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- Zontivity (vorapaxar) / Merck (MSD)
PAR1 Inhibition Vorapaxar as a Potential Therapeutic Approach in Chronic Thromboembolic Pulmonary Hypertension (PS-31) - May 31, 2024 - Abstract #ERS2024ERS_5149;
- Zontivity (vorapaxar) / Merck (MSD)
Development and optimisation of a novel 9-parameter flow cytometry panel for human platelet phenotyping (Exhibition Hall) - May 17, 2024 - Abstract #ISTH2024ISTH_1414;
The assay performed equally well in WB and washed platelets. Focusing on WB, we found the assay detected differential changes in receptor expression of all 9 receptors in response to multiple agonists.
- Zontivity (vorapaxar) / Merck (MSD)
The effect of clinically used antiplatelets drugs and flavonoid metabolite 4-methylcatechol in diabetes mellitus type I patients and generally healthy volunteers. (Exhibition Hall) - May 17, 2024 - Abstract #ISTH2024ISTH_1401;
Additional analysis confirmed that lower aggregation responses were observed to 2 aggregation triggers in plasma samples with glycemia over 7 mM. In contrast to approved drugs, the effect of 4-MC was higher in DM1 patients than in healthy controls.
- Zontivity (vorapaxar) / Merck (MSD)
PAR1 Inhibition Vorapaxar as a Potential Therapeutic Approach in Chronic Thromboembolic Pulmonary Hypertension: Experimental Insights and Implications (208 A-D) - May 17, 2024 - Abstract #ISTH2024ISTH_695;
In the murine IVC model, we found that thrombus mass and volume gradually decreased over time (N = 10), consistent with thrombus dissolution. Furthermore, after administering vorapaxar for 7 days, we observed a significant reduction in thrombus mass and volume (P = 0.002, N = 10), and the vorapaxar group exhibited faster dissolution of thrombi over time compared to the control group.
- | Inrebic (fedratinib) / BMS, Zontivity (vorapaxar) / Merck (MSD), Braftovi (encorafenib) / Ono Pharma, Pierre Fabre, Pfizer
Journal: Mass Spectrometry-Based Proteomics Analysis Unveils PTPRS Inhibits Proliferation and Inflammatory Response of Keratinocytes in Psoriasis. (Pubmed Central) - May 13, 2024
PTPRS expression was decreased in PsO, and PTPRS negatively regulated PsO. PTPRS may be involved in PsO pathogenesis through the inhibition of keratinocyte proliferation and inflammatory responses and is a potential treatment target for PsO.
- | Zontivity (vorapaxar) / Merck (MSD)
Journal: Correlations among different platelet aggregation pathways in a group of healthy volunteers. (Pubmed Central) - Apr 15, 2024
Our results indicate that a response to one inducer can predict the response for other triggers or even to an antiplatelet drug. These data are useful for future testing but should be also confirmed in patients.
- || Zontivity (vorapaxar) / Merck (MSD)
Review, Journal: Thrombin as target for prevention of recurrent events after acute coronary syndromes. (Pubmed Central) - Mar 4, 2024
We explored the evidence supporting thrombin generation in the pathophysiology of recurrent events post-ACS and the role of thrombin as a viable therapeutic target. One specific target is factor XI inhibition, which is involved in thrombin generation, but may also allow for the preservation of normal hemostasis.
- | Zontivity (vorapaxar) / Merck (MSD)
Journal, Benefit-risk assessment: Quantifying the Benefit-Risk Trade-Off for Individual Patients in a Clinical Trial: Principles and Anti-Thrombotic Case Study. (Pubmed Central) - Jan 28, 2024
One specific target is factor XI inhibition, which is involved in thrombin generation, but may also allow for the preservation of normal hemostasis. While overall RCT of treatment benefit versus risk are valuable, models determining each individual patient's estimated absolute benefit and risk provides more useful insight regarding patient-specific benefit-risk trade-off, to better enable personalized therapeutic decision-making.
