Zontivity (vorapaxar) / Merck (MSD) 
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 30 Diseases   1 Trial   1 Trial   342 News 


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  • ||||||||||  Zontivity (vorapaxar) / Merck (MSD), PD98059 / Wayne State University
    Preclinical, Journal:  Antiapoptotic Effect by PAR-1 Antagonist Protects Mouse Liver Against Ischemia-Reperfusion Injury. (Pubmed Central) -  Feb 28, 2020   
    The results of the present study revealed that hepatic IRI induces significant enhancement of PAR-1 expression on SECs, which may be associated with suppression of survival signaling pathways such as ERK 1/2, resulting in severe apoptosis-induced hepatic damage. Thus, the selective PAR-1 antagonist attenuates hepatic IRI through an antiapoptotic effect by the activation of survival-signaling pathways.
  • ||||||||||  Zontivity (vorapaxar) / Merck (MSD)
    Journal:  Prognostic and Practical Validation of Current Definitions of Myocardial Infarction Associated With Percutaneous Coronary Intervention. (Pubmed Central) -  Nov 19, 2019   
    P3
    Suboptimal concordance was observed between ACL and local investigators in identifying patients with PCI complications detected on angiography. (Trial to Assess the Effects of Vorapaxar [SCH 530348; MK-5348] in Preventing Heart Attack and Stroke in Participants With Acute Coronary Syndrome [TRA·CER] [Study P04736]; NCT00527943; EARLY ACS: Early Glycoprotein IIb/IIIa Inhibition in Patients With Non-ST-Segment Elevation Acute Coronary Syndrome [Study P03684AM2]; NCT00089895).
  • ||||||||||  Clinical, Journal:  An update on novel antiplatelets in vascular patients. (Pubmed Central) -  Nov 8, 2019   
    Other novel antiplatelets demonstrate positive results, but further studies focused on vascular patients are necessary. Novel experimental antiplatelets are still in early phases of the clinical and preclinical studies.
  • ||||||||||  The Effects of Antiplatelet Agents on Endocytosis (Hall B, Level 2 (Orange County Convention Center)) -  Nov 7, 2019 - Abstract #ASH2019ASH_1863;    
    In summary, our data show platelets endocytose and release key angiogenic regulators, a process which can be blocked through pre-treatment with various antiplatelet agents. Given the important role of platelets to tumor neovascularization, preventing the endocytosis of pro-angiogenic mediators could represent a novel mechanism that contributes to the inhibitory effects of antiplatelet agents on tumor growth and metastasis.
  • ||||||||||  Zontivity (vorapaxar) / Merck (MSD)
    Plasma Circulating Factors in Recurrent Nephrotic Syndrome Increases Podocyte Motility via Signalling Pathways That Mimic PAR-1 Activation (Exhibit Hall, Walter E. Washington Convention Center) -  Oct 14, 2019 - Abstract #KIDNEYWEEK2019KIDNEY_WEEK_3081;    
    Methods Conditionally immortalised human podocytes (ciPods) were treated with 1) PAR-1 agonist; 2) Relapse and paired-remission plasma from FSGS patients, along with three different PAR-1 inhibitors, Vorapaxar, SCH 79797, and FR17113...Conclusion We reveal a consistent signalling pathway in ‘circulating factor’ SRNS that leads to increased podocyte motility and proteinuria and suggests direct therapeutic targets. Funding Government Support - Non-U.S.
  • ||||||||||  aspirin / Generic Mfg., Zontivity (vorapaxar) / Merck (MSD)
    Journal:  Peri-Procedural Platelet Reactivity in Percutaneous Coronary Intervention. (Pubmed Central) -  Sep 18, 2019   
    However, several issues regarding the anti-platelet treatment such as benefits/risks of anti-platelet therapy pre-treatment and duration, and definite association between speed and potency of various anti-platelet agents and clinical outcomes remain controversial. We believe that a better understanding of peri-PCI platelet reactivity and its relations to outcomes may lead to the development of more effective and safe treatment strategies.
  • ||||||||||  Zontivity (vorapaxar) / Merck (MSD)
    Journal:  SCH79797 improves outcomes in experimental bacterial pneumonia by boosting neutrophil killing and direct antibiotic activity. (Pubmed Central) -  Sep 16, 2019   
    However, the newer-generation PAR1 antagonist, vorapaxar (SCH530348), had no appreciable effect on neutrophil activity or direct bacterial killing, which suggests the effects seen with SCH79797 may be PAR1 independent. In summary, we observed that intrapulmonary treatment with SCH79797 has significant therapeutic effects in a model of E. coli pneumonia that appear to be due, in part, to both neutrophil-stimulating and direct antibacterial effects of SCH79797.
