溃疡治疗、内镜下黏膜剥离术（ESD）术后预防出血、非静脉曲张性上消化道出血、功能性消化不良等酸相关疾病领域，具有潜在的应用前景，相关临床研究仍在推进中，需更多真实世界数据进一步验证其临床价值。五、用药选择：集采+国谈，兼顾疗效、安全与经济
本次上市会上，药学领域专家重点解读了集采、国谈双重背景下，酸相关疾病治疗的药物经济学评价逻辑，强调临床用药需坚持“价值医疗”理念，兼顾疗效、安全性与经济性，严格遵循国家医保政策导向，合理选择药物，既保障患者获益，也推动医疗资源合理利用。1. 集采普惠民生，提升基础药物可及性
国家药品集中采购政策的实施，是惠及民生的重要举措——通过“以量换价”，大幅降低了包括PPI在内的常用药物价格，让更多普通患者能负担得起基础治疗，有效减轻了患者经济负担，同时提升了基础药物的临床可及性，为酸相关疾病的规范化治疗奠定了基础。
临床实践中，集采中选的PPI品种，凭借价格优势和明确的疗效，仍是轻症酸相关疾病患者的优选，尤其是对于轻症、间歇性发作的GERD/RE患者，按需短期使用集采PPI，既能满足临床治疗需求，又能控制医疗成本，符合国家政策导向和价值医疗理念。2. 药物经济学核心：不看单药价格，看全周期价值
药物经济学的核心，并非单纯对比单药价格，而是对药物的安全性、有效性、经济性进行综合评价，结合患者病情、治疗周期、并发症风险等因素，评估药物的全周期治疗成本。
对于中重度、难治性、合并高危因素的患者，部分PPI可能因起效慢、黏膜愈合率低导致病情反复、住院时间延长、出现并发症，反而增加整体医疗支出；而利那拉生等P-CAB类药物，虽单药价格高于部分集采PPI，但能快速控制症状、促进黏膜愈合，减少复发和再治疗，从长期治疗角度来看，反而具有更优的成本效果比，也能更好地保障患者长期健康。3. 分层用药原则：精准匹配，兼顾政策与临床需求
结合国家集采、国谈政策导向及临床实际需求，酸相关疾病临床用药应坚持“分层用药、精准匹配”的原则，实现疗效、安全与经济的双赢：
轻症、间歇性发作的GERD/RE患者：优先选择集采中选的PPI品种，按需短期治疗，既能满足治疗需求，又能响应国家集采政策，减轻患者经济负担；
中重度、难治性、合并高危因素的患者：结合患者具体病情，可选择抑酸作用更强、安全性更优的P-CAB类药物（如利那拉生），早期强效控制病情，降低后续复发和并发症的风险，符合价值医疗的核心要求。4. 利那拉生医保落地：创新药惠及更多患者
本次上市会同步介绍，戊二酸利那拉生酯胶囊已通过国家医保谈判正式落地河北及全国各省市——这也是国家医保政策支持创新药、惠及民生的具体体现。医保政策的覆盖，大幅降低了患者用药经济负担，提升了这款创新药的临床可及性，让更多符合适应症的患者能用上更优质、更适合的治疗药物，同时也为临床医生提供了更多精准用药选择。总结：精准诊疗，合理用药，守护消化道健康
酸相关疾病的诊疗，已进入精准化、个体化、全周期管理的新阶段，传统抑酸药物的局限性，推动了新型抑酸药物的研发与应用，而国家集采、国谈政策的推进，既保障了基础药物的可及性，也为创新药的临床应用提供了支持，形成了“基础治疗有保障、精准治疗有选择”的良好格局。
本次河北省利那拉生上市会，不仅完成了新药的上市启动，更通过学术交流，系统梳理了酸相关疾病的诊疗规范、药物进展及药物经济学应用逻辑，为省内临床医生提供了实用的学术参考。利那拉生作为酯键P-CAB类创新药，其独特的作用机制、明确的临床疗效和良好的安全性，为酸相关疾病的治疗提供了新的思路，尤其在中重度反流性食管炎、难治性GERD等病例中，具有重要的临床价值。
对于临床医生而言，需严格遵循国家政策导向，结合患者病情、药物特点及医保政策，制定个体化治疗方案，既重视集采药物的基础保障作用，也合理运用创新药弥补临床短板；同时，持续关注相关学术进展及真实世界研究数据，不断优化临床用药策略。
希望本文整理的学术干货，能为医疗卫生专业人士提供实用参考，也期待未来有更多创新药物和诊疗方案问世，在国家政策的指引下，共同推动酸相关疾病诊疗水平的提升，守护大众消化道健康。
2026-03-06
·药通社
这两年，要问仿制药哪款药竞争大？毫无疑问会想到富马酸伏诺拉生片。
从2022年，山东新时代首家过评之后，截至目前，富马酸伏诺拉生片过评企业已达41家，尚有65家报产，原研化合物专利还未到期，竞争就已超百家。
而正是因为原研化合物专利还未到期，富马酸伏诺拉生片也尚未被纳入国采。
但值得注意的是，这个品种距离进国采时间很近了，原研专利届满时间是2026年8月29日，仅剩五个多月时间，即使今年的12批国采赶不上，13批国采也基本板上钉钉。
按往常国采时间推测，富马酸伏诺拉生片更大几率进入13批国采，而按目前申报情况来看，到那时这个品种的竞争很大概率会破一百家，创下历史竞争之最。
如若今年12批国采来的比较晚，富马酸伏诺拉生片专利到期，刚好被纳入，竞争也势必要突破六十家，竞争同样相当激烈，尚不论还有超30家企业在做BE。
那么这个品种为何引得如此多企业布局？
首先是市场大。我国消化道疾病患者基数庞大，发病率高，尤其是胃部疾病，胃食管反流病、反流性食管炎、胃溃疡、十二指肠溃疡及幽门螺杆菌感染在18至64岁成年人群中的患病率分别约为10.5%、5.4%、2.5%、4.5%和41.5%。
据摩熵医药数据显示，2022年前与胃酸分泌相关的药物单医院端销售额就超四百亿，排名前三都是拉唑类（PPI），注射用奥美拉唑2021年医院端销售额高达50亿。
图源：摩熵医药
2022年起，随着拉唑类接连被集采，替丁类药物开始占主导，而2024年开始替丁类药物也开始被集采，开始降价，整体销售额跌到了两百万。
胃酸分泌相关的药物销售额确实在下降，但年一百多亿的需求量从未变过。
也是在这几年，P-CAB类药物开始在胃酸治疗领域崭露头角，全球首款就是伏诺拉生。
富马酸伏诺拉生片，由日本武田制药与大冢制药联合研发，作为全球首批上市的钾离子竞争性酸阻滞剂，于2014年在日本率先获批上市，随后逐步拓展至全球多个国家和地区。
2018年3月30日武田在国内提交上市，因与现有治疗手段相比具有明显临床优势，富马酸伏诺拉生片被纳入优先审评，并于2019年12月正式获批，商品名“沃克”，成为国内首款获批的P-CAB类药物。
其吸收与起效不受进食状态影响，患者可在任意时间给药，相较于PPI类药物需严格餐前服用的给药要求，大幅提升了患者的用药依从性。