- | Zontivity (vorapaxar) / Merck (MSD)
Journal: Tubulovascular protection from protease-activated receptor-1 depletion during AKI-to-CKD transition. (Pubmed Central) - Oct 23, 2023
While overall RCT of treatment benefit versus risk are valuable, models determining each individual patient's estimated absolute benefit and risk provides more useful insight regarding patient-specific benefit-risk trade-off, to better enable personalized therapeutic decision-making. Our findings elucidate a detrimental role of PAR-1 in vascular dysfunction and profibrotic responses upon tissue injury during AKI-to-CKD transition and provide an attractive therapeutic strategy for post-injury repair in AKI.
- | Zontivity (vorapaxar) / Merck (MSD), Verzenio (abemaciclib) / Eli Lilly
Journal: Novel chemical scaffold as potential drug against Leishmania donovani: Integrated computational and experimental approaches. (Pubmed Central) - Aug 11, 2023
Our findings elucidate a detrimental role of PAR-1 in vascular dysfunction and profibrotic responses upon tissue injury during AKI-to-CKD transition and provide an attractive therapeutic strategy for post-injury repair in AKI. The three compounds, Abemaciclib, Bazedoxifene, and Vorapaxar, had shown effective anti-leishmanial activities with IC values of 0.92?
- | Zontivity (vorapaxar) / Merck (MSD)
Journal: Synthesis and Biological Evaluation of Resveratrol Methoxy Derivatives. (Pubmed Central) - Aug 2, 2023
In terms of their anti-tumor activity, 3-MRESV exhibited the highest potency in PC-3 cells, while 3,4'-DMRESV and TMRESV showed the greatest efficacy in HCT116 cells. In conclusion, methoxy derivatives of resveratrol possess similar or improved anti-platelet and anti-cancer effects, thereby holding potential as bioactive compounds in various pathological conditions.
- || Zontivity (vorapaxar) / Merck (MSD)
Review, Journal: Dual Antiplatelet Therapy: A Concise Review for Clinicians. (Pubmed Central) - Jul 29, 2023
Carotid artery disease patients with transient ischemic attack or stroke benefit from antiplatelet therapy and combining ASA and clopidogrel is more effective than ASA alone...The use of combination therapies may provide added benefits but should be weighed against the risk of bleeding. Further research and clinical trials are needed to optimize antiplatelet treatment in different patient populations and clinical scenarios.
- | Zontivity (vorapaxar) / Merck (MSD)
Journal: Antagonizing the irreversible thrombomodulin-initiated proteolytic signaling alleviates age-related liver fibrosis via senescent cell killing. (Pubmed Central) - Jul 3, 2023
Therapeutically, THBD signaling depletion or inhibition using vorapaxar, an FDA-approved drug, effectively ablates senescent cells and restores tissue homeostasis in liver fibrosis models. Collectively, these results uncover proteolytic THBD signaling as a conserved pro-survival pathway essential for senescent cell viability, thus providing a pharmacologically exploitable senolytic target for senescence-associated diseases.
- Zontivity (vorapaxar) / Merck (MSD)
GDF-15 is associated with worse ischemic and bleeding outcomes in the acute phase and during follow-up in patients with acute coronary syndrome: insights from the TRACER trial (Station 5) - May 13, 2023 - Abstract #ESC2023ESC_750;
Methods Venous blood samples were obtained at the index event in 6800 patients and again after one month in 5313 patients with non-ST-segment elevation ACS (NSTE-ACS) randomized to vorapaxar vs placebo on top of dual antiplatelet treatment in the TRACER study...Conclusions In patients with NSTE-ACS levels of GDF-15 are independently associated with CV death, MI or ischemic stroke and non-procedural bleeding and contribute prognostic information both at the index event and after one month. Levels of GDF-15 remain stable over time and provide similar prognostic information in the acute and follow-up setting.
