替奈普酶(Tenecteplase) - 药物靶点：PLG_在研适应症：急性缺血性卒中，ST段抬高心肌梗死，急性心肌梗塞_专利_临床

概要

基本信息

药物类型

酶

别名

Metalyse、Tenecteplase (USAN/INN)、TNK

+ [6]

靶点

PLG

作用方式

刺激剂

作用机制

PLG刺激剂(纤溶酶原刺激剂)

治疗领域

神经系统疾病心血管疾病其他疾病

在研适应症

急性缺血性卒中ST段抬高心肌梗死急性心肌梗塞+ [2]

非在研适应症

导管功能障碍新型冠状病毒感染心脏停搏+ [7]

原研机构

Genentech, Inc.

在研机构

Boehringer Ingelheim International GmbH

Genentech, Inc.

Boehringer Ingelheim GmbH

+ [3]

非在研机构-

权益机构

Boehringer Ingelheim GmbH

Genentech, Inc.

最高研发阶段批准上市

首次获批日期

美国 (2000-06-02),

急性心肌梗塞

最高研发阶段(中国)批准上市

特殊审评-

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结构/序列

Sequence Code 431641667

来源: *****

关联

136

项与替奈普酶相关的临床试验

NCT07375966

/ Not yet recruiting临床2期IIT

Repeated Intravenous Thrombolysis for Ischemic Stroke With Medium to Large Vessel Occlusion Presenting Within 4.5 Hours of Onset With Tenecteplase (RITIS-TNK2): a Prospective, Randomized, Open Label, Blinded Assessment of Outcome, and Multi-center Study

While intravenous thrombolysis (IVT) within 4.5 hours is the standard medical reperfusion therapy, its efficacy is limited, particularly for large or medium vessel occlusions (LVO/MeVO), with low recanalization rates for IVT with rt-PA. The newer thrombolytic agent, tenecteplase (TNK), offers practical advantages-including single bolus administration, a longer half-life, and potentially higher fibrin specificity-and has been shown to be non-inferior to rt-PA.
Despite advances, a significant proportion of patients with LVO/MeVO do not achieve early clinical improvement after standard IVT, likely due to persistent occlusion from a high thrombus burden. Endovascular therapy, while highly effective for LVO, has limited accessibility. Therefore, there is an urgent need for more effective and widely accessible pharmacological strategies.
This study proposes a rescue strategy based on the hypothesis that a second dose of IVT may improve outcomes in patients with imaging-confirmed LVO or MeVO who show no significant neurological improvement one hour after standard TNK thrombolysis (administered within 4.5 hours of stroke onset). The primary aim of this study is to formally evaluate the efficacy and safety of a repeated dose of intravenous tenecteplase in this specific patient population.

开始日期2026-03-01

申办/合作机构

中国人民解放军北部战区总医院

NCT07375953

/ Not yet recruiting临床2期IIT

Repeated Intravenous Thrombolysis for Ischemic Stroke Within 3.0 Hours of Onset With Tenecteplase (RITIS-TNK): a Prospective, Randomized, Open Label, Blinded Assessment of Outcome, and Multi-center Study

Despite being the standard pharmacological reperfusion therapy for acute ischemic stroke, intravenous thrombolysis is limited by suboptimal recanalization rates. Tenecteplase (TNK), a newer thrombolytic agent, offers practical advantages over alteplase, including single bolus administration. However, a significant proportion of patients fail to achieve early clinical improvement after standard thrombolysis, likely due to persistent vessel occlusion.
This study proposes to investigate a rescue strategy for patients who do not show significant neurological improvement within one hour after receiving standard intravenous tenecteplase within 3 hours of stroke onset. The primary objective is to evaluate the safety and feasibility of administering a second dose of tenecteplase in this scenario. The study will also explore the potential efficacy of this approach in improving recanalization and functional outcomes.

