A Phase 3 Prospective, Blinded, Randomized, Placebo Controlled, International Multicenter Study to Assess the Safety and Efficacy of a Single SQ Injection of Zalunfiban in Subjects With ST-elevation MI in the Pre-hospital Setting

This is a Phase 3 prospective, blinded, randomized, placebo controlled, international multicenter study. Subjects with STEMI will be enrolled in the ambulance if they meet all eligibility criteria. These subjects will be evaluated by (para)medics who transport the subjects to the participating hospitals in Europe and North America. Hospitals and ambulance services with experience in ambulance studies will be selected. Each subject will receive a single subcutaneous injection containing either Disaggpro(tm) zalunfiban Dose 1 (0.110 mg/kg) or Disaggpro(tm) zalunfiban Dose 2 (0.130 mg/kg) or placebo

开始日期2021-04-24

申办/合作机构

CeleCor Therapeutics, Inc.

NCT04284995

/ Completed临床2期

A Phase 2 Open Label Study to Assess the PK and PD Properties of a Single Subcutaneous Injection of RUC-4 in Patients With a ST-elevation Myocardial Infarction Presenting to the Cardiac Catheterization Lab With Planned Primary Coronary Angioplasty

RUC-4 is a novel, promising and fast acting (5-15 minutes) αIIbβ3 receptor antagonist with a high-grade inhibition of platelet aggregation (≥80%) shortly after subcutaneous administration. This study is designed to extend the findings in CEL-01 to patients with ST-elevation myocardial Infarction (STEMI) presenting to the cardiac catheterization laboratory with planned coronary angioplasty.

开始日期2020-06-02

申办/合作机构

CeleCor Therapeutics, Inc.

[+2]

NCT03844191

/ Completed临床1期

A Randomized Phase 1 Dose-Escalation Study in Healthy Volunteers and Subjects on Aspirin With Stable Coronary Artery Disease to Assess the Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of Subcutaneous RUC-4

This study is designed to assess tolerability of the weight-adjusted dose of RUC-4 (mg/kg) required to achieve 80% or more inhibition of the initial slope of platelet aggregation to 20 µM ADP by Light Transmission Aggregometry (LTA) within 15 minutes of SC administration of RUC-4 with return toward baseline values within 4 hours in healthy volunteers and subjects on aspirin with stable coronary artery disease (CAD). In the Dose Expansion Part, VerifyNow PRUTest will be used to measure platelet aggregation in addition to LTA.
Since the goal of RUC-4 therapy is to achieve maximal antiplatelet therapy as rapidly as possible, first the tolerability of the weight-adjusted dose (mg/kg) that inhibits ADP-induced platelet aggregation by 80% or more in 5 of 6 healthy volunteers will be identified. A similar dose escalation will be subsequently performed in subjects with CAD who are taking aspirin. To facilitate administration using a single weight-adjusted (mg/kg) dose for a defined group of subjects weighing between 55 and 120 kg, the study will also evaluate the safety and biologic effect on platelet aggregation of the weight adjusted (mg/kg) dose when administered to subjects with weights at either end of this range.

开始日期2019-02-18

申办/合作机构

CeleCor Therapeutics, Inc.

[+3]

100 项与 Zalunfiban 相关的临床结果

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100 项与 Zalunfiban 相关的转化医学

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100 项与 Zalunfiban 相关的专利（医药）

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项与 Zalunfiban 相关的文献（医药）

2024-11-01·Journal of Computational Biophysics and Chemistry

Molecular Docking, Quantum Mechanics and Molecular Dynamics Simulation of Anti-CAD Drugs Against High-Risk Xanthine Dehydrogenase Variants Associated with Oxidative Stress Pathways

作者: Sudhan, M. ; Ahmed, Shiek S. S. J. ; Emran, Talha Bin ; Attia, Sabry M. ; Ahmad, Sheikh F. ; Janakiraman, V.

Xanthine dehydrogenase (XDH) contributes significantly to generating reactive oxygen species in coronary artery disease (CAD). XDH has been proposed as a therapeutic target, but its genetic variants could affect protein structure and drug response. We aimed to assess protein structure modification occur due to genetic variants and to screen 215 CAD drugs for their utility in personalized CAD treatment against the XDH variants. A series of computational methods were implemented to identify pathogenic variants that cause XDH structure instability localized at the con served regions contributing to functional significance. Then, the XDH structures with the pathogenic variants were modeled using two different approaches to select the best models for docking with the CAD drugs. Finally, the stability of the docked complexes and their ability to transfer electrons were evaluated using molecular dynamics (MD) simulations and quantum mechanics/molecular mechanics (QM/MM) calculation. Among 751 variants examined; R149C and Q919R showed high pathogenicity, localized in conserved regions could alter protein structure and function. Further, docking of CAD drugs against XDH (native, R149C and Q919R) showed vericiguat with higher affinity, ranging from −7.95 kcal/mol to −10.41 kcal/mol, than the well-known XDH inhibitor (febuxostat, −5.73 kcal/mol to −8.35 kcal/mol). This indicates that vericiguat will be effective in CAD treatment, regardless of the XDH variants. Additionally, MD simulation and QM/MM confirmed vericiguat stability and electron transfer ability to form hydrogen bonds with the XDH protein. In conclusion, vericiguat will be beneficial for the personalized treatment of CAD by inhibiting XDH variants. Additional clinical studies are necessary to confirm our findings.