- | Zontivity (vorapaxar) / Merck (MSD)
Journal: The Impact of Convertase Subtilisin/Kexin Type 9 Monoclonal Antibodies with and without Apheresis on Platelet Aggregation in Familial Hypercholesterolemia. (Pubmed Central) - May 2, 2023
Levels of GDF-15 remain stable over time and provide similar prognostic information in the acute and follow-up setting. This study showed for the first time the suitability of PCSK9ab treatment for reduction of platelet reactivity in FH patients.
- || Zontivity (vorapaxar) / Merck (MSD)
If we can translate findings from the CAD space to the HF space, therapies that don’t have a clear “sweet spot” rarely get adopted (eg, vorapaxar). (Twitter) - Mar 20, 2023
- ||| rivaroxaban / Generic mfg., Zontivity (vorapaxar) / Merck (MSD)
More on anti-thrombo 🩸Too bad vorapaxar went away 🩸arterial thrombosis: platelet activation + thrombus (dual pathway inhibition) 🩸Read Compass! Not just #PAD, but CAD (90% had it)=24% RRR on rivaroxaban👊🏾 🩸Voyager: early separation (3m), ongoing divergence. #ACC23 (Twitter) - Mar 7, 2023
- | Folotyn (pralatrexate) / Aurobindo, Zontivity (vorapaxar) / Merck (MSD), Victrelis (boceprevir) / Roche, Merck (MSD)
Journal: Bias-force guided simulations combined with experimental validations towards GPR17 modulators identification. (Pubmed Central) - Mar 2, 2023
Small interference of the RNA (siRNA)- silenced the GPR17 to further validate the targeted binding of Sacubitril with GPR17. In the current investigation, we have identified new repurposable GPR17 specific drugs which are likely to increase the opportunity to treat orphan deadly diseases.
- | Zontivity (vorapaxar) / Merck (MSD)
Preclinical, Journal: Vorapaxar proven to be a promising candidate for pulmonary fibrosis by intervening in the PAR1/JAK2/STAT1/3 signaling pathway-an experimental in vitro and vivo study. (Pubmed Central) - Feb 27, 2023
(TGF?) receptor II and inhibits the TGF?/Smad signaling pathway. In conclusion, Vorapaxar inhibits the activation of pulmonary fibroblasts induced by thrombin by targeting protease activated receptor 1 and alleviates BLM-induced pulmonary fibrosis in mice.
- | Zontivity (vorapaxar) / Merck (MSD)
Biomarker, Journal: The Effect of Protease-Activated Receptor-1 (PAR-1) Inhibition on Endothelial-Related Biomarkers in Patients with Coronary Artery Disease. (Pubmed Central) - Jan 3, 2023
In conclusion, Vorapaxar inhibits the activation of pulmonary fibroblasts induced by thrombin by targeting protease activated receptor 1 and alleviates BLM-induced pulmonary fibrosis in mice. Significant endothelial biomarker changes during PAR-1 inhibition were observed in post-MI and NSTEMI patients.
- ||| Zontivity (vorapaxar) / Merck (MSD)
Clinical: When a trial ‘wins’ on a PEP, FDA has used a favorable subgroup to optimize benefit-risk (vorapaxar example driven by favorable safety subgroup). In this case there is a favorable efficacy subgroup (low EF). Challenge with galactic HF is what constitutes confirmatory evidence. (Twitter) - Dec 15, 2022
- || I wish we had better data on this. I think I would go with a different drug. Add in plavix or cilistazol or vorapaxar to aspirin/xarelto. Or just add them all! (Twitter) - Nov 5, 2022
- Zontivity (vorapaxar) / Merck (MSD)
Protease Activated Receptor-1 (PAR-1) Inhibition By Parmodulin 2, but Not Vorapaxar, Protects Sickle Cell Mice from Heme-Induced Acute Chest Syndrome (ENMCC - Hall D) - Nov 4, 2022 - Abstract #ASH2022ASH_1862;
Vorapaxar, an irreversible antagonist of PAR-1 which blocks all PAR-1 signaling pathways, did not protect SS mice against heme-induced ACS. In contrast, PM2 completely alleviated heme-induced lung injury and death in SS mice.
