Approved: July 20, 2011 
Brilinta is a reversible inhibitor of platelet aggregation and works by binding to the
adenosine diphosphate (ADP) P2Y12 receptor on the surface of the platelets
 . The PLATO trial demonstrated
Brilinta superiority over Plavix in heart attack and death prevention. This, however, was seen
when Brilinta was combined with aspirin doses of <100 mg . One
stipulation of Brilinta’s approval was a boxed warning mandated by the FDA stating:
“Maintenance doses of aspirin above 100 mg reduce the effectiveness of Brilinta ”.
Brilinta is the first reversible oral P2Y12 receptor antagonist. The
irreversible binding of Plavix exhibits in a slow offset with a gradual recovery of platelet
function. Consequently, the effects of Plavix will last about 3-5 days after the drug is
stopped due to the lifetime of the platelets . Plavix is a prodrug that requires a
two-step metabolic conversion to its active metabolite. Due to this process, the onset of action is
relatively slow. In contrast, Brilinta is not a prodrug and does not require metabolic
activation to inhibit the P2Y12 receptor. Both Brilinta and Plavix undergo
metabolism by CYP enzymes, resulting in formation of additional active metabolites. Plavix is
primarily metabolized through 2C19 whereas Brilinta uses the more common 3A4 pathway.
Involvement of the 3A4 pathway increases the risk for statin related adverse effects with doses of
more than 40mg a day of either simvastatin or lovastatin. Monitoring of patient’s digoxin
levels while on Brilinta is extremely important to avoid possible digoxin toxicity with initiation
or change in Brilinta therapy , . The most common non hemorrhagic
event was dyspnea. This was significantly higher than Plavix (13.8% versus 7.8%)
. The PLATO
study showed that acute coronary syndrome patients treated with Brilinta had significantly decreased
rates of death from vascular causes, myocardial infarction, or stroke versus Plavix . The rates of major bleeding were not different
between the two treatment groups. However, there were significantly more patients in the
Birlinta group with intracranial bleeding (p=0.06) . Plavix has more convenient once daily dosing and is also ~ 20% cheaper.
Plavix costs around $5.66/ day and Brilinta around $7.24/day.
Will Brilinta find a place in therapy? Time will tell with the generic of Plavix,
clopidogrel, due out in May of 2012 after being granted an additional 6 months to their patent due
to pediatric exclusivity  .
- "Brilinta." Daily
Med. NIH, 20 July 2011. Web. 8 Aug. 2011.
FDA. US Department of Health and Human Services, July 2011. Web. 8 Aug. 2011.
- James, S., A. Akerblom, C. P.
Cannon, et. al. "Comparison of Ticagrelor, the First Reversible Oral P2Y(12) Receptor
Antagonist, with Clopidogrel in Patients with Acute Coronary Syndromes: Rationale, Design, and
Baseline Characteristics of the PLATelet Inhibition and Patient Outcomes (PLATO) Trial."
American Heart Journal 157.4 (2009): 599-605. Print.
- Goodman, Louis S., Alfred
Gilman, Laurence L. Brunton, John S. Lazo, and Keith L. Parker. "Clopidogrel."
Goodman & Gilman's the Pharmacological Basis of Therapeutics. 11th ed. New York:
McGraw-Hill, 2006. 1483. Print.
DailyMed. FDA, Sept. 2009. Web. 08 Aug. 2011.
- Wallentin L, Becker RC, Budaj A, et al. Ticagrelor versus clopidogrel in
patients with acute coronary syndromes.
N Engl J Med 2009;361:1045-57.
- "AstraZeneca's Brilinta
Drug Priced Above Plavix In US - WSJ.com." Business News & Financial News -
The Wall Street Journal - Wsj.com. Wall Street Journal, 28 July 2011. Web. 08 Aug. 2011.
- Bristol-Myers Squibb and
Sanofi-aventis Announce U.S. FDA Decision to Grant Pediatric Exclusivity For
Bristol-Myers Squibb. 25 Jan. 2011. Web. 8 Aug. 2011.