2020年，伏诺拉生就成功纳入国家医保乙类目录，定价为28元/20mg。此后销售额就开始疯涨，以一年破1亿，两年近5亿的速度增长，2025年三季度破7亿，不出意外全年将正式破10亿。
图源：摩熵医药
原料药方面，伏诺拉生分子结构简单，原料药供应企业多，已有四十多家企业的原料药登记，以目前顺利的过评情况看，研发难度也不高。
综上，胃病市场庞大，伏诺拉生临床疗效明确，单品市场增速快且价格可观，本身研发难度也不高，企业能花比较低的成本获得一款市场不错的药物，发展成如今百余家企业竞争也不足为奇了。
国内的胃部疾病药物需求已经从2019年的拉唑类（PPI）占主导目前已转换为了替丁类(H2RAs)占主导，未来或许是P-CAB类的天下。
除伏诺拉生外，国内还有4款P-CAB类新药，分别是罗欣的替戈拉生、柯菲平的凯普拉生、上海生诺医药的戊二酸利那拉生酯和大熊制药的菲优拉生。
每一款都足够引发热议。
替戈拉生是中国首款自主研发的P-CAB类药物，由罗欣药业2015年从一家韩国药企引进，2022年4月获批上市，随后两年内接连获批反流性食管炎、十二指肠溃疡、幽门螺杆菌根除三大核心适应证，成为目前国内首个获批三个适应证的P-CAB药物。
此品种市场同样强悍，2022年上市，24年销售额就破3亿，2025年前三个季度已破4亿。
凯普拉生由复星医药与柯菲平医药联合开发，于2023年2月获批，同年12月快速纳入国家医保，它的核心突破在于对伏诺拉生的分子结构进行了优化，通过增强水溶性和提升胃内分布浓度，在从药代动力学层面实现更快速、更高效的抑酸效率。
凯普拉生在2023年上市，2025年前三季度销售额已破2亿。
利那拉生酯于2024年12月获批上市，由生诺医药研发，是国内第四款获批上市P-CAB药物，2025年12月，华东医药与研发企业生诺医药达成了商业化合作。
菲优拉生于2025年9月获批，大熊制药株式会社研发，扬子江药业旗下海尼药业以3800亿韩元 (3.38亿美元) 的价格，获得了盐酸菲优拉生片在国内的权益。
目前这5款P-CAB类还都是片剂，已有多家企业在进行改良剂型研究，主要是改良研发注射剂，消化道疾病这一庞大而持久的治疗市场，竞争会持续。
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专利到期带量采购优先审批
2026-02-18
“The past year was marked by significant progress for Cinclus Pharma. Our first Phase III study has had a promising start, and we expect to present topline results during the second half of the year. The strategic licensing agreement with Zentiva provides a strong platform for successful commercialization in Europe and lays a solid foundation for expansion into other markets. Following the inclusion of linaprazan glurate on China’s national reimbursement list, our Chinese partner plans to launch the product on the market in 2026. With superior acid control compared to existing treatment options, linaprazan glurate has the potential to meet the substantial medical need among patients suffering from the more severe forms of erosive GERD, which we aim to confirm in the ongoing Phase III study”, says Christer Ahlberg CEO of Cinclus Pharma.
“The past year was marked by significant progress for Cinclus Pharma. Our first Phase III study has had a promising start, and we expect to present topline results during the second half of the year. The strategic licensing agreement with Zentiva provides a strong platform for successful commercialization in Europe and lays a solid foundation for expansion into other markets. Following the inclusion of linaprazan glurate on China’s national reimbursement list, our Chinese partner plans to launch the product on the market in 2026. With superior acid control compared to existing treatment options, linaprazan glurate has the potential to meet the substantial medical need among patients suffering from the more severe forms of erosive GERD, which we aim to confirm in the ongoing Phase III study”, says Christer Ahlberg CEO of Cinclus Pharma.