2023-12-19·Journal of the American Heart Association

Critical Analysis of Thrombocytopenia Associated With Glycoprotein IIb/IIIa Inhibitors and Potential Role of Zalunfiban, a Novel Small Molecule Glycoprotein Inhibitor, in Understanding the Mechanism(s)

Review

作者: Rikken, Sem A. O. F. ; Kereiakes, Dean J. ; Coller, Barry S. ; van 't Hof, Arnoud W. J. ; ten Berg, Jurriën M.

Thrombocytopenia is a rare but serious complication of the intravenous glycoprotein IIb/IIIa (GPIIb/IIIa; integrin αIIbβ3) receptor inhibitors (GPIs), abciximab, eptifibatide, and tirofiban. The thrombocytopenia ranges from mild (50 000–100 000 platelets/μL), to severe (20 000 to <50 000/μL), to profound (<20 000/μL). Profound thrombocytopenia appears to occur in <1% of patients receiving their first course of therapy. Thrombocytopenia can be either acute (<24 hours) or delayed (up to ~14 days). Both hemorrhagic and thrombotic complications have been reported in association with thrombocytopenia. Diagnosis requires exclusion of pseudothrombocytopenia and heparin‐induced thrombocytopenia. Therapy based on the severity of thrombocytopenia and symptoms may include drug withdrawals and treatment with steroids, intravenous IgG, and platelet transfusions. Abciximab‐associated thrombocytopenia is most common and due to either preformed antibodies or antibodies induced in response to abciximab (delayed). Readministration of abciximab is associated with increased risk of thrombocytopenia. Evidence also supports an immune basis for thrombocytopenia associated with the 2 small molecule GPIs. The latter bind αIIbβ3 like the natural ligands and thus induce the receptor to undergo major conformational changes that potentially create neoepitopes. Thrombocytopenia associated with these drugs is also immune‐mediated, with antibodies recognizing the αIIbβ3 receptor only in the presence of the drug. It is unclear whether the antibody binding depends on the conformational change and whether the drug contributes directly to the epitope. Zalunfiban, a second‐generation subcutaneous small molecule GPI, does not induce the conformational changes; therefore, data from studies of zalunfiban will provide information on the contribution of the conformational changes to the development of GPI‐associated thrombocytopenia.

2023-11-01·Journal of thrombosis and thrombolysis

Comparison of the effects of the GPIIb-IIIa antagonist Zalunfiban and the P2Y12 antagonist Selatogrel on Platelet Aggregation.

Article

作者: Rikken, A O F Sem ; van 't Hof, Arnoud W J ; Ten Berg, Jurriën M ; Gibson, C Michael ; Jennings, Lisa K ; Granger, Christopher B ; Curry, Benjamin J

Understanding the pharmacodynamic effects of platelet inhibitors is standard for developing more effective antithrombotic therapies. An example is the antithrombotic treatment of acute coronary syndrome (ACS), in particular ST-elevated myocardial infarction (STEMI) patients who are in need for rapid acting strong antithrombotic therapy despite the use of aspirin and oral P2Y12-inhibitors. In this study, we evaluated two injectable platelet inhibitors under clinical development (the P2Y12 antagonist selatogrel and the GPIIb-IIIa antagonist zalunfiban) that may be amenable to pre-hospital treatment of STEMI patients. Platelet reactivity was assessed at inhibitor concentrations that represent clinically relevant levels of platelet inhibition (IC20-50%, 1/2Cmax, and Cmax). Light transmission aggregometry (LTA), was used to evaluate the initial rate of aggregation (primary slope, PS) and maximal aggregation (MA). Both adenosine diphosphate (ADP) and thrombin receptor agonist peptide (TRAP) were used as agonists. Zalunfiban demonstrated similar inhibition of platelet aggregation when blood was collected in PPACK or TSC, whereas selatogrel demonstrated greater inhibition in PPACK. In this study, using PPACK anticoagulant, selatogrel and zalunfiban affected PS in response to ADP equivalently at all drug concentrations tested. In contrast, zalunfiban had significantly greater potency at its Cmax concentration compared to selatogrel using TRAP as agonist. Upon evaluation of MA responses at lower doses, selatogrel had greater inhibition of MA in response to ADP than zalunfiban; however, at concentrations that represent Cmax, the drugs were equivalent. Zalunfiban also had greater inhibition of MA in response to TRAP at the Cmax dose. These data suggest that zalunfiban may provide greater protection in reducing thrombus formation than selatogrel, especially since thrombin is an early, key primary agonist in the pathophysiology of thrombotic events.

