Milvexian, a novel factor XIa inhibitor for stroke prevention: pharmacokinetic and pharmacodynamic evaluation

Expert Opin Drug Metab Toxicol. 2024 Sep;20(9):873-880. doi: 10.1080/17425255.2024.2399721. Epub 2024 Sep 2.

Abstract

Introduction: Antiplatelets and oral anticoagulants are commonly used to treat patients with various cardiovascular and cerebrovascular diseases. However, the primary concern for clinicians remains the risk of bleeding, thus necessitating the development of new therapies. Milvexian is a new anticoagulant that inhibits factor XIa, preventing the pathological formation of thrombi without increasing bleeding risk.

Areas covered: This drug evaluation examines the pharmacokinetic properties of milvexian and provides information on its pharmacodynamics and clinical efficacy in treating some cerebrovascular conditions.

Expert opinion: Milvexian shows a good pharmacokinetic profile with low renal elimination rates, justifying its use in patients with a high degree of renal impairment, and without relevant drug-drug interactions. In patients affected by acute non-cardioembolic ischemic stroke or high-risk transient ischemic stroke, milvexian, in addition to dual antiplatelet therapy, seems to have a positive efficacy profile without any safety concerns, especially in terms of intracranial hemorrhage. Two phase 3 trials are ongoing to investigate the efficacy and safety of milvexian for preventing cardioembolic and non-cardioembolic ischemic stroke.

Keywords: Cerebral hemorrhage; factor XIa inhibitor; ischemic stroke; major bleeding; milvexian.

Publication types

  • Review

MeSH terms

  • Animals
  • Anticoagulants* / administration & dosage
  • Anticoagulants* / adverse effects
  • Anticoagulants* / pharmacokinetics
  • Anticoagulants* / pharmacology
  • Factor XIa* / antagonists & inhibitors
  • Hemorrhage / chemically induced
  • Humans
  • Ischemic Stroke / prevention & control
  • Platelet Aggregation Inhibitors / administration & dosage
  • Platelet Aggregation Inhibitors / adverse effects
  • Platelet Aggregation Inhibitors / pharmacokinetics
  • Platelet Aggregation Inhibitors / pharmacology
  • Stroke* / prevention & control

Substances

  • Anticoagulants
  • Factor XIa
  • Platelet Aggregation Inhibitors