Financial summary, October-December 2025 » Net sales amounted to TSEK 13,632 (4,580). » Operating income/loss (EBIT) amounted to TSEK -62,011 (-56,889). » Net income/loss for the period was TSEK -61,184 (-54,259) and earnings/loss per share before and after dilution were SEK -1.31 (-1.17). » Total cash flow for the period amounted to TSEK -50,814 (-79,197). » Cash and cash equivalents at the end of the period amounted to TSEK 487,254 (566,716). Financial summary, January-December 2025 » Net sales amounted to TSEK 57,470 (4,580). » Operating income/loss (EBIT) amounted to TSEK -199,558 (-169,639). » Net income/loss for the period was TSEK -183,972 (-168,031) and earnings/loss per share before and after dilution were SEK -3.95 (-4.54). » Total cash flow for the period amounted to TSEK -77,836 (476,833). » Cash and cash equivalents at the end of the period amounted to TSEK 487,254 (566,716). Significant events during the period October-December 2025
Financial summary, October-December 2025
Financial summary, January-December 2025
Significant events during the period October-December 2025
» In early October, it was announced that the first patient had been dosed in the company’s Phase III study, HEEALING 1, which aims to confirm the efficacy of linaprazan glurate in patients with erosive gastroesophageal reflux disease. » In the beginning of October Cinclus Pharma presented an abstract on linaprazan glurate at the United European Gastroenterology Week (UEGW) in Berlin. The abstract highlights positive data on the optimized tablet formulation developed for Phase III studies and future commercialization. » In October Cinclus Pharma received positive feedback from a recent Chemistry, Manufacturing and Controls (CMC) meeting with the FDA. During the meeting, the FDA provided clear guidance and alignment with the company’s proposed CMC strategy preparation for the upcoming new drug application (NDA) submission. » Cinclus Pharma announced in November that it had sponsored a scientific abstract highlighting the clinical and economic costs of PPI treatment failures in patients with severe erosive GERD. The abstract was presented at the ISPOR Europe 2025 conference in Glasgow. » Cinclus Pharma hosted a virtual event to share insights on clinical practice for erosive Gastroesophageal Reflux Disease (GERD) patients in December. The event featured Professor Prateek Sharma from the Cancer Center in Kansas City who provided insights on the current treatment landscape and the unmet medical need among patients with erosive GERD, as well as the potential of Cinclus Pharma’s drug candidate linaprazan glurate. » Cinclus Pharma has recruited Magnus Christensen as CFO. He will assume his new role in the spring of 2026. » Linaprazan glurate earns China’s National Reimbursement Listing for the treatment of erosive GERD. This enables broad patient access, and the product is now expected to be launched on the Chinese market in 2026. Significant events after the end of the period