项与 Zalunfiban 相关的新闻（医药）

2025-09-23

·PRNewswire

PHASE 3 STUDY OF NOVEL ANTI-PLATELET DRUG FOR HEART ATTACK REPORTS POSITIVE TOPLINE RESULTS

DEL MAR, Calif., Sept. 23, 2025 /PRNewswire/ -- CeleCor Therapeutics' multinational Phase 3 clinical trial of its investigational heart-attack drug Disaggpro™ (zalunfiban) has shown positive primary efficacy and primary safety outcomes. The full results from the CeleBrate study will be released on Nov. 10 as part of the late-breaking sessions at the American Heart Association Scientific Sessions in New Orleans. At least 50% of heart-attack deaths occur before the patient reaches the hospital. Even as in-hospital treatment for heart attacks has greatly improved, aspirin is the only antiplatelet treatment routinely used in the U.S. for heart attacks before patients can get to the hospital. Disaggpro was designed to change that, as it can be administered in several pre-hospital settings for rapid treatment of ST-segment elevation (STEMI) heart attacks. The priority in treating STEMI heart attacks is opening the coronary artery as soon as possible after the onset of symptoms to prevent death or irreversible heart damage. About 40% of heart-attack patients have STEMIs, the most severe form of heart attack, in which blood flow to a portion of the heart is almost always cut off by a blood clot. Disaggpro is a next-generation investigational GPIIb/IIIa inhibitor that was specifically designed to administer by subcutaneous injection using an auto-injector, allowing a full dose to be contained in a volume of less than 1 milliliter (less than ¼ teaspoon). It reaches maximal effect within 15 minutes and has a pharmacokinetic half-life of about one hour. About the CeleBrate study CeleBrate was a pivotal Phase 3 prospective, double-blinded, randomized, placebo-controlled trial designed to assess the safety and efficacy of a single subcutaneous injection of Disaggpro in STEMI patients in the pre-hospital setting. It enrolled 2,467 patients at 45 sites in the United States, Canada, Mexico and Europe. Eligible STEMI patients were enrolled at home, in the ambulance or in a hospital emergency department. More information about the study can be found here. BUSINESS CONTACT: Rob Hillman, [email protected] MEDIA CONTACT: Lisa Guiterman, [email protected] SOURCE CeleCor Therapeutics, Inc. WANT YOUR COMPANY'S NEWS FEATURED ON PRNEWSWIRE.COM? 440k+ Newsrooms & Influencers 9k+ Digital Media Outlets 270k+ Journalists Opted In GET STARTED

临床3期AHA会议临床结果

100 项与 Zalunfiban 相关的药物交易

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研发状态

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
ST段抬高心肌梗死	临床3期	美国	CeleCor Therapeutics, Inc.	2021-04-24
ST段抬高心肌梗死	临床3期	加拿大	CeleCor Therapeutics, Inc.	2021-04-24
ST段抬高心肌梗死	临床3期	捷克	CeleCor Therapeutics, Inc.	2021-04-24
ST段抬高心肌梗死	临床3期	法国	CeleCor Therapeutics, Inc.	2021-04-24
ST段抬高心肌梗死	临床3期	匈牙利	CeleCor Therapeutics, Inc.	2021-04-24
ST段抬高心肌梗死	临床3期	墨西哥	CeleCor Therapeutics, Inc.	2021-04-24
ST段抬高心肌梗死	临床3期	荷兰	CeleCor Therapeutics, Inc.	2021-04-24
ST段抬高心肌梗死	临床3期	罗马尼亚	CeleCor Therapeutics, Inc.	2021-04-24
冠状动脉疾病	临床2期	荷兰	CeleCor Therapeutics, Inc.	2020-06-02
冠心病	临床1期	美国	CeleCor Therapeutics, Inc.	2019-02-18

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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


NCT04825743 (CeleBrate, PRNewswire) 人工标引	临床3期	ST段抬高心肌梗死	2,467	zalunfiban	簾鏇鏇鹽獵製壓鹽鹽糧(艱膚築壓範衊鏇餘鹹夢) = positive 觸繭構糧鬱顧簾積觸餘 (淵夢製夢鬱顧構獵醖構 ) 更多	积极	2025-09-23
NCT04825743 (CeleBrate, PRNewswire) 人工标引	临床3期	ST段抬高心肌梗死	2,467	Placebo		积极	2025-09-23
NCT04825743 (CELEBRATE, ESC2022)	临床2期	ST段抬高心肌梗死	27	Zalunfiban	繭壓糧醖蓋壓繭餘壓糧(齋膚鬱遞網遞鏇齋鏇築) = 壓餘遞鹹淵獵蓋襯壓淵構鑰遞鬱餘淵憲築選膚 (選窪糧糧膚獵齋鹹網壓 )	-	2022-03-18
ISTH2021	临床1期	ST段抬高心肌梗死	-	RUC-4 (Zalunfiban)	齋選觸選獵廠蓋淵夢顧(遞憲醖鹽廠願鬱築窪築) = 願鏇廠網獵積願範艱繭艱鹽窪鑰獵觸鏇願鬱襯 (膚壓膚製鹹製繭糧膚壓 )	-	2021-07-17