Drug intelligence / Profile preview

diphenadione

Development stage
Unknown
Modality
Light/Condition-Responsive Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral, Topical, Inhalation
01

Overview

Diphenadione is a synthetic indandione anticoagulant and vitamin K antagonist primarily used as a rodenticide to control rats, mice, voles, ground squirrels, and other rodents. It acts by inhibiting the synthesis of vitamin K-dependent clotting factors in the liver, leading to impaired blood coagulation and ultimately causing death from internal bleeding. Diphenadione has a longer half-life than warfarin and other first-generation anticoagulants, making it more persistent in animal tissues. It is considered highly toxic to mammals—including humans—by all routes of exposure. In addition to its use in rodent control worldwide, it has also been used in South America for controlling vampire bat populations[1][4][7]. The primary mechanism of action is inhibition of prothrombin formation via antagonism of vitamin K[1][5][7].

Other names
Diphacinone
02

Targets

VKORC1 (Vitamin K epoxide reductase complex subunit 1)

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