- | Zontivity (vorapaxar) / Merck (MSD)
Biomarker, Journal: Biomarker-Based Prediction of Recurrent Ischemic Events in Patients With Acute Coronary Syndromes. (Pubmed Central) - Nov 3, 2022
P3
The ABC-ACS ischemia score showed good calibration and discrimination and might be useful for risk prediction and decision support in patients with ACS. (A Comparison of Ticagrelor [AZD6140] and Clopidogrel in Patients With Acute Coronary Syndrome [PLATO]; NCT00391872; Trial to Assess the Effects of Vorapaxar [SCH 530348; MK-5348] in Preventing Heart Attack and Stroke in Participants With Acute Coronary Syndrome [TRACER]; NCT00527943).
- Zontivity (vorapaxar) / Merck (MSD)
TARGETING SENESCENT HEPATOCYTES USING THETHBD-PAR1 INHIBITOR VORAPAXAR AMELIORATES NAFLD PROGRESSION (Room 145) - Oct 23, 2022 - Abstract #AASLD2022AASLD_455;
Inhibiting THBD-PAR1 signaling with Vorapaxar suppresses hepatocyte senescence and liver fibrosis in mouse models of NAFLD. The THBD-PAR1 axis may be a new therapeutic target in NAFLD.
- Zontivity (vorapaxar) / Merck (MSD)
Tubulovascular Protection of Protease-Activated Receptor-1 Deficiency During AKI-to-CKD Transition (Exhibit Hall, Orange County Convention Center, West Building) - Oct 13, 2022 - Abstract #KIDNEYWEEK2022KIDNEY_WEEK_3366;
Importantly, vascular regenerative capacity was higher in mice treated with vorapaxar during AKI, particularly showing significant increase of VEGF in full treatment and VEGFR2 in pre-treatment with vorapaxar. Conclusion Our findings elucidate a detrimental role of PAR-1 in vascular dysfunction and profibrotic responses upon tissue injury during AKI-to-CKD transition and provide an attractive therapeutic strategy for post-injury repair in AKI.
- || Zontivity (vorapaxar) / Merck (MSD)
Review, Journal: Sex-Related Differences in Platelet Aggregation: A Literature Review Supplemented with Local Data from a Group of Generally Healthy Individuals. (Pubmed Central) - Oct 8, 2022
The aggregatory responses to AA and TRAP decreased with age in both sexes, while responses to ADP, U-46619, and PAF were affected by age only in women. In conclusion, more studies are needed to decipher the biological importance of sex-related differences in platelet aggregation in part to enable personalized antiplatelet treatment.
- | Zontivity (vorapaxar) / Merck (MSD)
Journal: Hemostatic Effect of 20(S)-Panaxadiol by Induced Platelet Aggregation Depending on Calcium Signaling Pathway. (Pubmed Central) - Oct 7, 2022
Besides, PD increased the phosphorylation of phosphoinositide 3-kinase/protein kinase B/glycogen synthase kinase 3β (PI3K/Akt/GSK3β) of human platelets. PD is an important hemostatic ingredient in Panax notoginseng, which induced platelet aggregation by affecting the calcium signaling and activating the PI3K/Akt/GSK3β signaling pathway.
- | Uptravi (selexipag) / J&J, Nippon Shinyaku, Zontivity (vorapaxar) / Merck (MSD), Tekturna (aliskiren) / PDL
Journal: Molormer: a lightweight self-attention-based method focused on spatial structure of molecular graph for drug-drug interactions prediction. (Pubmed Central) - Sep 29, 2022
In the case study section, we used Molormer to make predictions of new interactions for the drugs Aliskiren, Selexipag and Vorapaxar and validated parts of the predictions. Code and models are available at https://github.com/IsXudongZhang/Molormer.
