Ticagrelor Resistance in Cardiovascular Disease and Ischemic Stroke

Author:

He Song1,Lin Yapeng12,Tan Quandan1,Mao Fengkai1,Chen Kejie3,Hao Junli4,Le Weidong5,Yang Jie67ORCID

Affiliation:

1. Department of Neurology, The First Affiliated Hospital of Chengdu Medical College, Chengdu 610072, China

2. International Clinical Research Center, Chengdu Medical College, Chengdu 610072, China

3. School of Public Health, Chengdu Medical College, Chengdu 610072, China

4. School of Biomedical Sciences and Technology, Chengdu Medical College, Chengdu 610072, China

5. Institute of Neurology, Sichuan Provincial People’s Hospital, University of Electronic Science and Technology of China, Chengdu 610072, China

6. Department of Neurology, Sichuan Provincial People’s Hospital, University of Electronic Science and Technology of China, Chengdu 610072, China

7. Sichuan Provincial Key Laboratory for Human Disease Gene Study, Chengdu 610072, China

Abstract

Ticagrelor, acting as a reversible platelet aggregation inhibitor of P2Y12 receptors (P2Y12R), is regarded as one of the first-line antiplatelet drugs for acute cardiovascular diseases. Though the probability of ticagrelor resistance is much lower than that of clopidogrel, there have been recent reports of ticagrelor resistance. In this review, we summarized the clinical application of ticagrelor and then presented the criteria and current status of ticagrelor resistance. We further discussed the potential mechanisms for ticagrelor resistance in terms of drug absorption, metabolism, and receptor action. In conclusion, the incidences of ticagrelor resistance fluctuated between 0 and 20%, and possible mechanisms mainly arose from its absorption and receptor action. Specifically, a variety of factors, such as the drug form of ticagrelor, gut microecology, and the expression and function of P-glycoprotein (P-gp) and P2Y12R, have been shown to be associated with ticagrelor resistance. The exact mechanisms of ticagrelor resistance warrant further exploration, which may contribute to the diagnosis and treatment of ticagrelor resistance.

Funder

National Natural Science Foundation of China

Chengdu Science and Technology Bureau

Sichuan Science and Technology Program

Publisher

MDPI AG

Subject

General Medicine

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