A novel vitamin K derived anticoagulant tolerant to genetic variations of vitamin K epoxide reductase.

ABSTRACT:

Background

Vitamin K antagonists (VKAs), such as warfarin, have remained the cornerstone of oral anticoagulation therapy in the prevention and treatment of thromboembolism for more than half a century. They function by impairing the biosynthesis of vitamin K-dependent (VKD) clotting factors through the inhibition of vitamin K epoxide reductase (VKOR). The challenge of VKAs therapy is their narrow therapeutic index and highly variable dosing requirements, which are partially the result of genetic variations of VKOR.

Objectives

The goal of this study was to search for an improved VKA that is tolerant to the genetic variations of its target enzyme.

Methods

A series of vitamin K derivatives with benzyl and related side-chain substitutions at the 3-position of 1,4-naphthoq

SUBMITTER: Chen X 

PROVIDER: S-EPMC7925372 | biostudies-literature | 2021 Mar

REPOSITORIES: biostudies-literature