开始日期2026-03-01

申办/合作机构

中国人民解放军北部战区总医院

NCT07361302

/ Not yet recruiting临床3期

TENACITY - A Phase III, Prospective, Randomized, Open-label, Blinded Endpoint Assessment (PROBE) to Assess Efficacy and Safety of i.v. Tenecteplase vs Standard of Care in Patients With Acute Ischemic Stroke (Including Wake-up Stroke), Last Known Well >4.5 h With Imaging Evidence of Salvageable Ischemic Tissue

This study is open to adults who had an acute stroke caused by a clot blocking a blood vessel in the brain (acute ischemic stroke). This study is for people who had an acute stroke or woke up with a stroke and were last seen well more than 4.5 hours before joining the study. Participants need to have imaging that shows there is brain tissue that can still be saved. They also should not be planned to receive a procedure to remove the blood clot.
The purpose of this study is to find out whether a medicine called tenecteplase helps people recover from an acute stroke. Tenecteplase is already used to treat people within 4.5 hours after they had a stroke. This study tests if tenecteplase also helps if it is given more than 4.5 hours after the stroke.
Participants are put into 2 groups randomly, which means by chance. One group gets tenecteplase as a single injection into a vein. The other group receives standard medical practice. Participants have an equal chance of receiving tenecteplase or the standard treatment.
Participants are in the study for about 3 months. In the beginning, participants stay in the hospital for about 1 week. During the study, participants have 7 clinical examinations or visits. The last 2 of these visits will likely be done from home, allowing participants to complete certain assessments remotely. Doctors regularly test participants' recovery using a scale that measures the level of disability or dependence in daily activities. The results are compared between the 2 groups to see whether the treatment works. The doctors also check participants' health and take note of any unwanted effects.

开始日期2026-02-17

申办/合作机构

Boehringer Ingelheim GmbH

100 项与替奈普酶相关的临床结果

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100 项与替奈普酶相关的转化医学

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100 项与替奈普酶相关的专利（医药）

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1,016

项与替奈普酶相关的文献（医药）

2026-12-01·Journal of Central Nervous System Disease

Immediate Brainstem Hemorrhage after Thrombolysis in Ischemic Stroke With Poorly Controlled Hypertension: Insights From Three Clinical Cases

Article

作者: Mei, Bin ; Yan, Nao ; Yang, Niao ; Sun, Dong ; Shen, Lei

Objective:

To report three cases of immediate brainstem hemorrhage following intravenous thrombolysis with tenecteplase (TNK) in patients with minor ischemic stroke, resulting in poor outcomes and death.

Methods:

We describe the clinical characteristics, imaging findings, and outcomes of three patients who developed brainstem parenchymal hemorrhage immediately after TNK thrombolysis.

Results:

All three patients had minor ischemic stroke (National Institute of Health stroke scale score ≤5) and presented with elevated blood pressure on admission. Blood pressure was lowered to guideline-recommended levels (<180 mmHg) using intravenous antihypertensives before thrombolysis. Despite rapid brain protection measures, including hematoma evacuation or external ventricular drainage in two cases and conservative management in one, all patients died due to brainstem hemorrhage.

Conclusion:

These cases suggest that fatal brainstem hemorrhage may occur after TNK thrombolysis in minor stroke. For patients with a history of poorly controlled hypertension, careful risk assessment and aggressive blood pressure management are critical if thrombolysis is considered.

2026-03-01·AMERICAN JOURNAL OF EMERGENCY MEDICINE

Extended thrombolysis in acute ischemic stroke: A Bayesian meta-analysis and umbrella review

Article

作者: Brophy, James M ; Garg, Ravi

BACKGROUND:

For acute ischemic stroke, national practice guidelines recommend thrombolysis within a 4.5-h time window from symptom onset. Randomized trials with advanced neuroimaging have now examined extended thrombolytic time windows, and multiple meta-analyses have provided positive endorsements. However, these previous meta-analyses have not fully exploited the available data, examined quality of life, or reported the probability of clinically meaningful effects. This meta-analysis addresses these potential shortcomings.

METHODS:

We performed a i) systematic literature review up to August 1, 2025, of all randomized controlled trials comparing thrombolysis (alteplase or tenecteplase) with the assistance of advanced neuroimaging to standard, non-thrombolytic therapy in acute ischemic stroke patients with unknown time or beyond 4.5 h since symptom onset and ii) an umbrella review of previous meta-analyses addressing this issue. Our primary outcome was the mean difference in the utility-weighted modified Rankin Scale (uw-mRS) scores. Secondary outcomes were the absolute risk difference (ARD) for minor disability status and mortality. Bayesian random effects meta-analyses were performed assuming a normal-normal hierarchical model with non-informative priors, which permitted probability calculations for benefit, harm, and regions of practical equivalence (ROPE).

