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Milvexian,一种新型因子 XIa 抑制剂用于预防中风:药代动力学和药效学评价。

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

机构信息

Clinical Neurology, Department of Head, Neck and Neurosciences, Udine University Hospital, Udine, Italy.

Stroke Unit, Department of Head, Neck and Neurosciences, Udine University Hospital, Udine, Italy.

出版信息

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.

摘要

简介

抗血小板药物和口服抗凝剂常用于治疗各种心脑血管疾病患者。然而,临床医生主要关注的仍然是出血风险,因此需要开发新的治疗方法。Milvexian 是一种新型抗凝剂,可抑制因子 XIa,防止血栓的病理性形成,而不增加出血风险。

涵盖领域

本药物评价研究考察了 Milvexian 的药代动力学特性,并提供了有关其在治疗某些脑血管疾病方面的药效学和临床疗效的信息。

专家意见

Milvexian 表现出良好的药代动力学特征,肾脏清除率低,这使其可用于肾功能严重受损的患者,且无相关药物相互作用。在急性非心源性缺血性卒中和高危短暂性脑缺血发作患者中,Milvexian 联合双联抗血小板治疗似乎具有积极的疗效,且无安全性问题,特别是在颅内出血方面。两项 3 期临床试验正在进行中,以研究 Milvexian 预防心源性和非心源性缺血性卒中的疗效和安全性。

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