Pharmacokinetic drug evaluation of vorapaxar for secondary prevention after acute coronary syndrome

Expert Opin Drug Metab Toxicol. 2017 Mar;13(3):339-350. doi: 10.1080/17425255.2017.1289175. Epub 2017 Feb 7.

Abstract

Vorapaxar is the first protease-activated receptor-1 inhibitor approved for clinical use. Its main indication is the reduction in thrombotic cardiovascular events in patients with previous myocardial infarction or symptomatic peripheral artery disease. Areas covered: This article reviews the pharmacokinetics of vorapaxar and its potential use in secondary prevention after an acute coronary syndrome. Expert opinion: Vorapaxar inhibits platelet aggregation mediated by thrombin. This effect is carried out without affecting to coagulation parameters and bleeding times. This drug has showed a significant reduction of cardiovascular events in patients with chronic atherosclerosis but not during the admission for an acute coronary syndrome. The rate of major bleeding found in patients treated with vorapaxar in randomized trials was consistently higher than placebo in most of the analyzed subgroups. For this reason, cautious evaluation of risk-benefit profiles should be required before prescribing this drug.

Keywords: Acute coronary syndrome; antiplatelet; protease-activated receptor-1 inhibitor; secondary prevention; vorapaxar.

Publication types

  • Review

MeSH terms

  • Acute Coronary Syndrome / prevention & control*
  • Animals
  • Hemorrhage / chemically induced
  • Humans
  • Lactones / adverse effects
  • Lactones / pharmacokinetics*
  • Lactones / therapeutic use
  • Platelet Aggregation Inhibitors / adverse effects
  • Platelet Aggregation Inhibitors / pharmacokinetics*
  • Platelet Aggregation Inhibitors / therapeutic use
  • Pyridines / adverse effects
  • Pyridines / pharmacokinetics*
  • Pyridines / therapeutic use
  • Randomized Controlled Trials as Topic
  • Receptor, PAR-1 / antagonists & inhibitors
  • Secondary Prevention

Substances

  • Lactones
  • Platelet Aggregation Inhibitors
  • Pyridines
  • Receptor, PAR-1
  • vorapaxar