Ticagrelor (Brilinta; AstraZeneca Pharmaceuticals LP, Wilmington, DE, USA) is a direct acting, reversible, oral P2Y12 inhibitor.1) In the PLATelet inhibition and patient Outcomes (PLATO) study, compared to clopidogrel (Plavix; Bristol-Myers Squibb/Sanofi Pharmaceuticals, Bridgewater, NJ, USA), ticagrelor reduced the rate of death from vascular causes, myocardial infarction (MI), or stroke in pa...

T he PLATO trial was a phase 3, randomized, double-blind, parallel-group, multinational, clinical study comparing the efficacy of ticagrelor (formerly known as AZD6140, marketed as Brilinta) versus standard care treatment with clopi-dogrel. Patients (n=18 624) with moderate-to high-risk acute coronary syndrome undergoing coronary intervention or medically managed were randomized to ticagrelor 1...

The investigational ticagrelor-neutralizing antibody fragment, MEDI2452, is developed to rapidly and specifically reverse the antiplatelet effects of ticagrelor. However, the dynamic interaction of ticagrelor, the ticagrelor active metabolite (TAM), and MEDI2452, makes pharmacokinetic (PK) analysis nontrivial and mathematical modeling becomes essential to unravel the complex behavior of this sy...

BACKGROUND Ticagrelor provides enhanced antiplatelet efficacy but increased risk of bleeding and dyspnea. This study aimed to display the relationship between ADP-induced platelet-fibrin clot strength (MAADP) and clinical outcomes in acute coronary syndrome (ACS) patients treated by ticagrelor. METHODS Consecutive Chinese-Han patients with ACS who received maintenance dose of ticagrelor on to...

Ticagrelor [(1S,2S,3R,5S)-3-[7-[[(1R,2S)-2-(3,4-difluorophenyl) cyclopropyl]amino]-5-(propylthio)-3H-1,2,3-triazolo[4,5-d]pyrimidin-3-yl]-5-(2-hydroxyethoxy)-1,2-cyclopentanediol)] is a reversibly binding oral P2Y(12) receptor antagonist in development for the prevention of thrombotic events in patients with acute coronary syndromes. The pharmacokinetics, metabolism, and excretion of ticagrelor...

OBJECTIVES Two open-label, two-period, crossover studies in healthy volunteers were designed to determine the pharmacokinetic interactions between ticagrelor, a P2Y12 receptor antagonist, and a moderate (diltiazem) and a strong (ketoconazole) cytochrome P450 (CYP) 3A inhibitor. METHODS Seventeen volunteers received diltiazem (240 mg once daily) for 14 days. In the second study, ketoconazole (...

Novel antiplatelet drugs, including ticagrelor, are being successively introduced into the therapy of atherothrombotic conditions due to their superiority over a standard combination of clopidogrel with acetylsalicylic acid in patients with acute coronary syndromes (ACS). A P2Y12 receptor antagonist, ticagrelor, is unique among antiplatelet drugs, because ticagrelor inhibits the platelet P2Y12 ...

OBJECTIVE In a phase III clinical trial (PLATelet inhibition and patient Outcomes, PLATO), ticagrelor provided better clinical outcomes than clopidogrel in patients with acute coronary syndromes. In addition to P2Y12-receptor antagonism, ticagrelor prevents cell uptake of adenosine and has proven able to augment adenosine effects. Adenosine protects the heart against ischemia-reperfusion injury...

Objective—Our goal was to study the effects of ticagrelor on murine platelet function and thrombosis and characterize the time course of P2Y12 inhibition required to inhibit neointima formation following vascular injury. Methods and Results—Mice were treated with ticagrelor or vehicle. Platelet aggregation and P-selectin expression were assessed over time, and thrombus formation was assessed in...

BACKGROUND AND PURPOSE In patients with myocardial infarction, ticagrelor reduces cardiovascular and sepsis-related mortality, and can cause dyspnea. It is suggested that this is caused by adenosine receptor stimulation, because in preclinical studies, ticagrelor blocks the nucleoside transporter and increases cellular ATP release. We now investigated the effects of ticagrelor on the adenosine ...