Significant events after the end of the period
» At an Extraordinary General Meeting on 19 January, Kjell Andersson was elected as a new board member after Peter Unge had announced his wish to step down from his position on the company’s board. » In January, Cinclus Pharma announced that the European Medicines Agency (EMA) has provided positive feedback following scientific advice regarding Chemistry, Manufacturing and Controls (CMC) for linaprazan glurate. » In February, FDA provided a positive assessment of Cinclus Pharma’s nonclincial development plan for linaprazan glurate following a scientific advice meeting. Presentation of the interim report A webcast will be held on February 18, 2026, at 10:00 CET via Inderes. If you wish to participate via webcast please use the link below. Via the webcast you are able to ask written questions. https://cinclus-pharma.events.inderes.com/q4-report-2025 If you wish to participate via teleconference please register on the link below. After registration you will be provided phone numbers and a conference ID to access the conference. You can ask questions verbally via the teleconference. https://events.inderes.com/cinclus-pharma/q4-report-2025/dial-in
Presentation of the interim report
For additional information, please contact:
For additional information, please contact:
Christer Ahlberg, CEO Phone: +46 70 675 33 30 e-mail: christer.ahlberg@cincluspharma.com
Henrik Vikström, IR Phone: +46 70 952 80 06 e-mail: henrik.vikström@cincluspharma.com
About Cinclus Pharma
About Cinclus Pharma
Cinclus Pharma Holding AB (publ) is a late-stage clinical pharmaceutical company developing drugs for the treatment of acid-related diseases and disorders of the upper gastrointestinal tract. The company's leading drug candidate is linaprazan glurate, a prodrug of P-CAB linaprazan, which was originally developed by AstraZeneca. Linaprazan glurate has the potential to heal erosions in the esophageal mucosa and relieve symptoms of gastroesophageal reflux disease (GERD) more effectively than current treatments like proton pump inhibitors (PPI). The safety and efficacy of linaprazan and linaprazan glurate have been documented in over 30 phase I and two phase II studies involving more than 3,000 participants. The first Phase III study commenced in 2025. GERD affects approximately 133 million adults in the US and EU, and there is a significant need for new drugs to treat the most severe cases: around 10 million patients. Linaprazan glurate is developed to meet these needs. For more information, visit www.cincluspharma.com.
