Brilinta

BrilintaTM - Ticagrelor
Manufacturer: AstraZeneca
FDA Approval Date: 7/20/2011
Clinical Application
Indications:
In conjunction with aspirin, secondary prevention of thrombotic events in patients with unstable angina, NSTEMI, or STEMI managed medically or with PCI and or CABG
Place in therapy:
Patients in need of secondary prevention of thrombotic events after ACS
Contraindications:
Severe hepatic impairment Active pathological bleeding Intracranial Hemorrhage
Black Box Warnings:

Increased major/fatal bleeding risk Aspirin > 100 mg decreases ticagrelor efficacy
Precautions:
Caution with CYP3A4 inhibitors/inducers
Pregnancy:
Category C
Lactation:
Use not recommended
Drug Facts
Pharmacology: Non-thienopyridine, cyclopentyltriazolopyrimidine antiplatelet agent; selectively and reversibly binds to platelet P2Y12 class of ADP receptors, which prevents ADP mediated activation of the GPIIb/IIIa receptor complex, reducing platelet aggregation.
Drug Facts
Pharmacokinetics
A bioavailability ~ 36%, Tmax active metabolite ~ 2.6 hrs D Vd ~ 87.5L, > 99% protein-bound M oxidative metabolism primarily by CYP3A4 E Feces 58%, urine < 1% of partent and active metabolite from total dose administered, t ~ 7-9 hrs (parent and active metabolite)
Drug Interactions
Drug Interactions Object Drugs
Digoxin ( 40%) Simvastatin ( 60%)
Drug Interactions
Drug Interactions Precipitant Drugs
Strong CYP3A inhibitors: ticagrelor 7-fold Strong CYP3A inducers: ticagrelor 86%
Aspirin 75-100 mg: increased ticagrelor effect

Aspirin > 100 mg: decreased ticagrelor effect
Adverse Effects
Common Adverse Effects (ticagrelor%)[clopidogrel%]
Dyspnea: (13.8) [7.8] Headache: (6.5) [5.8] AF: (4.2) [4.6]
Serious Adverse Effects (ticagrelor%)[clopidogrel%]

Major Bleeding: (4.5) [3.8] Fatal/Life-threatening Bleeding: (2.1) [1.9]
Monitoring Parameters
Efficacy Monitoring
None
Toxicity Monitoring
CBC Signs of bleeding Renal function Uric acid Signs of dyspnea
Prescription Information
Dosing: Loading dose 180 mg, then 90 mg twice daily
Cost $217 (www.fiercepharma.com) accessed 08/22/2011
Literature Review: PLATO

DB, RCT of patients with ACS Ticagrelor (N = 9333); clopidogrel (N = 9291); 72% male, 92% Caucasian, 43% > 65 years of age Both given in combination with aspirin Treatment period = at least 6 months, but no more than 12 months
Canon CP, et al. Lancet. 2010;375(9711):283-93.

Primary Endpoint: Composite of first occurrence of CV death, non-fatal MI, or non-fatal stroke
Median exposure to ticagrelor = 277 days
Summary
Ticagrelor, Brilinta, is indicated for patients who have experienced an ACS requiring anticoagulation for prevention of thrombotic events. Ticagrelor should be dosed 180 mg loading dose followed by 90 mg twice daily administered with a dose of aspirin within the range of 75 100 mg daily. Ticagrelor does not require hepatic metabolism to its active metabolite, and may require less time for discontinuation if medically necessary. Compared to clopidogrel, ticagrelor is associated with fewer thrombotic events, MI, and overall mortality. However, ticagrelor is associated with increased risk of major bleeding and dyspnea.
References
1. 2. 3. 4. http://www.brilinta.com Brilinta package insert. AstraZeneca. Jul. 2011. Koval PG. The use of drug x in the treatment of a condition. Drugs 2009;23:2009-21. Cannon CP, et al. Comparison of ticagrelor with clopidogrel in patients with a planned invasive strategy for acute coronary syndromes (PLATO): a randomised double-blind study. Lancet. 2010;375(9711):283-93. Teng R, et al. Pharmacokinetics, pharmacodynamics, tolerability and safety of single ascending doses of ticagrelor, a reversibly binding oral P2Y(12) receptor antagonist, in healthy subjects. Eur J Clin Pharmacol. 2010;66(5):487-96. Cannon CP, et al. Safety, tolerability, and initial efficacy of AZD6140, the first reversible oral adenosine diphosphate receptor antagonist, compared with clopidogrel, in patients with non-ST-segment elevation acute coronary syndrome: primary results of the DISPERSE-2 trial. J Am Coll Cardiol. 2007;50(19):1844-51. Crouch MA, et al. P2Y12 receptor inhibitors: integrating ticagrelor into the management of acute coronary syndrome. Ann Pharmacother. 2011:45 [published online].
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BrilintaTM - Ticagrelor

FDA Approval Date: 7/20/2011

Black Box Warnings:

Aspirin 75-100 mg: increased ticagrelor effect

Serious Adverse Effects (ticagrelor%)[clopidogrel%]

Literature Review: PLATO

Literature Review: PLATO

Canon CP, et al. Lancet. 2010;375(9711):283-93.

Literature Review: PLATO

Canon CP, et al. Lancet. 2010;375(9711):283-93.

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