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January 26, 2014Cardiovascular ResearchOpen Access

Inhibiting thrombosis without causing bleeding: can EP3 blockers fulfil the dream?

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Key result

Blocking the EP3 receptor with DG-041 reduced thrombosis in murine models without impairing hemostasis, though theoretical risks of bleeding and systemic side effects remain.

Why the study?

Does blocking the EP3 receptor with DG-041 reduce thrombosis without causing bleeding?

Population

Murine models of thrombosis and healthy humans

Design

Editorial

Authors

RCRaffaele De Caterina

Discussion

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Member takes

Overview

EP3 blockade merits human translation studies; leaves open confirmation of hemostatic safety and systemic effects.

Structured PICO

Does blocking the EP3 receptor with DG-041 reduce thrombosis without causing bleeding?

P
Population
Murine models of thrombosis (triggered by arachidonic acid, ferric chloride, or scratching atherosclerotic plaques) and healthy humans (as discussed from the referenced study)
I
Intervention
DG-041 (EP3 receptor blocker)
O
Outcome
Thrombosis reduction and bleeding timesurrogate

The editorial highlights the potential of EP3 receptor blockade with DG-041 to decouple antithrombotic efficacy from bleeding risk, while cautioning about theoretical systemic limitations.

Limitations

  • Inhibited platelets could theoretically still lead to bleeding at remote injury sites.
  • PGE2 production is susceptible to inhibition by COX inhibitors, potentially abrogating effects.
  • Ubiquitous nature of EP3 receptors may lead to untoward effects in other organs or systems.
  • Inhibited platelets might still lead to bleeding at remote injury sites
  • Primary agonist PGE2 is susceptible to inhibition by COX inhibitors
  • Ubiquitous nature of EP3 may lead to untoward effects in other organs

Cite This Study

Raffaele De Caterina (2014) conducted an editorial in Thrombosis. EP3 receptor blocker (DG-041) was evaluated. Blocking the EP3 receptor with DG-041 reduced thrombosis in murine models without impairing hemostasis, though theoretical risks of bleeding and systemic side effects remain.

synapsesocial.com/papers/6a9460bbd1fa461db0c57780https://doi.org/10.1093/cvr/cvu020
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Also Consider

Synapse has enriched 5 closely related papers on similar clinical questions. Consider them for comparative context:

  1. 1Blocking the EP3 receptor for PGE2 with DG-041 decreases thrombosis without impairing haemostatic competence2013 · 53 citations
  2. 2Blocking the receptor EP3 to PGE2 as a way to safely prevent atherothrombosis2016
  3. 3Antagonists of the EP<sub>3</sub> Receptor for Prostaglandin E<sub>2</sub> Are Novel Antiplatelet Agents That Do Not Prolong Bleeding2009 · 69 citations
  4. 4DG-041 inhibits the EP3 prostanoid receptor—A new target for inhibition of platelet function in atherothrombotic disease2008 · 68 citations
  5. 5Effects on platelet function of an EP3 receptor antagonist used alone and in combination with a P2Y12antagonist bothin-vitroandex-vivoin human volunteers2012 · 32 citations