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Vitamin K antagonist(warfarin)

Joon Bum Kim · FDA-approved active Small molecule

Warfarin inhibits vitamin K-dependent clotting factors (II, VII, IX, X) by blocking the vitamin K epoxide reductase enzyme, thereby reducing thrombin generation and blood clot formation.

Warfarin inhibits vitamin K-dependent clotting factors (II, VII, IX, X) by blocking the vitamin K epoxide reductase enzyme, thereby reducing thrombin generation and blood clot formation. Used for Atrial fibrillation for stroke prevention, Venous thromboembolism (deep vein thrombosis and pulmonary embolism) treatment and prevention, Mechanical heart valve thromboprophylaxis.

At a glance

Generic nameVitamin K antagonist(warfarin)
SponsorJoon Bum Kim
Drug classVitamin K antagonist
TargetVitamin K epoxide reductase (VKORC1)
ModalitySmall molecule
Therapeutic areaCardiovascular
PhaseFDA-approved

Mechanism of action

Warfarin acts as a vitamin K antagonist by inhibiting the enzyme vitamin K epoxide reductase, which is essential for the gamma-carboxylation of vitamin K-dependent coagulation factors. This prevents the synthesis of functional clotting factors II, VII, IX, and X in the liver, leading to prolonged prothrombin time (PT/INR) and reduced thrombotic risk. The anticoagulant effect develops over several days as existing clotting factors are cleared from circulation.

Approved indications

Common side effects

Key clinical trials

Primary sources

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SourceUsed for
ClinicalTrials.govTrial enrolment, design, endpoints, results

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