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Letter to the Editor

Error in Brilinta Pharmacokinetics

Naeem Khan MD

To the Editor:

AstraZeneca has identified an error in the article titled “Meeting Highlights: American College of Cardiology” in the May 2015 issue of P&T on page 361. Please refer to the comments below and the pharmacokinetics section of the Brilinta prescribing information that provide information supporting a correction of inaccurate information in the article.

The article provides a summary on “Cangrelor in Elderly Patients Undergoing PCI: Findings From CHAMPION-PHOENIX.” A quote from the study author within the summary states: “Many of the PCI drugs, like clopidogrel or ticagrelor, are prodrugs and have to be metabolized, whereas cangrelor is an intravenous drug that is basically 100% bioavailable.”

Unlike the thienopyridines (e.g., clopidogrel), Brilinta (a cyclopentyltriazolopyrimidine) is not a prodrug.13

Brilinta is orally active and it does not require hepatic metabolism to exert its pharmacological action.1,2 CYP3A4 is the major enzyme responsible for Brilinta metabolism and the formation of its active metabolite.3 The systemic exposure to the active metabolite is approximately 30%–40% of the exposure of Brilinta.

The above information should in no way be construed as a recommendation for the use of this product in any manner other than as approved by the Food and Drug Administration (FDA) and as described in the prescribing information for Brilinta. Prescribing information for FDA-approved AstraZeneca products may be obtained from www.astrazeneca-us.com or by calling the Information Center at AstraZeneca at 1-800-236-9933. For further medical information requests, please contact AstraZeneca at 1-877-893-1510.

The prescribing information for this product contains boxed warnings. Please consult the warning section of the prescribing information for further details and other important safety information.

References

  1. Husted S, Emanuelsson H, Heptinstall S, et al. Pharmacodynamics, pharmacokinetics, and safety of the oral reversible P2Y12 antagonist AZD6140 with aspirin in patients with atherosclerosis: a double-blind comparison to clopidogrel with aspirin. Eur Heart J 2006;27;(9):1038–1047.
  2. Husted S, van Giezen JJJ. Ticagrelor: the first reversibly binding oral P2Y12 receptor antagonist. Cardiovasc Ther 2009;27;(4):259–274.
  3. Brilinta (ticagrelor) prescribing information Wilmington, Delaware: AstraZeneca LP. March 2015;