RESULTS:

Six original randomized trials of extended thrombolysis and 7 meta-analyses were identified but none had considered a uw-mRS score or reported direct probability statements regarding benefit or harm. Our primary uw-mRS outcome showed a ROPE probability of 99 % with only a 1 % probability of a clinically beneficial response with extended alteplase. There was also a 72 % probability that mortality increased by at least 1 life / 100 treated with extended thrombolysis.

CONCLUSIONS:

In contrast with previous publications, this meta-analysis and umbrella review highlights the uncertainty of clinical benefits from extended thrombolysis treatment windows and the need for further high-quality research before this treatment is accepted into routine practice.

2026-03-01·ANNALS OF PHARMACOTHERAPY

Weighing in on the Recent Approval of Tenecteplase for Acute Ischemic Stroke: Significance of Body Weight and the New Dosing Schedule

Letter

作者: Shiue, Harn J. ; Sands, Kara A. ; Dumitrascu, Oana M.

132

项与替奈普酶相关的新闻（医药）

2026-02-04

·drugs

Guideline Updated for Early Management of Acute Ischemic Stroke

WEDNESDAY, Feb. 4, 2026 -- In a guideline issued by the American Heart Association/American Stroke Association and published online Jan. 26 in Stroke , updated recommendations are presented for the early management of patients with acute ischemic stroke (AIS). Shyam Prabhakaran, M.D., from the University of Chicago, and colleagues updated the guideline for the early management of patients with AIS to replace the 2018 guideline. The authors note that mobile stroke units (MSU) enable rapid identification and treatment of thrombolytic-eligible patients with AIS and included recommendations relating to MSU implementation. For patients with suspected stroke in the prehospital setting, the guideline endorses consideration of the characteristics of the local system of care and direct transport to the closest endovascular thrombectomy (EVT)-capable hospital. For patients with AIS, intravenous thrombolysis is a mainstay of medical management; the new guideline endorses the use of either alteplase or tenecteplase in the 4.5-hour thrombolytic treatment window. Rapid thrombolytic treatment within the 4.5-hour window is recommended for eligible patients with disabling deficits, regardless of the National Institutes of Health Stroke Scale (NIHSS) score, without advanced imaging selection. The benefit of thrombolysis has not been demonstrated for patients with nondisabling deficits in the 4.5-hour window. EVT has been established as standard treatment for patients with AIS with large vessel occlusion and should be considered in patients previously considered ineligible. For patients with basilar artery occlusion presenting within 24 hours of symptom onset and with an NIHSS score ≥10, EVT is strongly recommended. Recommendations are also included for interventional treatment in pediatric patients with AIS. "New recommendations in the guideline expand access to cutting-edge treatments, such as clot-removal procedures and medications, simplify imaging requirements so more hospitals can act quickly, and introduce guidance for pediatric stroke for the first time," Prabhakaran said in a statement. Several members of the Writing Committee and Peer Review Committee disclosed ties to the biopharmaceutical industry. Abstract/Full Text

AHA会议临床研究

2026-02-02

·drugs

IV Tenecteplase Not Recommended for Central Retinal Artery Occlusion

MONDAY, Feb. 2, 2026 -- Intravenous tenecteplase administered within 4.5 hours after onset of central retinal artery occlusion does not improve vision recovery at 30 days compared with oral aspirin , according to a study published in the Jan. 29 issue of the New England Journal of Medicine . Stephen J. Ryan, M.D., from Oslo University Hospital in Norway, and colleagues conducted a phase 3, randomized, controlled trial involving adults with acute, nonarteritic central retinal artery occlusion who had symptom onset within 4.5 hours before treatment. Patients at 16 sites in six countries were randomly assigned to receive intravenous tenecteplase and oral placebo or intravenous placebo and oral aspirin (40 and 38 individuals, respectively). Vision recovery was assessed as the primary end point, defined as a best corrected visual acuity (BCVA) in the affected eye of up to 0.7 logMAR at 30 days. The researchers found that 20 and 24 percent of patients in the tenecteplase and aspirin groups, respectively, had vision recovery at 30 days (risk difference, −3.7 percentage points; 95 percent confidence interval, −22.0 to 14.7; P = 0.69). With regard to secondary visual end points of a BCVA of up to 0.5 logMAR, mean improvement in BCVA, and perimetry score at 30 days, no substantial difference was seen between the groups. A greater incidence of adverse events was seen in the tenecteplase group, including one fatal intracranial hemorrhage. "These findings do not support the routine use of thrombolytic therapy to treat central retinal artery occlusion," the authors write. The study was supported by an unconditional grant from Boehringer Ingelheim Norway for the purchase of tenecteplase. Abstract/Full Text (subscription or payment may be required)