- ||| Zontivity (vorapaxar) / Merck (MSD)
Monotherapy: Vorapaxar monotherapy was perhaps a missed opportunity in this regard? (Twitter) - Sep 2, 2022
- || Zontivity (vorapaxar) / Merck (MSD)
Review, Journal: Improving Outcomes in Cardiovascular Diseases: A Review on Vorapaxar. (Pubmed Central) - Aug 13, 2022
Another recently published VORA-PRATIC (Vorapaxar in Patients with Prior Myocardial Infarction Treated with prasugrel and ticagrelor) study showed that among post-MI patients treated with potent P2Y12 inhibitors (prasugrel or ticagrelor), vorapaxar reduced platelet-driven global thrombogenicity, an effect that persisted, albeit attenuated, in the absence of aspirin. The current review summarizes an up to date literature on pharmacokinetics, pharmacodynamics, and clinical efficacy of vorapaxar and proposes future directions of research.
- Sex Differences in Protein Biomarkers and Measures of Fat Distribution (Zone 3, Science and Technology Hall, Level 200) - Aug 11, 2022 - Abstract #AHA2022AHA_3589;
The current review summarizes an up to date literature on pharmacokinetics, pharmacodynamics, and clinical efficacy of vorapaxar and proposes future directions of research. Abstract is embargoed at this time.
- | Zontivity (vorapaxar) / Merck (MSD)
Journal: Epidemiology of heart failure hospitalization in patients with stable atherothrombotic disease: Insights from the TRA 2°P-TIMI 50 trial. (Pubmed Central) - Aug 6, 2022
Abstract is embargoed at this time. In patients with stable atherosclerosis, prior HF, age, T2DM, polyvascular disease, CKD, BMI, prior MI, and hypertension are important predictors of HHF risk.
- || Zontivity (vorapaxar) / Merck (MSD)
Vorapaxar (Twitter) - Aug 2, 2022
- || Zontivity (vorapaxar) / Merck (MSD), Tracleer (bosentan) / J&J, Roche
Review, Journal: Review new concepts in pharmacotherapy for peripheral arterial disease. (Pubmed Central) - Jun 29, 2022
Personalized management, identification of risk factors and shared-decision making are crucial in improving the best medical therapy for patients with PAD. Further studies are needed to assess the long-term safety and efficacy of novel strategies in real-world patients.
- Zontivity (vorapaxar) / Merck (MSD)
Thrombin receptor protease-activated receptor 1 (PAR1) related cytotoxic CD8+ T cell activity is associated with atrial myopathy and pro-inflammatory immune response in early atrial fibrillation (Research Gateway 10) - Jun 15, 2022 - Abstract #ESC2022ESC_5177;
Further studies are needed to assess the long-term safety and efficacy of novel strategies in real-world patients. Targeting the FXa/FIIa-PAR1-CD8+ axis might be a promising approach to reduce atrial fibrosis and inflammation.
- | Zontivity (vorapaxar) / Merck (MSD)
Journal: PAR4 Primarily Mediates Thrombin-induced Morphological Changes in MEG-01 Cells through PI3K/Akt and RhoA/ROCK Signaling Pathways. (Pubmed Central) - May 14, 2022
Selective blockade of PAR1 and PAR4 by vorapaxar and BMS-986120, respectively, indicated that PAR4 activation primarily mediates thrombin-induced morphological changes in MEG-01 cells...As in the platelets, PAR4-mediated signaling pathways are significant in thrombin-induced morphological changes in MEG-01 cells. Based on the close similarity to thrombin-induced signaling in platelets, MEG-01 cell line is a useful complementary in vitro model that can be used in research on platelets and thrombosis.
