Ticagrelor: a novel oral antiplatelet agent

To review the pharmacology, clinical efficacy, and tolerability of ticagrelor and to discuss implications for use in the elderly.

A literature search was conducted in MEDLINE from 1966 to July 2010 using the MESH terms and key words AZD6140, ticagrelor, P2Y12 receptor antagonist. The search was limited to studies in English language with human subjects.

Randomized controlled clinical trials were reviewed. References that were deemed relevant to pharmacodynamic/pharmacokinetic studies of P2Y₁₂ antagonists and their historical background were also included.

Ticagrelor is the first reversible oral P2Y₁₂ antagonist currently undergoing Food and Drug Administration review for approval. The advantages of ticagrelor over clopidogrel are a more rapid onset of action, offset, and reversibility at the platelet P2Y₁₂ receptor site. In the Study of Platelet Inhibition and Patient Outcomes trial, ticagrelor reduced the incidence of death as a result of cardiovascular causes, with no increase in major bleeding or bleeding related to coronary artery bypass graft (CABG) compared with clopidogrel. Subgroup analyses suggested that elderly patients may benefit more from ticagrelor than from clopidogrel. However, the increase in non-CABG-related bleeding and unique adverse events may limit ticagrelor's use in the elderly.

The use of ticagrelor in the elderly should be determined on a case-by-case basis. More studies need to be conducted prior to establishing a role in therapy for the elderly.