临床3期临床结果

2026-01-30

·今日头条

2026脑梗热点：青年发病激增，科研与医保新政双突破

2026年初，脑梗成为健康领域热议焦点，青年患者占比显著上升，同时科研突破与医保新政为患者带来新希望，引发广泛关注。临床数据显示，30-45岁脑梗患者占比已达25%，年轻化与长期熬夜、高糖饮食、久坐、烟酒无度及高血压失控密切相关。38岁的职场人突发剧烈呕吐伴肢体麻木，确诊为脑干梗死，此前他常熬夜加班、奶茶不离手，却未重视血压偏高问题。专家强调，年轻人需警惕单侧麻木、言语不清、视物模糊等早期信号，牢记FAST原则：面部歪斜、手臂无力、言语不清，立即就医。科研方面，北京天坛医院证实依达拉奉右莰醇联合取栓治疗，可提升患者90天功能独立率至55%，为联合治疗提供高等级证据。深圳团队发现DKK2蛋白是脑梗损伤扩大关键靶点，为新药研发开辟方向。医保新政也传来利好，2026年起溶栓、取栓费用全额报销，替奈普酶降至1200元/支，康复报销期限延长至1年，社区医院报销比例最高达95%，大幅减轻患者负担。从青年发病预警到科研突破、医保兜底，2026年脑梗防治正全方位升级，守护脑血管健康需从日常做起。

100 项与替奈普酶相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D06070	替奈普酶	B01AD11	DB00031

研发状态

批准上市

10 条最早获批的记录,

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适应症	国家/地区	公司	日期
急性缺血性卒中	美国	Genentech, Inc.	2025-02-28
ST段抬高心肌梗死	美国	Genentech, Inc.	2025-02-28
急性心肌梗塞	美国	Genentech, Inc.	2000-06-02

未上市

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
闭塞	临床3期	巴西	Boehringer Ingelheim GmbH	2022-01-20
大脑中动脉梗塞	临床3期	美国	Genentech, Inc.	2019-03-02
大脑中动脉梗塞	临床3期	加拿大	Genentech, Inc.	2019-03-02
脑卒中	临床3期	美国	Genentech, Inc.	2019-03-02
脑卒中	临床3期	加拿大	Genentech, Inc.	2019-03-02
血栓形成	临床3期	美国	Genentech, Inc.	2019-03-02
血栓形成	临床3期	加拿大	Genentech, Inc.	2019-03-02
胸腔积液	临床3期	美国	Genentech, Inc.	2008-01-01
肺栓塞	临床3期	奥地利	Boehringer Ingelheim GmbH	2007-11-16
肺栓塞	临床3期	比利时	Boehringer Ingelheim GmbH	2007-11-16

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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