- Zontivity (vorapaxar) / Merck (MSD)
Thrombin and ADP pathways of platelet aggregation are dysregulated in participants with diabetes in the Framingham Heart Study (ExCel Center, ICC Capital Suite Room 10&11) - May 13, 2022 - Abstract #ISTH2022ISTH_846;
Participants with diabetes (N=351) were significantly older (60.1±8.5 vs 53.8±9.2 years, P=1.39E-15) and had greater aspirin use (38.7% vs 19.5%). As expected, fasting blood glucose (P=2.38E-38) and HbA1c (P=1.98E-53) were significantly greater in those diagnosed with diabetes.
- | Zontivity (vorapaxar) / Merck (MSD)
Journal: Lead Optimization to Advance Protease-Activated Receptor-1 Antagonists in Early Discovery. (Pubmed Central) - Apr 19, 2022
Toward this goal, extensive structure-activity relationship studies using a C-ring-truncated version of Vorapaxar culminated in the discovery of three leads, represented as 13, 14, and 23. Among these leads, compound 14 possessed favorable pharmacokinetic properties and an off-target profile, which supported additional profiling in an exploratory rat toxicology study.
- | Kengreal (cangrelor) / Chiesi, Zontivity (vorapaxar) / Merck (MSD)
Journal: Protease-activated receptor antagonists prevent thrombosis when dual antiplatelet therapy is insufficient in an occlusive thrombosis microfluidic model. (Pubmed Central) - Apr 19, 2022
We then investigated whether the PAR1 antagonist vorapaxar or the PAR4 antagonist BMS 986120, alone or in combination with DAPT, prevented occlusive thrombosis...However, occlusive thrombosis was prevented by combining DAPT with PAR antagonism. These data demonstrate that PAR antagonists may be a useful addition to DAPT in some patients and further demonstrate the utility of in vitro models of occlusive thrombosis.
- | Kengreal (cangrelor) / Chiesi, Zontivity (vorapaxar) / Merck (MSD)
Journal: Potential antiviral properties of antiplatelet agents against SARS-CoV-2 infection: an in silico perspective. (Pubmed Central) - Mar 23, 2022
At the same time, vorapaxar, ticagrelor, and cilostazol are the best binders of the spike protein. Therefore, these compounds could be successful candidates against COVID-19 that need to be tested experimentally.
- | Zontivity (vorapaxar) / Merck (MSD)
Journal: Vorapaxar for Prevention of Major Adverse Cardiovascular and Limb Events in Peripheral Artery Disease. (Pubmed Central) - Mar 12, 2022
Vorapaxar, used in addition to aspirin, has demonstrated robust reductions in MACE and MALE in PAD patients. In this article, we provide a contemporary review of the current state of PAD and the role of antithrombotic medications in the treatment of PAD, as well as the current clinical data on vorapaxar and strategies to integrate vorapaxar into contemporary medical management of peripheral artery disease.
- || Zontivity (vorapaxar) / Merck (MSD)
Clinical, Journal: No benefit of vorapaxar on walking performance in patients with intermittent claudication. (Pubmed Central) - Mar 11, 2022
P4
This study found no benefit of vorapaxar in patients with IC and reiterates the need for future drug therapy studies that expand the benefits of supervised exercise therapy in patients with IC. ClinicalTrials.gov Identifier: NCT02660866.
- | Zontivity (vorapaxar) / Merck (MSD)
Journal: Lack of miRNA-17 family mediates high glucose-induced PAR-1 upregulation in glomerular mesangial cells. (Pubmed Central) - Feb 19, 2022
We found that high glucose stimulated proliferation of the mesangial cells whereas PAR-1 inhibition with vorapaxar attenuated the cell proliferation...So miR-20a was selected to confirm the role of miR-17 family on PAR-1 upregulation, finding that miR-20a-5p overexpression reversed the upregulation of PAR-1 in mRNA and protein levels induced by high glucose in HMCs. In summary, our finding indicated that PAR-1 upregulation mediated proliferation of glomerular mesangial cells induced by high glucose, and deficiency of miR-17 family resulted in PAR-1 upregulation.
