Characterization of the Adenosine Pharmacology of Ticagrelor Reveals Therapeutically Relevant Inhibition of Equilibrative Nucleoside Transporter 1

Armstrong, Duncan; Summers, Claire; Ewart, Lorna; Nylander, Sven; Sidaway, James E.; Giezen, J.J.J. van

doi:10.1177/1074248413511693

Cited by 225 publications

(194 citation statements)

References 33 publications

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“…Another effect of ticagrelor is, that it increases adenosine plasma concentration in patients with ACS (128). This effect is mediated by blocking cellular uptake of adenosine through inhibition of equilibrative nucleoside transporter 1 (ENT1) (129). Adenosine is one of the key molecules that regulate numerous physiological processes by activating four G-proteincoupled adenosine receptors (ARs), A1, A2A, A2B, and A3 ARs.…”

Section: Ticagrelormentioning

confidence: 99%

Platelets, inflammation and anti-inflammatory effects of antiplatelet drugs in ACS and CAD

Müller¹,

Chatterjee²,

Rath³

et al. 2015

Thromb Haemost

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SummaryPlatelets play a pivotal role in chronic inflammation leading to progression of atherosclerosis and acute coronary events. Recent discoveries on novel mechanisms and platelet-dependent inflammatory targets underpin the role of platelets to maintain a chronic inflammatory condition in cardiovascular disease. There is strong and clinically relevant crosslink between chronic inflammation and platelet activation. Antiplatelet therapy is a cornerstone in the prevention and treatment of acute cardiovascular events. The benefit of antiplatelet agents has mainly been attributed to their direct anti-aggregatory impact. Some anti-inflammatory off-target effects have also been described. However, it is unclear whether these effects are secondary due to inhibition of platelet activation or are caused by direct distinct mechanisms interfering with inflammatory pathways. This article will highlight novel platelet associated targets that contribute to inflammation in cardiovascular disease and elucidate mechanisms by which currently available antiplatelet agents evolve anti-inflammatory capacities, in particular by carving out the differential mechanisms directly or indirectly affecting platelet mediated inflammation. It will further illustrate the prognostic impact of antiplatelet therapies by reducing inflammatory marker release in recent cardiovascular trials.

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Section: Ticagrelormentioning

confidence: 99%

Platelets, inflammation and anti-inflammatory effects of antiplatelet drugs in ACS and CAD

Müller¹,

Chatterjee²,

Rath³

et al. 2015

Thromb Haemost

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“…In addition to P2Y 12 inhibition, ticagrelor also increases extracellular adenosine levels by inhibiting the equilibrative nucleoside transporter-1. 11 As well as being an additional mechanism for the antiplatelet effects of ticagrelor, 12 the increase in local adenosine levels enhances adenosine-mediated coronary blood flow. [13][14][15] Guideline Update: NSTE-ACS The AHA/ACC Task Force on Practice Guidelines has published a 2014 update for the care of patients with NSTE-ACS.…”

Section: Pathophysiology Of Acs: the Role Of Plateletsmentioning

confidence: 99%

Acute Coronary Syndrome: Focus on Antiplatelet Therapy

Bobadilla

2016

Critical Care Nurse

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The American Heart Association/American College of Cardiology in 2014 published a focused update of the 2007 and 2012 guidelines for non–ST-segment elevation acute coronary syndrome (NSTE-ACS). The management of ST-segment elevation myocardial infarction (STEMI) is described in a separate guideline published in 2013. The focused updates to the guidelines contain updated recommendations for dual antiplatelet therapy, including use of the P2Y12 inhibitor ticagrelor, which was recently approved by the Food and Drug Administration. Nurses caring for patients with acute coronary syndrome must have a good understanding of the current treatment guidelines for such patients, to help ensure delivery of evidence-based care. This review article uses a case study–based approach to describe how the new guidelines affect clinical decision making when choosing appropriate antiplatelet therapy for patients with NSTE-ACS or STEMI, depending on the patient’s clinical history and presenting characteristics.

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“…Finally, ticagrelor induces adenosine tri-phosphate (ATP) release from human red blood cells in a dosedependent manner (13), which may contribute to increasing APL. It remains however unclear whether the off-target properties of ticagrelor, which were discovered and characterized in animals or ex vivo models (14,15), contribute to its clinical effects in humans at currently approved regimen.…”

Section: Introductionmentioning

confidence: 99%

Rationale and design of the Hunting for the off-target propertIes of Ticagrelor on Endothelial function and other Circulating biomarkers in Humans (HI-TECH) trial

Ariotti

Leeuwen

Brugaletta

et al. 2017

American Heart Journal

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Characterization of the Adenosine Pharmacology of Ticagrelor Reveals Therapeutically Relevant Inhibition of Equilibrative Nucleoside Transporter 1

Cited by 225 publications

References 33 publications

Platelets, inflammation and anti-inflammatory effects of antiplatelet drugs in ACS and CAD

Platelets, inflammation and anti-inflammatory effects of antiplatelet drugs in ACS and CAD

Acute Coronary Syndrome: Focus on Antiplatelet Therapy

Rationale and design of the Hunting for the off-target propertIes of Ticagrelor on Endothelial function and other Circulating biomarkers in Humans (HI-TECH) trial

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