NCT04526951 (TenCRAOS, Pubmed \| N Engl J Med)	临床3期	视网膜动脉闭塞	78	Tenecteplase	獵範糧衊構淵鹽蓋艱淵(積鹽鏇憲膚製遞齋窪簾) = There was a greater incidence of adverse events in the tenecteplase group, including one fatal intracranial hemorrhage. 壓餘獵壓願積鹽壓鑰網 (顧襯願壓網憲築夢淵選 ) 更多	不佳	2026-01-29
				Aspirin
NCT04526951 (TenCRAOS, EURETINA2025)	临床3期	视网膜动脉闭塞	78	Tenecteplase	窪醖網選窪衊範遞餘壓(鏇鹹繭壓襯顧淵壓選簾) = 襯鬱積糧選範衊繭鑰遞鹽蓋壓夢醖遞壓簾襯遞 (網襯壓積夢憲簾築窪憲 ) 更多	不佳	2025-09-04
				Aspirin	窪醖網選窪衊範遞餘壓(鏇鹹繭壓襯顧淵壓選簾) = 範積艱鏇積遞築齋齋襯鹽蓋壓夢醖遞壓簾襯遞 (網襯壓積夢憲簾築窪憲 ) 更多
NCT04086147 \| NCT04516993 (CHABLIS-T; CHABLIS-T II, Pubmed \| J Am Heart Assoc)	临床2期	-	199	Tenecteplase	夢鹽蓋餘觸構廠糧壓積(顧窪觸蓋願齋糧願窪製) = 淵夢鹹鑰繭願鹹網夢餘鑰鏇糧願觸遞衊觸觸積 (鏇廠選糧遞襯觸構襯襯 ) 更多	积极	2025-06-17
NCT02777580 \| NCT00623623 (STREAM-1 and STREAM-2, Pubmed \| Am Heart J)	N/A	心肌梗塞 \| ST段抬高心肌梗死 \| 急性心肌梗塞	1,103	Full-dose TNK	觸糧觸膚艱糧選觸網廠(獵繭構繭醖鏇選鑰鑰醖) = 淵鹽窪簾齋築繭衊壓淵醖範鏇鹹鑰範壓選範壓 (簾襯選築構壓夢構淵願 ) 更多	积极	2025-06-01
				Half-dose TNK	觸糧觸膚艱糧選觸網廠(獵繭構繭醖鏇選鑰鑰醖) = 膚顧獵醖膚鬱簾遞鹹範醖範鏇鹹鑰範壓選範壓 (簾襯選築構壓夢構淵願 ) 更多
AAN2025	N/A	急性缺血性卒中	917	Tenecteplase	築獵艱網獵網齋廠積蓋(齋鹽壓製餘範範衊獵鹹): RR = 0.8 (95% CI, 0.35 ~ 1.83), P-Value = 0.597 更多	积极	2025-04-07
				Alteplase
NCT03889249 (FDA_CDER) 人工标引	临床3期	急性缺血性卒中	1,147	TNKase	齋膚觸廠範憲廠製襯網(鹽網製齋膚壓遞構鏇餘) = 醖積積願製廠鏇艱窪鹹鹽壓鹹簾鏇獵餘壓顧願 (獵廠築製憲廠網憲願選 )	积极	2025-02-28
				Activase	齋膚觸廠範憲廠製襯網(鹽網製齋膚壓遞構鏇餘) = 網艱糧淵夢艱衊憲顧願鹽壓鹹簾鏇獵餘壓顧願 (獵廠築製憲廠網憲願選 )
ChiCTR2200064809 (Pubmed \| JAMA)	临床3期	急性缺血性卒中	540	Intra-arterial Tenecteplase	鹹鹽鏇鹽繭獵鹹築鹽夢(鹽鑰簾網鏇鬱鏇蓋鑰簾): adjusted risk ratio = 1.15 (95% CI, 0.97 ~ 1.36) 更多	不佳	2025-02-18
				Tenecteplase (Control Group (No intra-arterial thrombolysis))
NCT04516993 (CHABLIS-T II, Pubmed \| Stroke)	临床2期	脑卒中	224	Tenecteplase 0.25 mg/kg	顧網範蓋蓋糧積鏇襯鹽(鬱醖顧觸憲網製蓋觸艱): adjusted relative risk = 3.0 (95% CI, 1.6 ~ 5.7), P-Value = 0.001 更多	积极	2025-02-01
				Tenecteplase (Best Medical Treatment)
NCT05172934 (ALLY Pilot Trial, Pubmed \| Stroke)	临床2期	血栓形成	20	Intraarterial Tenecteplase	選襯範鏇獵鏇膚觸構構(蓋網餘淵積網齋衊鑰齋) = 廠窪觸願鬱觸構膚壓鏇膚壓獵鹹觸獵蓋淵積憲 (顧構淵製襯鑰網糧鹽窪 )	积极	2025-02-01
NCT02398656 (TEMPO-2, CTgov)	临床3期	缺血性卒中 \| 急性缺血性卒中 \| 闭塞	1,274	Tenecteplase (Tenecteplase (tNK))	鹹觸淵鹹膚糧壓觸夢窪 = 願膚觸醖壓築鑰衊艱鏇廠構願蓋鑰願襯遞鹽鬱 (壓膚醖壓網糧夢衊築網, 憲衊窪繭衊襯觸築選繭 ~ 鏇夢淵窪膚築製鏇憲夢) 更多	-	2025-01-31
				Antiplatelet treatment (Control (Antiplatelet Agents))	鹹觸淵鹹膚糧壓觸夢窪 = 鏇遞糧簾餘製餘衊鹹淵廠構願蓋鑰願襯遞鹽鬱 (壓膚醖壓網糧夢衊築網, 顧夢鹽積淵繭膚鏇鹹壓 ~ 鑰窪醖憲願簾遞獵網夢) 更多