  • ||||||||||  Zontivity (vorapaxar) / Merck (MSD)
    Journal:  Vorapaxar stabilizes permeability of the endothelial barrier under cholesterol stimulation via the AKT/JNK and NF‑κB signaling pathways. (Pubmed Central) -  Aug 30, 2019   
    The present study found that vorapaxar could alleviate the inflammatory response induced by a high concentration of cholesterol stimulation and increase the release of nitric oxide (NO) via the protein kinase B (AKT) signaling pathway and regulation of the intracellular concentration of Ca2+ ([Ca2+]i). We also found that vorapaxar could reduce the damage of DNA caused by cholesterol stimulation and regulate the cell cycle via the AKT/JNK signaling pathway and its downstream molecules glycogen synthase kinase 3β (GSK‑3β) and connexin 43, maintaining the integrity of the endothelial barrier and proliferation of endothelial cells, serving a protective role in endothelial cells.
  • ||||||||||  Zontivity (vorapaxar) / Merck (MSD)
    Journal:  Entry from the lipid bilayer: a possible pathway for inhibition of a peptide G protein-coupled receptor by a lipophilic small molecule. (Pubmed Central) -  Jul 17, 2019   
    These data are consistent with vorapaxar binding to PAR1 via a pathway that passes between TMs 6 and 7 from the lipid bilayer, in agreement with the most consistent pathway observed by molecular dynamics. While some evidence exists for ligand entry into rhodopsin and lipid-activated GPCRs from the cell membrane, our study provides the first such evidence for a peptide-activated GPCR and suggests that metastable intermediates along drug binding and dissociation pathways can be stabilized by specific interactions between lipids and the ligand.
  • ||||||||||  Brilinta (ticagrelor) / AstraZeneca, Zontivity (vorapaxar) / Merck (MSD), Effient (prasugrel) / Eli Lilly, Daiichi Sankyo
    Journal:  Oral antiplatelet agents in cardiovascular disease. (Pubmed Central) -  Jul 11, 2019   
    This review article summarizes the current evidence on oral antiplatelet agents in cardiovascular disease. Keywords: Aspirin, clopidogrel, prasugrel, ticagrelor, vorapaxar, cardiovascular disease.
  • ||||||||||  Brilinta (ticagrelor) / AstraZeneca, Zontivity (vorapaxar) / Merck (MSD), Effient (prasugrel) / Eli Lilly, Daiichi Sankyo
    Journal:  Oral antiplatelets in primary and secondary prevention of myocardial infarction: a review. (Pubmed Central) -  Jun 23, 2019   
    In this review paper, we have summarized the continuing controversy about the use of oral antiplatelet therapy and their role in primary as well as secondary prevention of MI by describing results from major clinical trials. The safety and the efficacy of the above medications have been reviewed and described in this paper.
  • ||||||||||  Brilinta (ticagrelor) / AstraZeneca, Zontivity (vorapaxar) / Merck (MSD), Effient (prasugrel) / Eli Lilly, Daiichi Sankyo
    Review, Journal:  Oral Antiplatelet Therapy for Secondary Prevention of Acute Coronary Syndrome. (Pubmed Central) -  May 29, 2019   
    This paper reviews current evidence and guidelines for oral antiplatelet therapy for secondary prevention following ACS, with respect to decreased risk of ischemic events versus bleeding risk according to individual patient characteristics and risk factors. Specifically, data are reviewed from clinical studies of clopidogrel, prasugrel, ticagrelor and vorapaxar, as well as the results of systematic reviews and meta-analyses looking at the benefits and risks of oral antiplatelet therapy, and the relative merits of shorter versus longer duration of dual antiplatelet therapy, in different patient groups.
  • ||||||||||  fondaparinux / generics
    Clinical, Review, Journal:  Clinical effects with inhibition of multiple coagulative pathways in patients admitted for acute coronary syndrome. (Pubmed Central) -  May 24, 2019   
    Numerous antithrombotic cocktails including oral anticoagulants with or without aspirin have been tested in large clinical trials with the goal of further reduction of ischemia and bleeding risk. The aim of this review is to discuss clinical outcomes resulting from inhibition of multiple coagulative pathways in patients with ACS in light of evidence from large randomized controlled clinical trials.