Attachments
Attachments
Year End Report 2025
临床3期引进/卖出临床2期高管变更财报
100 项与 戊二酸利那拉生酯 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 |
|---|---|---|---|
| 反流性食管炎 | 中国 | 2024-12-01 |
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 |
|---|---|---|---|---|
| 食管炎 | 临床3期 | - | 2026-03-01 | |
| 幽门螺杆菌感染 | 临床3期 | 中国 | 2026-01-21 | |
| 幽门螺杆菌感染 | 临床3期 | 中国 | 2026-01-21 | |
| 十二指肠溃疡 | 临床3期 | 中国 | 2025-12-17 | |
| 糜烂性食管炎 | 临床3期 | 美国 | 2025-10-03 | |
| 糜烂性食管炎 | 临床3期 | 保加利亚 | 2025-10-03 | |
| 糜烂性食管炎 | 临床3期 | 捷克 | 2025-10-03 | |
| 糜烂性食管炎 | 临床3期 | 德国 | 2025-10-03 | |
| 糜烂性食管炎 | 临床3期 | 匈牙利 | 2025-10-03 | |
| 糜烂性食管炎 | 临床3期 | 波兰 | 2025-10-03 |
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临床结果
临床结果
适应症
分期
评价
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| 研究 | 分期 | 人群特征 | 评价人数 | 分组 | 结果 | 评价 | 发布日期 |
|---|
临床1期 | 75 | (25 mg Linaprazan Glurate QD) | 網齋醖壓鬱淵願顧願築(夢蓋簾築膚繭觸顧製繭) = 鏇壓繭醖醖繭選餘鬱選 衊構繭齋願鏇選鹹積築 (遞鑰簾艱淵簾網蓋壓築, 1650.6) 更多 | - | 2025-05-07 | ||
(50 mg Linaprazan Glurate QD) | 網齋醖壓鬱淵願顧願築(夢蓋簾築膚繭觸顧製繭) = 鬱願壓艱顧鏇蓋廠範衊 衊構繭齋願鏇選鹹積築 (遞鑰簾艱淵簾網蓋壓築, 2281.0) 更多 | ||||||
临床2期 | 248 | 選積淵壓獵範夢遞醖夢(顧獵鏇膚鬱壓蓋願蓋鑰) = 襯餘夢鑰鬱壓餘壓鏇艱 鏇齋鏇壓醖糧膚鹽繭鹹 (鏇淵選鹽壓鏇遞製範淵 ) 更多 | 积极 | 2025-04-04 | |||
選積淵壓獵範夢遞醖夢(顧獵鏇膚鬱壓蓋願蓋鑰) = 遞範壓構壓膚鏇積廠窪 鏇齋鏇壓醖糧膚鹽繭鹹 (鏇淵選鹽壓鏇遞製範淵 ) 更多 | |||||||
临床1期 | - | 67 | (Reference Formulation (Treatment A)) | 製範範範艱願窪餘廠繭(蓋衊網廠淵選夢觸齋範) = 繭觸醖構願鬱製觸製齋 蓋網觸鑰醖鬱簾獵餘鬱 (選鑰範製鏇鬱簾淵鹹鬱, 1.51) 更多 | - | 2025-04-03 | |
(Test Formulation (Treatment B)) | 製範範範艱願窪餘廠繭(蓋衊網廠淵選夢觸齋範) = 簾積觸簾獵淵艱願廠範 蓋網觸鑰醖鬱簾獵餘鬱 (選鑰範製鏇鬱簾淵鹹鬱, 1.32) 更多 | ||||||
临床2期 | 90 | 膚糧糧獵鏇網蓋夢顧鬱(窪壓窪鑰網觸壓鬱鹽鑰) = The incidence of drug-related treatment-emergent adverse events did not differ among groups 鬱鬱廠夢鹹築衊繭齋壓 (齋壓廠範選觸觸築觸壓 ) 更多 | 积极 | 2025-04-01 | |||
临床1期 | 35 | (Part I) | 膚壓範繭構範鏇淵積壓(鹽鬱積觸網選壓壓膚襯) = 構鑰襯鹽鹽窪鑰鹹壓淵 醖選膚廠製遞蓋網構網 (鏇壓積鹽鏇襯壓廠餘鏇, 5649) 更多 | - | 2025-01-03 | ||
Midazolam+Linaprazan glurate hydrochloride (HCl) (Part II) | 鏇願窪蓋鬱鹹艱觸觸淵(蓋廠衊鏇鬱蓋鹽網鹹鹹) = 憲築築淵鏇遞獵壓鹹衊 窪鹹壓夢艱蓋壓夢淵淵 (積願構鑰網築壓鑰廠鹽, 13.98) 更多 | ||||||
临床2期 | 248 | (X842 25 mg BID) | 壓壓憲願選憲窪簾窪構 = 壓衊鹽廠範製獵餘積鬱 襯繭簾範齋遞積遞鏇觸 (構選醖繭鏇製淵獵鏇積, 壓憲遞觸艱鹽築窪觸觸 ~ 鑰製範憲遞顧壓襯廠繭) 更多 | - | 2023-11-01 | ||
(X842 50 mg BID) | 壓壓憲願選憲窪簾窪構 = 鏇構構餘觸淵獵壓製艱 襯繭簾範齋遞積遞鏇觸 (構選醖繭鏇製淵獵鏇積, 獵蓋選鏇艱製鏇顧積繭 ~ 鏇齋鏇衊觸衊餘廠廠築) 更多 | ||||||
N/A | - | - | Linaprazan glurate 25 mg BID | 窪窪襯獵廠餘衊鑰範膚(鏇築鹽鹹糧選夢醖糧構) = 夢鹹構衊憲鬱獵淵顧壓 築顧艱製範衊願簾選襯 (繭餘積遞壓醖膚廠遞積, 59.7 ~ 84.7) | - | 2023-10-15 | |
Linaprazan glurate 50 mg BID | 窪窪襯獵廠餘衊鑰範膚(鏇築鹽鹹糧選夢醖糧構) = 鏇築積網製簾顧窪選夢 築顧艱製範衊願簾選襯 (繭餘積遞壓醖膚廠遞積, 73.8 ~ 91.1) |
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