Top

Published in:

01-10-2012

Pharmacodynamic effects of EV-077: results of an in vitro pilot investigation in healthy volunteers

Authors: Antonio Tello-Montoliu, Fabiana Rollini, Bhaloo Desai, Giuseppe Pasqualino, Ronakkumar Patel, Alexandra Santana Sorensen, Kjell S. Sakariassen, Dominick J. Angiolillo

Published in: Journal of Thrombosis and Thrombolysis | Issue 3/2012

Excerpt

Antiplatelet agents are important for the treatment of patients with atherosclerotic disease manifestations. Antiplatelet agents act by inhibiting platelet activation and aggregation processes, which are mediated by several activating factors including thromboxane A2 (TxA₂), adenosine diphosphate (ADP), and thrombin. In particular, TxA₂ induced platelet activation is a pivotal pharmacological target as supported by the undisputable benefit of aspirin in secondary prevention of ischemic events [1, 2]. …

Ueno M, Kodali M, Tello-Montoliu A, Angiolillo DJ (2011) Role of platelets and antiplatelet therapy in cardiovascular disease. J Atheroscler Thromb 18:431–442PubMedCrossRef

Moncada S, Vane JR (1978) Pharmacology and endogenous roles of prostaglandin endoperoxides, thromboxane A2, and prostacyclin. Pharmacol Rev 30:293–331PubMed

Hanson J, Rolin S, Reynaud D, Qiao N, Kelley LP, Reid HM, Valentin F, Tippins J, Kinsella BT, Masereel B, Pace-Asciak C, Pirotte B, Dogné JM (2005) In vitro and in vivo pharmacological characterization of BM-613[N-n-pentyl-N′-[2-(4′-methylphenylamino)-5-nitrobenzenesulfonyl]urea], a novel dual thromboxane synthase inhibitor and thromboxane receptor antagonist. J Pharmacol Exp Ther 313:293–301PubMedCrossRef

Patrono C, García Rodríguez LA, Landolfi R, Baigent C (2005) Low-dose aspirin for the prevention of atherothrombosis. N Engl J Med 353:2373–2383PubMedCrossRef

Sakariassen KS, Alberts P, Fontana P, Mann J, Bounameaux H, Sorensen AS (2009) Effects of pharmaceutical interventions targeting thromboxane receptors and thromboxane synthase in cardiovascular and renal diseases. Fut Cardiol 5:479–493CrossRef

Pratico D (2008) Prostanoid and isoprostanoid pathways in atherogenesis. Atherosclerosis 201:8–16PubMedCrossRef

Fontana P, Alberts P, Sakariassen KS, Bounameaux H, Meyer JP, Sorensen AS (2011) The dual thromboxane receptor antagonist and thromboxane synthase inhibitor EV-077 is a more potent inhibitor of platelet function than aspirin. J Thromb Haemost 9:2109–2111PubMedCrossRef

Sakariassen KS, Muggli R, Baumgartner HR (1989) Measurements of platelet interaction with components of the vessel wall in flowing blood. Methods Enzymol 169:37–70PubMedCrossRef

Tello-Montoliu A, Ueno M, Angiolillo DJ (2011) Antiplatelet drug therapy: role of pharmacodynamic and genetic testing. Fut Cardiol 7:381–402CrossRef

10.

Angiolillo DJ (2009) Variability in responsiveness to oral antiplatelet therapy. Am J Cardiol 103:27A–34APubMedCrossRef

11.

Cipollone F, Rocca B, Patrono C (2004) Cyclooxygenase-2 expression and inhibition in atherothrombosis. Arterioscler Thromb Vasc Biol 24:246–255PubMedCrossRef

12.

Cayatte AJ, Du Y, Oliver-Krasinski J, Lavielle G, Verbeuren TJ, Cohen RA (2000) The thromboxane receptor antagonist S18886 but not aspirin inhibits atherogenesis in apo E-deficient mice: evidence that eicosanoids other than thromboxane contribute to atherosclerosis. Arterioscler Thromb Vasc Biol 20:1724–1728PubMedCrossRef

13.

Roger S, Pawlowski M, Habib A, Jandrot-Perrus M, Rosa JP, Bryckaert M (2004) Costimulation of the Gi-coupled ADP receptor and the Gq-coupled TXA2 receptor is required for ERK2 activation in collagen-induced platelet aggregation. FEBS Lett 556:227–235PubMedCrossRef

Title: Pharmacodynamic effects of EV-077: results of an in vitro pilot investigation in healthy volunteers
Authors: Antonio Tello-Montoliu
Fabiana Rollini
Bhaloo Desai
Giuseppe Pasqualino
Ronakkumar Patel
Alexandra Santana Sorensen
Kjell S. Sakariassen
Dominick J. Angiolillo
Publication date: 01-10-2012
Publisher: Springer US
Published in: Journal of Thrombosis and Thrombolysis / Issue 3/2012
Print ISSN: 0929-5305
Electronic ISSN: 1573-742X
DOI: https://doi.org/10.1007/s11239-012-0795-6

Live Webinar | 27-06-2024 | 18:00 (CEST)

Keynote webinar | Spotlight on medication adherence

Reserve your place

Live: Thursday 27th June 2024, 18:00-19:30 (CEST)

WHO estimates that half of all patients worldwide are non-adherent to their prescribed medication. The consequences of poor adherence can be catastrophic, on both the individual and population level.

Join our expert panel to discover why you need to understand the drivers of non-adherence in your patients, and how you can optimize medication adherence in your clinics to drastically improve patient outcomes.

Prof. Kevin Dolgin

Prof. Florian Limbourg

Prof. Anoop Chauhan

Developed by: Springer Medicine

Obesity Clinical Trial Summary

At a glance: The STEP trials

A round-up of the STEP phase 3 clinical trials evaluating semaglutide for weight loss in people with overweight or obesity.

Developed by: Springer Medicine

Keynote webinar | Spotlight on medication adherence

Springer Medicine

Excerpt

Please log in to get access to this content

Other articles of this Issue 3/2012

Systemic thrombolysis for acute, severe Budd-Chiari syndrome

The in vitro effects of verbascoside on human platelet aggregation

The clinical significance of JAK2V617F mutation for Philadelphia-negative chronic myeloproliferative neoplasms in patients with splanchnic vein thrombosis

Effects on platelet function of a direct acting antagonist of coagulation factor Xa

Paradoxical thrombosis, part 2: anticoagulant and antiplatelet therapy

The relationship between intracranial arterial stenosis and glomerular filtration rate

Keynote webinar | Spotlight on medication adherence

Live: Thursday 27th June 2024, 18:00-19:30 (CEST)

At a glance: The STEP trials