  • ||||||||||  Review, Journal:  Diabetes and antiplatelet therapy: from bench to bedside. (Pubmed Central) -  Dec 1, 2018   
    Oral platelet P2Y receptor inhibitors with enhanced potency, such as prasugrel and ticagrelor, as well as antiplatelet therapies such as vorapaxar inhibiting the thrombin-mediated platelet signaling pathway, constitute treatment opportunities for patients with DM and have shown to be associated with a greater reduction in ischemic recurrences, albeit at the cost of more bleeding. This article reviews currently available antiplatelet agents and delivers an update on the advances and drawbacks of these agents used for secondary prevention in DM patients experiencing an ACS or undergoing PCI.
  • ||||||||||  Zontivity (vorapaxar) / Merck (MSD)
    Trial primary completion date:  OPTIMUS-5: Vorapaxar as an Add-On Antiplatelet Therapy in Patients With and Without Diabetes Mellitus (clinicaltrials.gov) -  Nov 28, 2018   
    P4,  N=64, Recruiting, 
    This article reviews currently available antiplatelet agents and delivers an update on the advances and drawbacks of these agents used for secondary prevention in DM patients experiencing an ACS or undergoing PCI. Trial primary completion date: Sep 2018 --> Dec 2018
  • ||||||||||  Clinical, Review, Journal:  Antithrombotic therapy for patients with STEMI undergoing primary PCI. (Pubmed Central) -  Aug 31, 2018   
    Prasugrel and ticagrelor provide a more prompt, potent, and predictable antiplatelet effect compared with clopidogrel, which translates into better clinical outcomes...Thrombin has an important role, suggesting the need for strategies directly targeting circulating thrombin or other factors of the coagulation cascade, such as oral anticoagulants (rivaroxaban), and the thrombin receptor on the platelet membrane (vorapaxar). In this Review, we provide an overview of currently available antithrombotic therapies used in patients with STEMI undergoing PPCI, results from pivotal clinical trials and their implications for guidelines, as well as recommendations for clinical practice.
  • ||||||||||  Zontivity (vorapaxar) / Merck (MSD)
    Trial completion, Trial completion date, Trial primary completion date:  Vorapaxar on Thrombin Generation and Coagulability (clinicaltrials.gov) -  Aug 22, 2018   
    P4,  N=90, Completed, 
    In this Review, we provide an overview of currently available antithrombotic therapies used in patients with STEMI undergoing PPCI, results from pivotal clinical trials and their implications for guidelines, as well as recommendations for clinical practice. Recruiting --> Completed | Trial completion date: Mar 2018 --> Aug 2018 | Trial primary completion date: Jan 2018 --> Jul 2018
  • ||||||||||  Zontivity (vorapaxar) / Merck (MSD)
    Journal:  Role for Thrombin Receptor Antagonism With Vorapaxar in Secondary Prevention of Atherothrombotic Events: From Bench to Bedside. (Pubmed Central) -  Jul 23, 2018   
    Vorapaxar is a direct inhibitor of PAR-1 and the only agent of this class approved for the prevention of recurrent ischemic events in patients with prior myocardial infarction or peripheral artery disease. In the present manuscript, we present a review of the pathophysiologic role of thrombin on thrombotic complications, the impact of vorapaxar on outcomes, including the most recent updates deriving from clinical trials, as well as future perspectives in the field.
  • ||||||||||  Zontivity (vorapaxar) / Merck (MSD)
    Trial completion date, Trial primary completion date:  OPTIMUS-5: Vorapaxar as an Add-On Antiplatelet Therapy in Patients With and Without Diabetes Mellitus (clinicaltrials.gov) -  Mar 31, 2018   
    P4,  N=64, Recruiting, 
    In the present manuscript, we present a review of the pathophysiologic role of thrombin on thrombotic complications, the impact of vorapaxar on outcomes, including the most recent updates deriving from clinical trials, as well as future perspectives in the field. Trial completion date: Jun 2018 --> Dec 2018 | Trial primary completion date: Mar 2018 --> Sep 2018
  • ||||||||||  Zontivity (vorapaxar) / Merck (MSD)
    Enrollment change, Trial withdrawal, Trial primary completion date:  Vorapaxar and Lower Extremity Bypass Grafts (clinicaltrials.gov) -  Jan 25, 2018   
    P4,  N=0, Withdrawn, 
    Trial primary completion date: Jul 2017 --> Jul 2019 N=100 --> 0 | Not yet recruiting --> Withdrawn | Trial primary completion date: Jul 2018 --> Jan 2018