- | Zontivity (vorapaxar) / Merck (MSD)
Journal: PAR4-Mediated PI3K/Akt and RhoA/ROCK Signaling Pathways Are Essential for Thrombin-Induced Morphological Changes in MEG-01 Cells. (Pubmed Central) - Feb 5, 2022
Treatment of a set of kinase inhibitors and 2-aminoethoxydiphenyl borate (2-APB) revealed that thrombin-mediated morphological changes were primarily regulated by calcium-independent pathways and PAR4 activation-induced PI3K/Akt and RhoA/ROCK signaling pathways in MEG-01 cells. These results indicate the importance of PAR4-mediated signaling pathways in thrombin-induced morphological changes in MEG-01 cells and provide a useful in vitro cellular model for platelet research.
- | Zontivity (vorapaxar) / Merck (MSD)
Journal, IO biomarker: Pleiotropic Effects of the Protease-Activated Receptor 1 (PAR1) Inhibitor, Vorapaxar, on Atherosclerosis and Vascular Inflammation. (Pubmed Central) - Jan 26, 2022
These results indicate the importance of PAR4-mediated signaling pathways in thrombin-induced morphological changes in MEG-01 cells and provide a useful in vitro cellular model for platelet research. PAR1 inhibition with vorapaxar may be effective in reducing residual thrombo-inflammatory event risk in patients with atherosclerosis independent of its effect on platelets.
- || Zontivity (vorapaxar) / Merck (MSD)
Clinical, Journal: Efficacy and Safety of Vorapaxar by Intensity of Background Lipid-Lowering Therapy in Patients With Peripheral Artery Disease: Insights From the TRA2P-TIMI 50 Trial. (Pubmed Central) - Jan 19, 2022
Thrombin inhibition with vorapaxar is effective regardless of background statin therapy. These results suggest that targeting both lipid and thrombotic risk in peripheral artery disease is necessary in order to optimize outcomes.
- || picotamide (C-AM-01) / Curatis, CapiThera, Zontivity (vorapaxar) / Merck (MSD)
Retrospective data, Review, Journal: Efficacy and Safety of Antiplatelet Therapies in Symptomatic Peripheral Artery Disease: A Systematic Review and Network Meta-Analysis. (Pubmed Central) - Jan 6, 2022
This updated network meta-analysis confirms that clopidogrel significantly decreases the risk of major adverse cardiovascular events compared with aspirin, without increasing bleeding risk. Clopidogrel should remain a mainstay of PAD treatment, at least in patients at higher bleeding risk.
- | Zontivity (vorapaxar) / Merck (MSD)
FDA event, Journal: Identification of SARS-CoV-2 main protease inhibitors from FDA-approved drugs by artificial intelligence-supported activity prediction system. (Pubmed Central) - Jan 6, 2022
Six (6) compounds among the 13 positive drugs were identified for the first time by the present study. Furthermore, it was verified that vorapaxar bound to M with a K value of 27 µM by SPR method and inhibited virus replication in SARS-CoV-2 infected cells with an EC value of 11 µM.Communicated by Ramaswamy H. Sarma.
- | Zontivity (vorapaxar) / Merck (MSD)
Journal: The thrombin receptor links brain derived neurotrophic factor to neuron cholesterol production, resiliency and repair after spinal cord injury. (Pubmed Central) - Jan 4, 2022
Pharmacologic inhibition of cortical neuron PAR1 using vorapaxar in vitro also decreased PTEN and promoted neurite outgrowth in a cholesterol dependent manner, including that driven by suboptimal brain derived neurotrophic factor (BDNF)...The link between PAR1, cholesterol and BDNF was further highlighted by demonstrating that the deleterious effects of PAR1 over-activation are overcome by supplementing cultures with BDNF, cholesterol or by blocking an inhibitor of adenylate cyclase, Gαi. These findings document PAR1-linked neurotrophic coupling mechanisms that regulate neuronal cholesterol metabolism as an important component of the machinery regulating CNS repair and point to new strategies to enhance neural resiliency after injury.